Gentiana macrophylla Pall.:a review of the basic source,traditional use,chemical components,pharmacological activities and quality control

Gentiana macrophylla Pall.(G.macrophylla),whose genus and family belong to the Gentianaceae and Gentiana.The main distribution centers of G.macrophylla resources were the Loess Plateau and the eastern Qinghai-Tibet Plateau in China.G.macrophylla,as a traditional medicine,has a long history and was used in different ethnic medicines.Its roots were used in traditional Chinese medicine,which had the effect of anti-inflammatory,anti-rheumatism,antiviral,promote blood circulation,eliminate swelling and pain,while its flowers were used in traditional Mongolian medicine,which had the effect of removing“Xieriwusu”(“Xieriwusu”means rheumatism),antiviral,reducing swelling.From previous studies,it could be found that there were more than forty components isolated and identified from G.macrophylla.The main chemical components were iridoids,flavonoids,triterpenoids,steroids,phenylpropanoids,and alkaloids.Iridoid terpenoid components represented by gentiopicroside and Loganic acid were the main components of the root of G.macrophylla,which had anti-inflammatory,antioxidant,hepatoprotective,analgesic,antibacterial and promote gastrointestinal tract activities.The flower mainly contains isoorientin and isovitexin as the representative of flavonoids.They have anti-tumor,liver protection,heart protection,inhibition of acetylcholinesterase and inhibition of melanin.It could be seen from previous studies that the research on G.macrophylla was mainly focused on the root,and the flower was rarely studied.It was reported that the experimental data of the anti-inflammatory and anti-tumor effects of G.macrophylla flowers show that its curative effect was very good.Therefore,the flowers of the flower of G.macrophylla can be used as potential medicinal parts for research.Given that flavonoids are mostly found in flowers and exhibit a range of functions,it is possible to investigate the flowers in order to learn more about G.macrophylla’s potential medical benefits.Based on botanical books,Chinese classic texts,medical monographs and academic search engines(Google,Google Scholar,Web of Science,SciFinder,Pubmed,CNKI,Sci-hub,Elsevier and Wanfang),the data and information on G.macrophylla in the past 20 years are inquired and summarized comprehensively.The basic source,traditional use,chemical composition,biological activity,pharmacodynamics and quality control of G.macrophylla was systematically reviewed,in order to provide reliable basis for the subsequent development and utilization of G.macrophylla.

Active components of Bupleuri Radix in the treatment of schizophrenia analyzed by network pharmacology and clinical verification

Background:Bupleuri Radix is a common Chinese medicinal material in traditional Chinese medicine.Currently,the therapeutic effect of treating schizophrenia is relatively well understood.However,there are fewer studies examining the underlying mechanisms of its treatment.The objective of the study was to investigate the primary mechanisms of Bupleuri Radix in treating schizophrenia through network pharmacology and clinical validation.Method:Network pharmacology revealed possible molecular mechanisms,followed by clinical verification.Sixty-seven schizophrenia patients undergoing treatment at the Hunan Brain Hospital between October and November 2022 were recruited and randomly divided into the olanzapine group and the olanzapine+Bupleuri Radix group.Additionally,32 healthy people undergoing physical examinations during the same period were included as the control group.The patient’s positive and negative symptom scale scores were compared.qPCR was used to detect the mRNA expression levels of ESR1,mTOR,EIF4E,and SMAD4 in peripheral blood.Results:Through network pharmacological analysis,it was concluded in this study that Bupleuri Radix might regulate the mTOR,PI3K-Akt,and HIF-1 signaling pathways.Clinical experiments indicated that compared with before treatment,the positive and negative symptom scale scores and total scores of the two treatment groups were significantly decreased after treatment(P<0.01).In addition,the positive and negative symptom scale scores and total scores in the olanzapine+Bupleuri Radix group were significantly decreased(P<0.01)compared to the olanzapine group after treatment.Before treatment,ESR1 mRNA expression levels in peripheral blood were significantly higher in the two treatment groups than in the control group,whereas the mRNA expression levels of mTOR,EIF4E,and SMAD4 in peripheral blood were significantly lower(P<0.01).The mRNA expression levels of mTOR,EIF4E,and SMAD4 in peripheral blood were significantly higher after therapy than before treatment,whereas the mRNA expression levels of ESR1 in peripheral blood were significantly lower(P<0.01).After therapy,the olanzapine+Bupleuri Radix group’s mRNA expression levels of mTOR,EIF4E,and SMAD4 were significantly higher than those of the olanzapine group,whereas the mRNA expression levels of ESR1 were significantly lower(P<0.01).Conclusion:The mechanism of Bupleuri Radix’s therapeutic efficacy in schizophrenia may involve the up-regulation of mTOR,EIF4E,and SMAD4 mRNA expression and the down-regulation of ESR1 mRNA expression in peripheral blood.

