Freeze drying or lyophilization of aqueous solutions is widely used in pharmaceutical industry. The in-creased importance Of the process is gaining a worldwide interest of research. A growing body of literature has de...Freeze drying or lyophilization of aqueous solutions is widely used in pharmaceutical industry. The in-creased importance Of the process is gaining a worldwide interest of research. A growing body of literature has demonstrated that the scientific approach can result in improved product quality with minimum trial and error em-piricism. Formulation and process development need a systematical understanding of the physical chemistry of freezing and freeze drying, material science and mechanisms of heat and mass transfer. This paper presents an overview on freeze ding of aqueous solutions based on publications in the past few decades. The important issuesof the process are analyzed.展开更多
The cultivation and management of different legume species and their varieties were tested in South-Western Finland at farmers' fields in two years, 2010 and 2011. The studied legumes were peas and lava beans, and in...The cultivation and management of different legume species and their varieties were tested in South-Western Finland at farmers' fields in two years, 2010 and 2011. The studied legumes were peas and lava beans, and included also such species which are seldom or not normally cultivated in Finland, namely soybeans and blue and white lupins. Seed samples were collected from legume farms. The quality of different legume species was analysed and compared to each others. The chemical qualities were analysed for crude protein, fat, fibre, ash, nitrogen-free extract and phytic acid contents, and amino acid composition. The quality of the varieties of lupins and soybeans were compared to the quality of pea and fava bean varieties, which are generally cultivated nowadays in Finland. The highest protein contents were in soybean (369 and 379 g kg^-1) and white lupin (382 g kg^-1) and the lowest in pea varieties. Amino acid composition of legumes is good, but lupins have lower lysine content (g 100 g^-1 protein) than other legumes. High fat contents were in soybeans (91 and 100 g kg^-1) and white lupin (101 g kgl), and moderate in blue lupin (30-49 g kg^-1). Fuego fava bean variety had lower protein content than Kontu. The highest phytic acid contents were in soybeans (18.9 and 22.6 mg kg^-1) and the lowest in white lupin (6.2 mg kg^-1). Lupins are interesting protein crops, especially white lupin with high protein and fat and low phytic acid contents. Lupins are not day length sensitive, like soybean, and therefore valuable for long-day cultivation conditions The present research strengthens the good chemical quality of legumes for food and feed purposes.展开更多
In order to study the effects of chemical osmotic pretreatment on the characteristics and quality of blueberry under hot air drying,fresh blueberries were pretreated with 2.5 g/100 mL K2CO3+0.6 g/100 mL olive oil,and ...In order to study the effects of chemical osmotic pretreatment on the characteristics and quality of blueberry under hot air drying,fresh blueberries were pretreated with 2.5 g/100 mL K2CO3+0.6 g/100 mL olive oil,and 5.0 g/100 mL K2CO3+0.6 g/100 mL olive oil at(45±0.5)℃,respectively.The changes of water content,rehydration,hardness,microstructure,color difference,active ingredient anthocyanin,total phenol and DPPH radical scavenging capacity of dried blueberries in different treatment groups under hot air drying were compared and analyzed.The results showed that the dehydration rates of blueberries vary greatly according to the type of pretreatments when the samples were dried to the same water content with hot air.Specifically,the dehydration rate of dried blueberries pretreated by 5.0%K2CO3 solution was the highest,followed by 2.5%K2CO3 osmotic pretreatment and lastly the control group;the corresponding dehydration time was 10,14 and 20h,respectively.The physical qualities of dried blueberries,involving the browning degree,color difference,rehydration and microstructure,were significantly different between the chemical osmotic pretreatment group and the control group(P<0.05).The chemical osmotic pretreatment of K2CO3 solution increased the dehydration rate of the samples,shortened the drying time and maintained the quality of blueberries dried with hot air.There was no significant difference between the physical quality of dried blueberries pretreated by 2.5%and 5.0%K2CO3 solution(P>0.05),whereas there was significant difference in drying time and nutrient quality which is characterized by total phenols,anthocyanins,DPPH radical scavenging rate,soluble total sugar(P<0.05).Conclusion:5.0%K2CO3 osmotic pretreatment combining with hot air drying can improve the dehydration rate,shorten the drying time and maintain the physical and nutritional quality.展开更多
Cucumeropsis mannii, an underutilized oil seed was processed into raw full fat and defatted seed flours and its chemical, functional properties and anti-nutritional factors were determined using standard techniques. T...Cucumeropsis mannii, an underutilized oil seed was processed into raw full fat and defatted seed flours and its chemical, functional properties and anti-nutritional factors were determined using standard techniques. The effects of sample concentration and pH on the foaming properties of the seed flours were determined. The results showed that the full fat and defatted seed flours contained the following in g/100 g sample; 5.0 and 5.1; 45.8 and 1.0; 39.4 and 78.7; 3.45 and 4.40; 1.50 and 3.05; 4.85 and 7.75 for moisture, crude fat, protein, ash, crude fibre and carbohydrate, respectively. The most abundant mineral elements in the seed flour (mg/100 g) are potassium (198.5), followed by nickel (30.0) and magnesium (28.4). The water absorption capacity, oil absorption capacity, foaming capacity and stability, least gelation concentration, emulsion capacity and bulk density are 55.5% and 125.0%; 128.8% and 184.0%; 10.5% and 17.0%; 3.0% and 1.5%; 16.0% and 10.0 g/mL; 85.0 and 115.0 mL/g; 0.42 and 0.25 g/mL, respectively. Defatting influenced the functional properties. The foaming capacity is dependent on sample concentration and pH. The protein solubility of the full fat and defatted seed flours was minimum between pH 3 and 4 and maximum at pH 11. The anti-nutritional composition of the seed flour revealed the following: tannic acid, 1.54 mg/100 g; phytin phosphorus, 0.70 rag/g; phytic acid, 2.48 mg/g; oxalate, 1.85 mg/g; alkaloids 1.97% and saponin 0.50%. The seed flours (full fat and defatted) have potential as nutrient supplement, thickeners and emulsifiers in food system.展开更多