Effects of different thermal processing methods on bioactive components,phenolic compounds,and antioxidant activities of Qingke(highland hull-less barley)

Qingke(highland hull-less barley)is a grain replete with substantial nutrients and bioactive ingredients.In this study,we evaluated the effects of boiling(BO),steaming(ST),microwave baking(MB),far-infrared baking(FB),steam explosion(SE),and deep frying(DF)on bioactive components,phenolic compounds,and antioxidant activities of Qingke compared with the effects of traditional roast(TR).Results showed that the soluble dietary fiber,beta-glucan and water-extractable pentosans of Qingke in dry heat processes of TR,SE,MB and FB had a higher content compared with other thermal methods and had a better antioxidant activity of hydroxyl radical scavenging and a better reduction capacity,while those in wet heat processes of BO and ST had a better antioxidant activity of ABTS radical scavenging and a better Fe^(2+) chelating ability.DF-and SE-Qingke had a higher content of tocopherol,phenolic,and flavonoid.Overall,6 free phenolic compounds and 12 bound phenolic compounds of Qingke were identified,and free phenolic compounds suffered more damage during thermal processing.Principal component analysis showed that SE had more advantages in retaining and improving the main biological active ingredients of Qingke,and it may be the best method for treating Qingke.

Effects of Different Sterilization Conditions on Active Components and Flavor of Apple Vinegar

[Objectives]To explore the effects of different sterilization conditions on nutrition and flavor of apple vinegar.[Methods]Five kinds of high temperature short time(HTST)sterilization conditions were selected to treat apple vinegar,and the volatile aroma components and the content of active components in apple vinegar before and after sterilization were analyzed.[Results]Compared with the control,the contents of total acid and malic acid in the samples after sterilization changed little,but the contents of citric acid increased significantly(P<0.01),and the contents of total phenols,ascorbic acid and total flavonoids decreased.Ethyl acetate,isopentyl acetate,ethyl caprylate,phenethyl acetate,1-pentanol,phenylethyl alcohol,acetic acid,and sec-butyl ether were the characteristic aroma components which contributed to the flavor of apple vinegar.As sterilization temperature increased,the content of esters decreased,while the content of acids,alcohols and aldehydes increased.The contents of nutrition,active components and volatile aroma components in apple vinegar under 100℃and 30 s sterilization conditions had little change compared with other sterilization conditions,so 100℃and 30 s were the optimal sterilization conditions.[Conclusions]Under different sterilization conditions,the content of flavor components in apple vinegar will change greatly,which will affect the quality of apple vinegar.

Research Progress of Natural Active Components against Damage from UV Radiation

The sun's ultraviolet(UV)rays are extremely harmful to the skin.In addition to causing sunburn and aging,excessive UV radiation can also lead to benign or malignant skin tumors.This paper reviews the researches on natural active components against damage from UV radiation,and summarizes the types of compounds,research methods and mechanisms of action.Moreover,the main problems in current research are put forward,and the possible development direction in the future is discussed.

Study on Component Synthesis Active Vibration Suppression Method Using Zero-placement Technique

The component synthesis active vibration suppression method （CSVS） can be applied to suppress the vibration of flexible systems. By this method, several same or similar time-varying components are arranged according to certain rules along the time axis. The synthesized command can suppress the arbitrary unwanted vibration harmonic while achieving the desired rigid body motion. The number of the components increases rapidly when the number of harmonic vibration is growing. In this article, the CSVS based on zero-placement technique is used to construct the synthesized command to suppress the multi-harmonics simultaneously in the discrete domain. The nature of zero-placement method is to put enough zeros to cancel system poles at necessary points. The designed synthesized command has equal time intervals between each component and which is much easier to be implemented. Using this method, the number of components increases linearly with the increasing of the number of being suppressed harmonics. For the spacecraft with flexible appendages, CSVS based on zero-placement is used to design the time optimal large angle maneuver control strategy. Simulations have verified the validity and superiority of the proposed approach.