The pyrolysis of isopsoralen was studied by synchrotron vacuum ultraviolet photoionization mass spectrometry at low pressure. The pyrolysis products were detected at different photon energies, the ratios of products t...The pyrolysis of isopsoralen was studied by synchrotron vacuum ultraviolet photoionization mass spectrometry at low pressure. The pyrolysis products were detected at different photon energies, the ratios of products to precursor were measured at various pyrolysis temperatures. The experimental results demonstrate that the main pyrolysis products are primary CO and sequential CO elimination products (C10H602 and C9H60). The decomposition channels of isopsoralen were also studied by the density functional theory, then rate constants for competing pathways were calculated by the transition state theory. The dominant decom- position channels of isopsoralen and the molecular structures for corresponding products were identified by combined experimental and theoretical studies.展开更多
AIM:To explore the therapeutic effects of Morinda officinalis capsules(MOP) on osteoporosis in ovariectomized rats.METHOD:Six-month-old female Sprague–Dawley rats were induced for postmenopausal osteoporosis(PMOP) by...AIM:To explore the therapeutic effects of Morinda officinalis capsules(MOP) on osteoporosis in ovariectomized rats.METHOD:Six-month-old female Sprague–Dawley rats were induced for postmenopausal osteoporosis(PMOP) by bilateral ovariectomy and divided into seven groups as follows:sham-operated group,ovariectomized(OVX) control group,OVX treated with xianlinggubao(XLGB)(270 mg·kg-1·d-1),OVX treated with alendronate sodium(ALN)(3 mg·kg-1·d-1),and OVX treated with Morinda officinalis capsule(MOP) of graded doses(90,270 and 810 mg·kg-1·d-1) groups.Oral treatments were administered daily on the 4th week after ovariectomy and lasted for 12 weeks.The bone mineral density was evaluated by dual-energy X-ray absorptiometry.The tartrate-resistant acid phosphatase(TRAP),alkaline phosphatase(AKP),and osteocalcin(OC) levels in the serum and plasma were determined by standard colorimetric and enzyme immunoassays methods.Bone biomechanical properties and morphological parameters were analyzed by three-point bending test and histomorphometry respectively.RESULTS:Morinda officinalis capsules at all doses were able to significantly prevent the OVX-induced loss of bone mass due to diminishing serum AKP and TRAP levels while elevating OC level in the plasma.Morinda officinalis capsules also enhanced the bone strength and prevented the deterioration of trabecular microarchitecture.CONCLUSION:Morinda officinalis capsules possess potent anti-osteoporotic activity in OVX rats which could be an effective treatment for postmenopausal osteoporosis.展开更多
AIM: To profile the chemical constituents in Jinqi Jiangtang tablets. METHOD: Based on the chromatographic retention behavior, fragmentation patterns of chemical components, and published lit- eratures, a high-perfo...AIM: To profile the chemical constituents in Jinqi Jiangtang tablets. METHOD: Based on the chromatographic retention behavior, fragmentation patterns of chemical components, and published lit- eratures, a high-performance liquid chromatography coupled with electrospray ionization quadrnpole time-of-flight tandem mass spectrometry (HPLC-ESI-Q-TOF/MS) method was established to characterize and identify components in Jinqi Jiangtang tablets. RESULTS: A total of 52 chemical compounds, including eight iridoid glycosides, seven phenolic acids, twelve alkaloids, six fla- vonoids, and nineteen saponins, were identified in Jinqi Jiangtang tablets. CONCLUSION: The established method could serve as a powerful tool for structural characterization and quality control of this Chinese herbal preparation.展开更多
AIM:To investigate the chemical constituents of the roots of Polygala sibirica L.(Polygalaceae) METHOD:The isolation was performed by solvent extraction and various chromatographic techniques,including silica gel,Seph...AIM:To investigate the chemical constituents of the roots of Polygala sibirica L.(Polygalaceae) METHOD:The isolation was performed by solvent extraction and various chromatographic techniques,including silica gel,Sephadex LH-20,ODS,semi-preparative HPLC,and preparative TLC.The chemical structures were elucidated based on extensive spectroscopic analysis,including HR-ESI-MS and 1D- and 2D-NMR spectroscopic data.RESULTS:A total of sixteen compounds,including five xanthones(5,7–10),five saccharide esters(1,3,4,12,13),two flavonoids(14,16),two triterpenoids(11,15),one phenylpropanoid(6),and one benzophenone glycoside(2) were isolated.Their structures were determined as sibiricose A7(1),sibiriphenone A(2),polygalatenoside A(3),polygalatenoside C(4),lancerin(5),3,4,5-trimethoxycinnamic acid(6),6-hydroxy-1,2,3,7-tetramethoxyxanthone(7),1,3,7-trihydroxy-2-methoxyxanthone(8),onjixanthone II(9),1,2,3,6,7-pentamethoxyxanthone(10),presenegenin(11),3'-O-3,4,5-trimethoxycinnamoyl-6-O-4-methoxy benzoyl sucrose(12),tenuifoliside C(13),5,3'-dihydroxy-7,4'-dimethoxyflavonol-3-O-β-D-glucopyranoside(14),tenuifolin(15),and rhamnetin 3-O-β-D-glucopyranoside(16).CONCLUSION:Compounds 1 and 2 are two new compounds from P.sibirica.展开更多
AIM:This study was designed to evaluate the anti-cancer actions of tanshinone I and tanshinone IIA,and six derivatives of tanshinone IIA on normal and cancerous colon cells.Structure activity relationship(SAR) analysi...AIM:This study was designed to evaluate the anti-cancer actions of tanshinone I and tanshinone IIA,and six derivatives of tanshinone IIA on normal and cancerous colon cells.Structure activity relationship(SAR) analysis was conducted to delineate the significance of the structural modifications of tanshinones for improved anti-cancer action.METHOD:Tanshinone derivatives were designed and synthesized according to the literature.The cytotoxicity of different compounds on colon cancer cells was determined by the MTT assay.Apoptotic activity of the tanshinones was measured by flow cytometry(FCM).RESULTS:Tanshinone I and tanshinone IIA both exhibited significant cytotoxicity on colon cancer cells.They are more effective in p53+/+ colon cancer cell line.It was also noted that the anti-cancer activity of tanshinone I was more potent and selective.Two of the derivatives of tanshinone IIA(N1 and N2) also exhibited cytotoxicity on colon cancer cells.CONCLUSIONS:The anti-colon cancer activity of tanshinone I was more potent and selective than tanshinone IIA,and is p53 dependent.The derivatives obtained by structural modifications of tanshinone IIA exhibited lower cytotoxicity on both normal and colon cancer cells.From steric and electronic characteristics point of view,it was concluded that structural modifications of ring A and furan or dihydrofuran ring D on the basic structure of tanshinones influences the activity.An increase of the delocalization of the A and B rings could enhance the cytotoxicity of such compounds,while a non-planar and small sized D ring region would provide improved anti-cancer activity.展开更多