Analysis of Active Components of Hexane Extractives of Morus alba Leaves

[Objective]The aim was to explore the active compound of Morus alba leaves with the analysis of active components of hexane extractives of M.alba leaves.[Method]Antibacterial assays of hexane extractives of M.alba leaves were done and the volatile components of hexane extractives of M.alba leaves with the strongest antibacterial activity were analyzed by gas chromatography-mass spectrometry（GC-MS）.[Result]The results of inhibitory effect of hexane extractives of M.alba leaves on Staphylococcus aureus and Escherichia coli showed that hexane extractives of M.alba leaves collected in June,July and August had antibacterial activity against S.aureus and had no antibacterial effect against E.coli.Furthermore,hexane extractives of M.alba leaves collected in June had the strongest antibacterial activity against S.aureus（inhibition diameter 10.95 mm）.The hexane extractives of M.alba leaves collected in June was analyzed by GC-MS,the main volatile components were tetradecane（16.76%）,dodecane（13.20%）,diisobutyl phthalate（10.26%）,decane（9.10%）,hexadecane（8.71%）,linolenyl alcohol（7.25%）,octadecane（5.88%）,eicosane（3.26%）,dibutyl phthalate（2.59%）.[Conclusion]Linolenyl alcohol was the potential antibacterial compound.

Volatile Components and Antitumor Activity of Ganoderma lucidum Spore Oil and Its Molecular Distillation Components

[Objectives]To compare the effects of molecular distillation on the flavor and antitumor activity of Ganoderma lucidum spore oil.[Methods]G.lucidum spore oil was separated and purified by molecular distillation technology,and the volatile components of different components of molecular distillation were analyzed by gas chromatography-ion mobility spectrometry(GC-IMS)technology.Human liver carcinoma cells(HepG2),human breast cancer cells(MCF-7),and human cervical cancer cells(Hela)were selected as the tumor cell lines to be tested,and the cell viability was detected by the MTT assay.[Results]Molecular distillation effectively reduced small molecular substances produced by oil oxidation in G.lucidum spore oil,such as heptanal,octanal,linalool,hexanal,E-2-octanal,3-ethylpyridine,etc.Among the heavy components,the content of esters was relatively high,mainly including ethyl levulinate,ethyl crotonate,and amyl butyrate.The MTT cytotoxicity test indicated that G.lucidum spore oil and its molecular distillation components had certain inhibitory effects on the growth of three tumor cells,and G.lucidum spore oil crude oil had the most significant antitumor activity.G.lucidum spore oil crude oil,heavy component,and light component had the most significant antitumor activity on HepG2 cells,followed by MCF-7 cells,and the weakest antitumor activity on Hela cells.The quality of G.lucidum spore oil became higher after molecular distillation,and the rancid smell was reduced,and molecular distillation had little effect on the antitumor activity of G.lucidum spores.[Conclusions]Molecular distillation technology can be applied to the refining of G.lucidum spore oil to improve product quality.

Insecticidal activities and active components of the alcohol extract from green peel of Juglans mandshurica

The extract of green peel of Juglans mandshurica Maxim was extracted by common method for studying its insecticidal activities and analyzing the active components. Results showed that the alcohol extract and the chloroform part of extract （separated with chloroform from alcohol extract） form green peel of J. mandshurica have insecticidal activities in contact toxicity and stomach toxicity against larvae of Lymantria dispar L.. After application of the extracts for five days, the corrected mortality of larvae of Lymantria dispar for both extracts was more than 50% in contact toxicity and stomach toxicity at the concentration of ≥ 5 g·L^-1. The insecticidal activity for both alcohol extract and chloroform part of extract is more effect in contact toxicity than in stomach toxicity, but no significant difference in the insecticidal activities was found between alcohol extract and chloroform part of extract. The active components in the chloroform part of extract from green peel of.J. mandshurica were analyzed by GC-MS. The analyzed results showed that the active components in the chloroform part of extract are： （1） joglone （5-hydroxy-1,4- naphthaoquinone）, the relative content 27.11%, （2） 1,5-Naphthalenediol, the relative content 9.52%, （3） 7-Methoxy-1-tetralone, the relative content 6.81%, （4） Benzofuran, 2,3-dihydro-, the relative content 6.76%, （5） 4-Hydroxy-2-methoxycinnamaldehyde, the relative content 3.99%, （6） 2-Methoxy-4-vinylphenol, the relative content 3.05%.

Network Pharmacology-based Research of Active Components of Albiziae Flos and Mechanisms of Its Antidepressant Effect

Albiziae Flos(AF)has been experimentally proven to have an antidepressant effect.However,due to the complexity of botanical ingredients,the exact pharmacological mechanism of action of AF in depression has not been completely deciphered.This study used the network pharmacology method to construct a component-target-pathway network to explore the active components and potential mechanisms of action of AF.The methods included collection and screening of chemical components,prediction of depression-associated targets of the active components,gene enrichment,and network construction and analysis.Quercetin and 4 other active components were found to exert an tidepressant effects mainly via monoaminergic neurotransmitters and cAMP signaling and neuroactive ligand・wceptor interaction pathways.DRD2,HTR1 A,and SLC6A4 were identified as important targets of the studied bioactive components of AF.This network pharmacology analysis provides guidance for further study of the antidepressant mechanism of AF.

Review of Factors Influencing Active Components of Lonicera japonica Thunb.

Lonicera japonica Thunb. is a typical medicinal and edible plant in China. It has antibacterial, anti-oxidant, anti-endotoxin, and anti-inflammatory effects, etc. Its pharmacological action is closely related to its active components. Based on the results of previous studies, this paper summarized the effects of variety, origin, cultivation conditions, pruning, harvesting period and processing methods on the active components of L. japonica , in the hope of providing theoretical guidance for high-yield and high-quality cultivation of L. japonica.

Review of Effects of Active Components of Gastrodiae Rhizoma on Central Nervous System

In order to explore the pharmacological effects of active components of Gastrodiae Rhizoma on the central nervous system,through consulting related literatures,this paper summarized the pharmacological effects of the active components of Gastrodiae Rhizoma.The pharmacological effects of the active components of Gastrodiae Rhizoma on the central nervous system include improving the ability of learning and memory,analgesia,sedation and hypnosis,anticonvulsant,anti-aging,anti-anxiety and neuroprotective effects.The active components of Gastrodiae Rhizoma have certain curative effect in the treatment of some diseases of the central nervous system.At present,it has been widely used clinically.There are no toxic and side effects at conventional doses,and it is worth popularizing and applying.

Effects of an immunosuppressive active component of Periplocae Cortex (Periploca sepium Bge.) on positive selection of thymocytes in vitro

Objective:To determine the effect of an immunosuppressive active component (periploside A) isolated from the stem bark of Periplocae Cortex (Periploca sepium Bge.),a Chinese medicinal herb used in the treatment of rheumatoid arthritis for centuries in China,on positive selection of thymocytes in vitro.Methods:Female C57BL/6 mice at 6 weeks of age were housed in specific pathogen-free conditions.Double-positive thymocytes from C57BL/6 mice were induced into positive selection in vitro with or without periploside A treatment.Cell viability and expression of CD69,CD4,and CD8 were analyzed by flow cytometry.Results:Flow cytometric examination of thymocyte populations revealed that the percentage of CD8+ single-positive thymocytes was decreased by periploside A upon differentiation induced by an anti-CD3 antibody.However,the percentage of CD4+ single-positive thymocytes was decreased by periploside A upon differentiation induced by phorbol 12-myristate 13-acetate/ionomycin.Expression of CD69 plays a major role in prohibiting differentiation of thymocytes.Treatment with periploside A decreased CD69 expression in thymocytes.Conclusion:These results demonstrate that periploside A influences positive selection of thymocytes in vitro.

Active component of Isatidis Radixon insulin resistance in diabetes mellitus rat

OBJECTIVE To investigate the role of active component of Isatidis Radix on insulin resistance in the diabetes mellitus rat.METHODS To induce diabetic rat model with long-term high sugar and high fat plus low-dose streptozotocin(25 mg·kg-1).Then rats were randomly divided into 6 groups:control group,model group,rosiglitazone maleate group(0.3mg·kg-1),high(100mg·kg-1),middle(50mg·kg-1)and low(25 mg·kg-1)active component of Isatidis Radix group.Drugs were adiministered orally once a day.After four weeks,following substances were measured:serum fasting blood glucose,total cholesterol,triglycerides,high density lipoprotein,low density lipoprotein,free fatty acids,fasting insulin,insulin index,pathological observation and immunohistochemistry technology of pancreas islet.RESULTS High and middle active component of Isatidis Radix group could decrease serum FBG,TC,TG,LDL,FFA,FINS and increase serum HDL,ISI;the damage of the pancreas islet has been restoration partly.CONCLUSION Active component of Isatidis Radix could improve insulin resistance in diabetic rats,which might be related to improvement of the function of pancreas islet.