AIM: The potential of Trifolium pratense (red clover) extract in the prevention of lipid disorder has attracted increasing attention in recent years. In this study, the aim was to determine whether and how red clov...AIM: The potential of Trifolium pratense (red clover) extract in the prevention of lipid disorder has attracted increasing attention in recent years. In this study, the aim was to determine whether and how red clover extract affected the development of murine diet-induced non-alcoholic steatohepatitis. METHOD: Non-alcoholic steatohepatitis was induced in C57BL/6 mice by feeding mice with a methionine-choline-deficient (MCD) diet. Hematoxylin and eosin staining was used for histological analyses. Real-time PCR was used to analyze the mRNA expression levels. RESULTS: Hepatic steatosis and neeroinflammation was observed in MCD diet-fed mice, and this diet-induced steatosis was sig- nificantly attenuated, whereas liver inflammation was not significantly attenuated, by red clover extract treatment. Consistent with the results of H&E staining, the MCD diet-induced increase of liver triglycerides and cholesterol levels were significantly reduced by red clover extract treatment. However, with the improvement in hepatic steatosis, mRNA levels of acetyl CoA oxidase, carnitine palrnitoyl transferase-l, and liver fatty acid-binding protein, three genes regulated by peroxisome proliferator-activated receptor (PPAR) ct, were unaffected. CONCLUSION: Red clover extract alleviated MCD diet-induced hepatic steatosis, but did not ameliorate liver inflammation in C57BL/6 mice, and the improvement in hepatic steatosis was not through activating PPAR^t.展开更多
AIM: To study the chemical constituents of the roots of Asparagus cochinchinensis (Asparagaceae). METHOD: The compounds were isolated with Diaion HP20, silica gel, and ODS chromatography, and their structures were...AIM: To study the chemical constituents of the roots of Asparagus cochinchinensis (Asparagaceae). METHOD: The compounds were isolated with Diaion HP20, silica gel, and ODS chromatography, and their structures were de- termined on the basis of chemical methods, HR-ESI-MS, and 1 D- and 2D-NMR techniques. RESULTS: Seven compounds were isolated from the n-butanol fraction of the roots of A. cochinchinensis, and their structures were elucidated as (25S)-26-O-β-D-glucopyranosyl-5β-furostan-3β, 22a, 26-triol-12-one-3-O-β-D-glucopyranoside (1), (25S)-26- O-β-D-glucopyranosyl-22a-methoxy-5β-furostan-3p, 26-diol-12-one-3-O-β-D-glucopyranoside (2), (25S)-26-O-β-D-glucopyra- nosyl-5β-furostan-3β, 22a, 26-triol (3), (25S)-26-O-β-D-glucopyranosyl-5β-furstan-3β, 22a, 26-triol-3-O-β-D-glucopyranoside (4), (25S)-26-O-β-D-glucopyranosyl-5β-furostan-3β, 22a, 26-triol-3-O-a-L-rhamnopyranosyl-(1, 4)-β-D-glucopyranoside (5), (25S)- 5β-spirostan-3fl-ol-3-O-a-L-rhamnopyranoside (6), and (25S)-5β-spirostan-3β-ol-3-O-β-D-glucopyranoside (7). CONCLUSION: Compounds 1 and 2 were two new furostanol saponins.展开更多
AIM: To evaluate the anti-HIV activity and mechanism of action of wikstroelide M, a daphnane diterpene from Daphne acutiloba Rehder (Thymelaeaceae). METHOD: The anti-HIV activities of wikstroelide M against differ...AIM: To evaluate the anti-HIV activity and mechanism of action of wikstroelide M, a daphnane diterpene from Daphne acutiloba Rehder (Thymelaeaceae). METHOD: The anti-HIV activities of wikstroelide M against different HIV strains were evaluated by cytopathic effect assay and p24 quantification assay with ELISA. The inhibitory effect of wikstroelide M on HIV reverse transcription was analyzed by real-time PCR and ELISA. The effect of wikstroelide M on HIV-1 integrase nuclear translocation was observed with a cell-based imaging assay. The effect of wikstroelide M on LEDGF/p75-IN interaction was assayed by molecular docking. RESULTS: Wikstroelide M potently inhibited different HIV-1 strains, including HIV-lmn, HIV-1AI7, and HIV-19495, induced a cytopathic effect, with ECs0 values ranging from 3.81 to 15.65 ng.mL-I. Wikstroelide M also had high inhibitory activities against HIV-2noD and HIV-2cBL_20-induced cytopathic effects with ECs0 values of 18.88 and 31.90 ng.mL 1. The inhibitory activities of wikstroelide M on the three HIV-1 strains were further confirmed by p24 quantification assay, with ECs0 values ranging from 15.16 to 35.57 ng.mL-1. Wikstroelide M also potently inhibited HIV-lnm induced cytolysis in MT-4 cells, with an ECs0 value of 9.60 ng.mL ~. The mechanistic assay showed that wikstroelide M targeted HIV-I reverse transcriptase and nuclear translocation of integrase through disrupting the interaction between integrase and LEDGF/p75. CONCLUSION: Wikslroelide M may be a potent HIV-1 and HIV-2 inhibitor, the mechanisms of action may include inhibition of reverse trascriptase activity and inhibition of integrase nuclear Iranslocation through dismpting the interaction between integrase and LEDGF/p75.展开更多
AIM: In the present study, the anti-inflammatory and antioxidant activities of the methanol extract of Ruta graveolens leaves (RG-M) were evaluated using various in vivo and in vitro models. METHOD: For anti-infla...AIM: In the present study, the anti-inflammatory and antioxidant activities of the methanol extract of Ruta graveolens leaves (RG-M) were evaluated using various in vivo and in vitro models. METHOD: For anti-inflammatory activity, RG-M was administered by the oral route (p.o.) in a carrageenan-induced paw edema model, and by the intraperitoneal route (i.p.) in an exudative inflammation model. In vitro inhibition of cyelooxygenase and li- poxygenase enzymes was evaluated. In vitro antioxidant activity was also examined. Endogenous antioxidant status was fiarther evaluated by ferric reducing ability of plasma model. RESULTS: RG-M showed maximum inhibition of carrageenan-induced edema (100 mg·kg ^-1- 33.36%; 200 mg·kg ^-1 _ 45.32% and 400 mg·kg ^-1 56.28%). In the exudative inflammation model, a significant reduction in leukocyte migration (200 mg·kg ^-1_ 54.75% and 400 mg·kg ^-1 - 77.97%) and protein exudation (200 mg·kg ^-131.14% and 400 mg·kg ^-1 - 49.91%) were observed. RG-M also exhibited inhibition of COX-1 (ICs0 182.27 μg·mL ^-1) and COX-2 (IC50 190.16 μg·mL ^-1) as well as 5-LOX (IC50 215.71μg·mL ^-1). Antioxidant activity was significant with improved endogenous antioxidant status. CONCLUSION: The results demonstrated the anti-inflammatory and antioxidant activity of RG-M with potent inhibitory effects on the arachidonic acid pathways.展开更多
AIM: To investigate the quinoline alkaloids from the roots ofDictamnus angustifolius G.Don ex Sweet (Rutaceae). METHOD: The quinoline alkaloids were isolated by various column chromatographic methods and their str...AIM: To investigate the quinoline alkaloids from the roots ofDictamnus angustifolius G.Don ex Sweet (Rutaceae). METHOD: The quinoline alkaloids were isolated by various column chromatographic methods and their structures were eluci- dated on the basis of spectral analysis. RESULTS: A new quinoline alkaloid, 5-methoxylrobustine (1), along with five known quinoline alkaloids were obtained, and their structures were identified as dictamnine (2), robustine (3), isopteleine (4), 7-fagarine (5), and skimmianine (6). Cytotoxicity testing of these alkaloids showed that all of them had weak cytotoxic activities against human breast cancer cells (MCF7). CONCLUSION: Compound 1 is a new quinoline alkaloid. Alkaloid 3 showed stronger anti-proliferation effect than the other al- kaloids.展开更多
AIM: To investigate the chemical constituents of Fitex negundo. METHOD: Compounds were isolated by different chromatographic methods and their structures were elucidated on the basis of NMR spectroscopy. RESULTS: F...AIM: To investigate the chemical constituents of Fitex negundo. METHOD: Compounds were isolated by different chromatographic methods and their structures were elucidated on the basis of NMR spectroscopy. RESULTS: Four compounds were isolated and identified as 2a, 3a, 24-trihydroxyurs-12, 20(30)-dien-28-oic acid-28-O- β-D-glucopyranosyl ester (1), corosolic acid (2), vulgarsaponin A (3) and 2a, 3a, 24-trihydroxyurs-12-en-28-oic acid-28-O-β-D- glucopyranosyl ester (4), respectively. CONCLUSION: Compound I is a new triterpenoid glycoside.展开更多
AIM:To investigate the histological and ultrastructural changes observed in pan masala intoxicated mammalian testes under the effect of cardamom.METHOD:Male Swiss mice were given pan masala orally at a dose of 2% of t...AIM:To investigate the histological and ultrastructural changes observed in pan masala intoxicated mammalian testes under the effect of cardamom.METHOD:Male Swiss mice were given pan masala orally at a dose of 2% of the feed and cardamom at a dose of 0.2% of the feed.They were divided into three groups,control(Group I),pan masala-treated(Group II),and a combination of pan masala and cardamom-treated group(Group III).Histologically,the testes of Group II mice displayed degeneration of tubular epithelium,disruption of spermatogenesis,and a marked reduction in germ cells.RESULTS:When cardamom was given,damage was less with fewer distorted cells and also improvement with normal tubules and spermatid differentiation in Group III.Ultrastructurally,pan masala-treated testes showed cytoplasmic vacuolation,shrinkage and pyknotic nuclei of spermatogonia,and abnormal acrosomal granules.CONCLUSION:When cardamom was given,the amelioration process was more evident showing a comparable morphology with control.展开更多
AIM: To investigate the active chloroform fraction of the ethanol extract oflpomoea carnea flowers on hematological changes in toluene diisocyanate-induced inflammation in Wistar rats. METHOD: Except for the control...AIM: To investigate the active chloroform fraction of the ethanol extract oflpomoea carnea flowers on hematological changes in toluene diisocyanate-induced inflammation in Wistar rats. METHOD: Except for the control group, all of the rats were sensitized with intranasal application of 5 μL of 10% toluene diiso- cyanate (TDI) for 7 days. One week after second sensitization, all of the rats were provoked with 5 ~tL of 5% TDI to induce airway hypersensitivity. After the last challenge, blood and bronchoalvelor lavage (BAL) fluid were collected and subjected to total and differential leucocytes count. Flash chromatography was performed on the most active chloroform fraction to isolate an individual component. RESULTS: Treatment with the ethanolic extract and its chloroform fraction at an oral dose of 200 mg·kg^ -1 showed a significant decrease in circulating neutrophil and eosinophil in blood and BAL as compared with standard dexamethasone (DEXA). The structure of the compound obtained from chloroform fraction oflpomea carnea was elucidated as stigmast-5, 22-dien-3β-ol on the basis of spectral data analysis. CONCLUSION: The chloroform fraction was found to be more effective to suppress airway hyper reactivity symptoms, and de- creased count of both total and differential inflammatory cells.展开更多
AIM: To evaluate the antifertility activity of Artemisia vulgar& leaves on female Wistar rats. METHOD: The plant extract was tested for its effect on implant formation at two dose levels, 300 and 600 mg.kg 1, respe...AIM: To evaluate the antifertility activity of Artemisia vulgar& leaves on female Wistar rats. METHOD: The plant extract was tested for its effect on implant formation at two dose levels, 300 and 600 mg.kg 1, respectively. The effective methanolic plant extract was further studied for estrogenic potency on ovariectomised immature female Wistar rats. RESULTS: The data presented in this study demonstrate the antifertility potential of Artemisia vulgar& methanolic leaf extract, which shows a strong and significant decrease in implant formation (100%), and a strong estrogenic effect resulting in a significant increase in uterine weight in immature ovariectomised rats. These observations suggest that the methanolic extract of Artemisia vulgaris leaves has strong anti-implantation activity and estrogenic activity. CONCLUSION: The methanolic plant extract ofA. vulgaris has antifertility activity.展开更多
基金Supported by the National Natural Science Foundation of China(21076042)Research Grants Council of Hong Kong SAR (RGC 600704)
文摘Freeze drying or lyophilization of aqueous solutions is widely used in pharmaceutical industry. The in-creased importance Of the process is gaining a worldwide interest of research. A growing body of literature has demonstrated that the scientific approach can result in improved product quality with minimum trial and error em-piricism. Formulation and process development need a systematical understanding of the physical chemistry of freezing and freeze drying, material science and mechanisms of heat and mass transfer. This paper presents an overview on freeze ding of aqueous solutions based on publications in the past few decades. The important issuesof the process are analyzed.
文摘The cultivation and management of different legume species and their varieties were tested in South-Western Finland at farmers' fields in two years, 2010 and 2011. The studied legumes were peas and lava beans, and included also such species which are seldom or not normally cultivated in Finland, namely soybeans and blue and white lupins. Seed samples were collected from legume farms. The quality of different legume species was analysed and compared to each others. The chemical qualities were analysed for crude protein, fat, fibre, ash, nitrogen-free extract and phytic acid contents, and amino acid composition. The quality of the varieties of lupins and soybeans were compared to the quality of pea and fava bean varieties, which are generally cultivated nowadays in Finland. The highest protein contents were in soybean (369 and 379 g kg^-1) and white lupin (382 g kg^-1) and the lowest in pea varieties. Amino acid composition of legumes is good, but lupins have lower lysine content (g 100 g^-1 protein) than other legumes. High fat contents were in soybeans (91 and 100 g kg^-1) and white lupin (101 g kgl), and moderate in blue lupin (30-49 g kg^-1). Fuego fava bean variety had lower protein content than Kontu. The highest phytic acid contents were in soybeans (18.9 and 22.6 mg kg^-1) and the lowest in white lupin (6.2 mg kg^-1). Lupins are interesting protein crops, especially white lupin with high protein and fat and low phytic acid contents. Lupins are not day length sensitive, like soybean, and therefore valuable for long-day cultivation conditions The present research strengthens the good chemical quality of legumes for food and feed purposes.
基金Supported by Science and Technology Innovation Project in Hunan Academy of Agricultural Sciences(2017JC66)International Science and Technology Innovation Cooperation Base Construction Project in Hunan(2018WK4011)~~
文摘In order to study the effects of chemical osmotic pretreatment on the characteristics and quality of blueberry under hot air drying,fresh blueberries were pretreated with 2.5 g/100 mL K2CO3+0.6 g/100 mL olive oil,and 5.0 g/100 mL K2CO3+0.6 g/100 mL olive oil at(45±0.5)℃,respectively.The changes of water content,rehydration,hardness,microstructure,color difference,active ingredient anthocyanin,total phenol and DPPH radical scavenging capacity of dried blueberries in different treatment groups under hot air drying were compared and analyzed.The results showed that the dehydration rates of blueberries vary greatly according to the type of pretreatments when the samples were dried to the same water content with hot air.Specifically,the dehydration rate of dried blueberries pretreated by 5.0%K2CO3 solution was the highest,followed by 2.5%K2CO3 osmotic pretreatment and lastly the control group;the corresponding dehydration time was 10,14 and 20h,respectively.The physical qualities of dried blueberries,involving the browning degree,color difference,rehydration and microstructure,were significantly different between the chemical osmotic pretreatment group and the control group(P<0.05).The chemical osmotic pretreatment of K2CO3 solution increased the dehydration rate of the samples,shortened the drying time and maintained the quality of blueberries dried with hot air.There was no significant difference between the physical quality of dried blueberries pretreated by 2.5%and 5.0%K2CO3 solution(P>0.05),whereas there was significant difference in drying time and nutrient quality which is characterized by total phenols,anthocyanins,DPPH radical scavenging rate,soluble total sugar(P<0.05).Conclusion:5.0%K2CO3 osmotic pretreatment combining with hot air drying can improve the dehydration rate,shorten the drying time and maintain the physical and nutritional quality.
文摘Cucumeropsis mannii, an underutilized oil seed was processed into raw full fat and defatted seed flours and its chemical, functional properties and anti-nutritional factors were determined using standard techniques. The effects of sample concentration and pH on the foaming properties of the seed flours were determined. The results showed that the full fat and defatted seed flours contained the following in g/100 g sample; 5.0 and 5.1; 45.8 and 1.0; 39.4 and 78.7; 3.45 and 4.40; 1.50 and 3.05; 4.85 and 7.75 for moisture, crude fat, protein, ash, crude fibre and carbohydrate, respectively. The most abundant mineral elements in the seed flour (mg/100 g) are potassium (198.5), followed by nickel (30.0) and magnesium (28.4). The water absorption capacity, oil absorption capacity, foaming capacity and stability, least gelation concentration, emulsion capacity and bulk density are 55.5% and 125.0%; 128.8% and 184.0%; 10.5% and 17.0%; 3.0% and 1.5%; 16.0% and 10.0 g/mL; 85.0 and 115.0 mL/g; 0.42 and 0.25 g/mL, respectively. Defatting influenced the functional properties. The foaming capacity is dependent on sample concentration and pH. The protein solubility of the full fat and defatted seed flours was minimum between pH 3 and 4 and maximum at pH 11. The anti-nutritional composition of the seed flour revealed the following: tannic acid, 1.54 mg/100 g; phytin phosphorus, 0.70 rag/g; phytic acid, 2.48 mg/g; oxalate, 1.85 mg/g; alkaloids 1.97% and saponin 0.50%. The seed flours (full fat and defatted) have potential as nutrient supplement, thickeners and emulsifiers in food system.
文摘The pyrolysis of isopsoralen was studied by synchrotron vacuum ultraviolet photoionization mass spectrometry at low pressure. The pyrolysis products were detected at different photon energies, the ratios of products to precursor were measured at various pyrolysis temperatures. The experimental results demonstrate that the main pyrolysis products are primary CO and sequential CO elimination products (C10H602 and C9H60). The decomposition channels of isopsoralen were also studied by the density functional theory, then rate constants for competing pathways were calculated by the transition state theory. The dominant decom- position channels of isopsoralen and the molecular structures for corresponding products were identified by combined experimental and theoretical studies.
基金supported by the Chongqing Science and Technology Commission Foundation(No.CSTC2010-AB5070)the Projects of Chongqing Science&Technology(No.CSTC2011jjA0324)+2 种基金the Southwest University Doctor Foundation(No.SWU111065)the Fundamental ResearchFunds for Central Universities(No.XDJK2010 C059)the South-west University Doctor Foundation(No.SWU112102)
文摘AIM:To explore the therapeutic effects of Morinda officinalis capsules(MOP) on osteoporosis in ovariectomized rats.METHOD:Six-month-old female Sprague–Dawley rats were induced for postmenopausal osteoporosis(PMOP) by bilateral ovariectomy and divided into seven groups as follows:sham-operated group,ovariectomized(OVX) control group,OVX treated with xianlinggubao(XLGB)(270 mg·kg-1·d-1),OVX treated with alendronate sodium(ALN)(3 mg·kg-1·d-1),and OVX treated with Morinda officinalis capsule(MOP) of graded doses(90,270 and 810 mg·kg-1·d-1) groups.Oral treatments were administered daily on the 4th week after ovariectomy and lasted for 12 weeks.The bone mineral density was evaluated by dual-energy X-ray absorptiometry.The tartrate-resistant acid phosphatase(TRAP),alkaline phosphatase(AKP),and osteocalcin(OC) levels in the serum and plasma were determined by standard colorimetric and enzyme immunoassays methods.Bone biomechanical properties and morphological parameters were analyzed by three-point bending test and histomorphometry respectively.RESULTS:Morinda officinalis capsules at all doses were able to significantly prevent the OVX-induced loss of bone mass due to diminishing serum AKP and TRAP levels while elevating OC level in the plasma.Morinda officinalis capsules also enhanced the bone strength and prevented the deterioration of trabecular microarchitecture.CONCLUSION:Morinda officinalis capsules possess potent anti-osteoporotic activity in OVX rats which could be an effective treatment for postmenopausal osteoporosis.
基金supported by the National Natural Science Foundation of China(No.81274159)"Eleventh-Five Years"Supporting Programs from the Ministry of Science and Technology of China(No.2008BAI51B01)
文摘AIM: To profile the chemical constituents in Jinqi Jiangtang tablets. METHOD: Based on the chromatographic retention behavior, fragmentation patterns of chemical components, and published lit- eratures, a high-performance liquid chromatography coupled with electrospray ionization quadrnpole time-of-flight tandem mass spectrometry (HPLC-ESI-Q-TOF/MS) method was established to characterize and identify components in Jinqi Jiangtang tablets. RESULTS: A total of 52 chemical compounds, including eight iridoid glycosides, seven phenolic acids, twelve alkaloids, six fla- vonoids, and nineteen saponins, were identified in Jinqi Jiangtang tablets. CONCLUSION: The established method could serve as a powerful tool for structural characterization and quality control of this Chinese herbal preparation.
基金financially supported by the National Key Technology R&D Program"New Drug Innovation"of China(Nos.2012ZX09301002-002-002,2012ZX09304-005)special funds for scientific research on traditional Chinese medicine(No.201307002)National Science Fund for Excellent Young Scholars(No.81222051)
文摘AIM:To investigate the chemical constituents of the roots of Polygala sibirica L.(Polygalaceae) METHOD:The isolation was performed by solvent extraction and various chromatographic techniques,including silica gel,Sephadex LH-20,ODS,semi-preparative HPLC,and preparative TLC.The chemical structures were elucidated based on extensive spectroscopic analysis,including HR-ESI-MS and 1D- and 2D-NMR spectroscopic data.RESULTS:A total of sixteen compounds,including five xanthones(5,7–10),five saccharide esters(1,3,4,12,13),two flavonoids(14,16),two triterpenoids(11,15),one phenylpropanoid(6),and one benzophenone glycoside(2) were isolated.Their structures were determined as sibiricose A7(1),sibiriphenone A(2),polygalatenoside A(3),polygalatenoside C(4),lancerin(5),3,4,5-trimethoxycinnamic acid(6),6-hydroxy-1,2,3,7-tetramethoxyxanthone(7),1,3,7-trihydroxy-2-methoxyxanthone(8),onjixanthone II(9),1,2,3,6,7-pentamethoxyxanthone(10),presenegenin(11),3'-O-3,4,5-trimethoxycinnamoyl-6-O-4-methoxy benzoyl sucrose(12),tenuifoliside C(13),5,3'-dihydroxy-7,4'-dimethoxyflavonol-3-O-β-D-glucopyranoside(14),tenuifolin(15),and rhamnetin 3-O-β-D-glucopyranoside(16).CONCLUSION:Compounds 1 and 2 are two new compounds from P.sibirica.
基金supported by the National Major Scientific and Technological Special Project for"Significant New Drugs Development"(No.2011ZX09401-028)
文摘AIM:This study was designed to evaluate the anti-cancer actions of tanshinone I and tanshinone IIA,and six derivatives of tanshinone IIA on normal and cancerous colon cells.Structure activity relationship(SAR) analysis was conducted to delineate the significance of the structural modifications of tanshinones for improved anti-cancer action.METHOD:Tanshinone derivatives were designed and synthesized according to the literature.The cytotoxicity of different compounds on colon cancer cells was determined by the MTT assay.Apoptotic activity of the tanshinones was measured by flow cytometry(FCM).RESULTS:Tanshinone I and tanshinone IIA both exhibited significant cytotoxicity on colon cancer cells.They are more effective in p53+/+ colon cancer cell line.It was also noted that the anti-cancer activity of tanshinone I was more potent and selective.Two of the derivatives of tanshinone IIA(N1 and N2) also exhibited cytotoxicity on colon cancer cells.CONCLUSIONS:The anti-colon cancer activity of tanshinone I was more potent and selective than tanshinone IIA,and is p53 dependent.The derivatives obtained by structural modifications of tanshinone IIA exhibited lower cytotoxicity on both normal and colon cancer cells.From steric and electronic characteristics point of view,it was concluded that structural modifications of ring A and furan or dihydrofuran ring D on the basic structure of tanshinones influences the activity.An increase of the delocalization of the A and B rings could enhance the cytotoxicity of such compounds,while a non-planar and small sized D ring region would provide improved anti-cancer activity.
基金supported by the Science and Technology Planning Project of Educational Commission of Fujian Province,China(No.JB12198) and Fujian Province,China(No.2010N0023)
文摘AIM: The potential of Trifolium pratense (red clover) extract in the prevention of lipid disorder has attracted increasing attention in recent years. In this study, the aim was to determine whether and how red clover extract affected the development of murine diet-induced non-alcoholic steatohepatitis. METHOD: Non-alcoholic steatohepatitis was induced in C57BL/6 mice by feeding mice with a methionine-choline-deficient (MCD) diet. Hematoxylin and eosin staining was used for histological analyses. Real-time PCR was used to analyze the mRNA expression levels. RESULTS: Hepatic steatosis and neeroinflammation was observed in MCD diet-fed mice, and this diet-induced steatosis was sig- nificantly attenuated, whereas liver inflammation was not significantly attenuated, by red clover extract treatment. Consistent with the results of H&E staining, the MCD diet-induced increase of liver triglycerides and cholesterol levels were significantly reduced by red clover extract treatment. However, with the improvement in hepatic steatosis, mRNA levels of acetyl CoA oxidase, carnitine palrnitoyl transferase-l, and liver fatty acid-binding protein, three genes regulated by peroxisome proliferator-activated receptor (PPAR) ct, were unaffected. CONCLUSION: Red clover extract alleviated MCD diet-induced hepatic steatosis, but did not ameliorate liver inflammation in C57BL/6 mice, and the improvement in hepatic steatosis was not through activating PPAR^t.
基金supported by the National Natural Science foundation of China(No.20962013)
文摘AIM: To study the chemical constituents of the roots of Asparagus cochinchinensis (Asparagaceae). METHOD: The compounds were isolated with Diaion HP20, silica gel, and ODS chromatography, and their structures were de- termined on the basis of chemical methods, HR-ESI-MS, and 1 D- and 2D-NMR techniques. RESULTS: Seven compounds were isolated from the n-butanol fraction of the roots of A. cochinchinensis, and their structures were elucidated as (25S)-26-O-β-D-glucopyranosyl-5β-furostan-3β, 22a, 26-triol-12-one-3-O-β-D-glucopyranoside (1), (25S)-26- O-β-D-glucopyranosyl-22a-methoxy-5β-furostan-3p, 26-diol-12-one-3-O-β-D-glucopyranoside (2), (25S)-26-O-β-D-glucopyra- nosyl-5β-furostan-3β, 22a, 26-triol (3), (25S)-26-O-β-D-glucopyranosyl-5β-furstan-3β, 22a, 26-triol-3-O-β-D-glucopyranoside (4), (25S)-26-O-β-D-glucopyranosyl-5β-furostan-3β, 22a, 26-triol-3-O-a-L-rhamnopyranosyl-(1, 4)-β-D-glucopyranoside (5), (25S)- 5β-spirostan-3fl-ol-3-O-a-L-rhamnopyranoside (6), and (25S)-5β-spirostan-3β-ol-3-O-β-D-glucopyranoside (7). CONCLUSION: Compounds 1 and 2 were two new furostanol saponins.
基金supported,in part,by grants from the National Natural Science Foundation of China(Nos.81102483,81001462)the 973 Program(No.2009CB522306)the Key Scientific and Technological Program of China(Nos.2009-ZX09501-029,2012ZX10001-006,2012ZX10001-007,2012ZX-09103-101-022),and Yunnan(No.2010GA001)
文摘AIM: To evaluate the anti-HIV activity and mechanism of action of wikstroelide M, a daphnane diterpene from Daphne acutiloba Rehder (Thymelaeaceae). METHOD: The anti-HIV activities of wikstroelide M against different HIV strains were evaluated by cytopathic effect assay and p24 quantification assay with ELISA. The inhibitory effect of wikstroelide M on HIV reverse transcription was analyzed by real-time PCR and ELISA. The effect of wikstroelide M on HIV-1 integrase nuclear translocation was observed with a cell-based imaging assay. The effect of wikstroelide M on LEDGF/p75-IN interaction was assayed by molecular docking. RESULTS: Wikstroelide M potently inhibited different HIV-1 strains, including HIV-lmn, HIV-1AI7, and HIV-19495, induced a cytopathic effect, with ECs0 values ranging from 3.81 to 15.65 ng.mL-I. Wikstroelide M also had high inhibitory activities against HIV-2noD and HIV-2cBL_20-induced cytopathic effects with ECs0 values of 18.88 and 31.90 ng.mL 1. The inhibitory activities of wikstroelide M on the three HIV-1 strains were further confirmed by p24 quantification assay, with ECs0 values ranging from 15.16 to 35.57 ng.mL-1. Wikstroelide M also potently inhibited HIV-lnm induced cytolysis in MT-4 cells, with an ECs0 value of 9.60 ng.mL ~. The mechanistic assay showed that wikstroelide M targeted HIV-I reverse transcriptase and nuclear translocation of integrase through disrupting the interaction between integrase and LEDGF/p75. CONCLUSION: Wikslroelide M may be a potent HIV-1 and HIV-2 inhibitor, the mechanisms of action may include inhibition of reverse trascriptase activity and inhibition of integrase nuclear Iranslocation through dismpting the interaction between integrase and LEDGF/p75.
基金Dr. S. Rana,Director,Research Institute in Indian System of Medicine(ISM),Joginder Nagar,Himachal Pradesh for providing supportthe active support of Prof. D. N. Sharma,Ex. Director,Abhilashi College of Pharmacy,Mandi,Himachal Pradesh,IndiaMr. Yogendra Tomar,Founder member,Health Quest Foundation for expert advice and support
文摘AIM: In the present study, the anti-inflammatory and antioxidant activities of the methanol extract of Ruta graveolens leaves (RG-M) were evaluated using various in vivo and in vitro models. METHOD: For anti-inflammatory activity, RG-M was administered by the oral route (p.o.) in a carrageenan-induced paw edema model, and by the intraperitoneal route (i.p.) in an exudative inflammation model. In vitro inhibition of cyelooxygenase and li- poxygenase enzymes was evaluated. In vitro antioxidant activity was also examined. Endogenous antioxidant status was fiarther evaluated by ferric reducing ability of plasma model. RESULTS: RG-M showed maximum inhibition of carrageenan-induced edema (100 mg·kg ^-1- 33.36%; 200 mg·kg ^-1 _ 45.32% and 400 mg·kg ^-1 56.28%). In the exudative inflammation model, a significant reduction in leukocyte migration (200 mg·kg ^-1_ 54.75% and 400 mg·kg ^-1 - 77.97%) and protein exudation (200 mg·kg ^-131.14% and 400 mg·kg ^-1 - 49.91%) were observed. RG-M also exhibited inhibition of COX-1 (ICs0 182.27 μg·mL ^-1) and COX-2 (IC50 190.16 μg·mL ^-1) as well as 5-LOX (IC50 215.71μg·mL ^-1). Antioxidant activity was significant with improved endogenous antioxidant status. CONCLUSION: The results demonstrated the anti-inflammatory and antioxidant activity of RG-M with potent inhibitory effects on the arachidonic acid pathways.
基金supported by the National New Drug Innovation Major Project of China(No.2011ZX09307-002-02)
文摘AIM: To investigate the quinoline alkaloids from the roots ofDictamnus angustifolius G.Don ex Sweet (Rutaceae). METHOD: The quinoline alkaloids were isolated by various column chromatographic methods and their structures were eluci- dated on the basis of spectral analysis. RESULTS: A new quinoline alkaloid, 5-methoxylrobustine (1), along with five known quinoline alkaloids were obtained, and their structures were identified as dictamnine (2), robustine (3), isopteleine (4), 7-fagarine (5), and skimmianine (6). Cytotoxicity testing of these alkaloids showed that all of them had weak cytotoxic activities against human breast cancer cells (MCF7). CONCLUSION: Compound 1 is a new quinoline alkaloid. Alkaloid 3 showed stronger anti-proliferation effect than the other al- kaloids.
基金supported by the Program for Changjiang Scholars and Innovative Research Team in the University(No.IRT0965)the Team Project of Natural Science Foundation of Guangdong Province(No.8351063201000003)the Science and Technology Planning Project of Guangdong Province(No.2012A080204005)
文摘AIM: To investigate the chemical constituents of Fitex negundo. METHOD: Compounds were isolated by different chromatographic methods and their structures were elucidated on the basis of NMR spectroscopy. RESULTS: Four compounds were isolated and identified as 2a, 3a, 24-trihydroxyurs-12, 20(30)-dien-28-oic acid-28-O- β-D-glucopyranosyl ester (1), corosolic acid (2), vulgarsaponin A (3) and 2a, 3a, 24-trihydroxyurs-12-en-28-oic acid-28-O-β-D- glucopyranosyl ester (4), respectively. CONCLUSION: Compound I is a new triterpenoid glycoside.
文摘AIM:To investigate the histological and ultrastructural changes observed in pan masala intoxicated mammalian testes under the effect of cardamom.METHOD:Male Swiss mice were given pan masala orally at a dose of 2% of the feed and cardamom at a dose of 0.2% of the feed.They were divided into three groups,control(Group I),pan masala-treated(Group II),and a combination of pan masala and cardamom-treated group(Group III).Histologically,the testes of Group II mice displayed degeneration of tubular epithelium,disruption of spermatogenesis,and a marked reduction in germ cells.RESULTS:When cardamom was given,damage was less with fewer distorted cells and also improvement with normal tubules and spermatid differentiation in Group III.Ultrastructurally,pan masala-treated testes showed cytoplasmic vacuolation,shrinkage and pyknotic nuclei of spermatogonia,and abnormal acrosomal granules.CONCLUSION:When cardamom was given,the amelioration process was more evident showing a comparable morphology with control.
文摘AIM: To investigate the active chloroform fraction of the ethanol extract oflpomoea carnea flowers on hematological changes in toluene diisocyanate-induced inflammation in Wistar rats. METHOD: Except for the control group, all of the rats were sensitized with intranasal application of 5 μL of 10% toluene diiso- cyanate (TDI) for 7 days. One week after second sensitization, all of the rats were provoked with 5 ~tL of 5% TDI to induce airway hypersensitivity. After the last challenge, blood and bronchoalvelor lavage (BAL) fluid were collected and subjected to total and differential leucocytes count. Flash chromatography was performed on the most active chloroform fraction to isolate an individual component. RESULTS: Treatment with the ethanolic extract and its chloroform fraction at an oral dose of 200 mg·kg^ -1 showed a significant decrease in circulating neutrophil and eosinophil in blood and BAL as compared with standard dexamethasone (DEXA). The structure of the compound obtained from chloroform fraction oflpomea carnea was elucidated as stigmast-5, 22-dien-3β-ol on the basis of spectral data analysis. CONCLUSION: The chloroform fraction was found to be more effective to suppress airway hyper reactivity symptoms, and de- creased count of both total and differential inflammatory cells.
基金Dr. Ravindra Reddy,Principal,P. Ramireddy Memorial College of Pharmacy for providing all the necessary assistance required for this study and also his moral support
文摘AIM: To evaluate the antifertility activity of Artemisia vulgar& leaves on female Wistar rats. METHOD: The plant extract was tested for its effect on implant formation at two dose levels, 300 and 600 mg.kg 1, respectively. The effective methanolic plant extract was further studied for estrogenic potency on ovariectomised immature female Wistar rats. RESULTS: The data presented in this study demonstrate the antifertility potential of Artemisia vulgar& methanolic leaf extract, which shows a strong and significant decrease in implant formation (100%), and a strong estrogenic effect resulting in a significant increase in uterine weight in immature ovariectomised rats. These observations suggest that the methanolic extract of Artemisia vulgaris leaves has strong anti-implantation activity and estrogenic activity. CONCLUSION: The methanolic plant extract ofA. vulgaris has antifertility activity.