LW-AFC and its active components ameliorate corticosterone-induced long-term potentiation impairment in mice

OBJECTIVE LW-AFC is extracted from the classical traditional Chinese medicinal prescription-Liuwei Dihuang Decoction.Previous studies have showed that LW-AFC could improve learning&memory ability in amny animal models.In this study,we focused on evaluating the effect of several main active components fromLW-AFC(B-B;loganin,LOG;morroniside,MOR;paeoniflorin,PF and stachyose,STA)on LTP.METHODS In vivo recording of LTP was used in this study to evaluate the effects of LW-AFC and it′s active components on coticorsterone(Cort)induced LTP impairment.RESULTS The results showed that LW-AFC could ameliorate Cort-induced LTP impairment.The effect of LW-AFC was abolished when the immune function was inhibited.Single administration(ig,ip,icv)of any of the components had no effect on Cort-induced LTP impairment.Consecutively intragastric administration or intraperitoneal injections(chronic administration)of B-B,LOG,MOR or PF for 7 d showed protective effect on Cort-induced LTP impairment.Intragastric administration of STA for 7 d protected LTP from impairment induced by Cort,while there was little improving effect when STA was administrated via intraperitoneal injection.In addition,when the intestinal microbiota was disrupted by applying the antibiotic cocktail,STA showed little protective effect against Cort.CONCLUSION In conclusion,LW-AFC and it′s components showed positive effects against cort induced LTP impairment,it seems that all displayed protective effects via indirectly,immune modulation might be the common pathway for all components;the exact pathways are different in each component,B-B,LOG,MOR and PF could be absorbed into the bloods tream and then modulate the peripheral immune function,while STA could not be absorbed and modulates the immune function via modulating intestinal microbiota.Further studies are needed to invesgate the underlying mechanisms and the synergetic effects of all components.

Optimization of Extraction Process for Antioxidant Active Components in Seeds of Firmiana platanifolia

[Objectives]To optimize the extraction process of antioxidant active components from seeds of Firmiana platanifolia.[Methods]The seeds of F.platanifolia were taken as the research object.The primary samples of seeds of F.platanifolia were prepared following the procedure of selection,cleaning,shelling,drying and pulverization.The DPPH·(1,1-diphenyl-2-picrylhydrazyl)scavenging rate of the extract of seeds of F.platanifolia was used as an indicator,to conduct the single factor experiment for determining optimum single factors such as extraction solvent,extraction time,solid-to-liquid ratio,and extraction temperature.Then the experimental design was optimized by the response surface methodology.[Results]Single factor experiment showed that the optimal extraction solvent for the antioxidant active components of F.platanifolia seeds was ethyl acetate,the optimal extraction time was 50 min,the optimum solid-to-liquid ratio was 1∶6 g/mL,and the optimal extraction temperature was 60℃.The response surface optimization experiment showed that the optimal extraction process of the antioxidant active component extract of F.platanifolia seeds was:the extraction solvent was ethyl acetate,the extraction time was 45 min,the solid-to-liquid ratio was 1∶5 g/mL,and the extraction temperature was 55℃,which was basically consistent with the results of single factor experiment.Under the optimal extraction conditions,the DPPH·scavenging rate of ethyl acetate extract(200 mg/mL)of F.platanifolia seeds was 94.25%,which was equivalent to that of vitamin E(V E)solution(147.39 mg/L)dissolved with ethyl acetate.[Conclusions]The ethyl acetate extract of F.platanifolia seeds has a strong antioxidant capacity of eliminating DPPH·in vitro.

Changes in Active Components before and after Microorganism Fermentation of Rhizoma Paridis(Chonglou)

[Objectives] To study the changes in active components before and after microorganism fermentation of Rhizoma Paridis( Chonglou). [Methods]Analytical methods using total saponins and total flavonoids as indicators were established. UV spectrophotometry was used to determine the changes in active components before and after fermentation of Rhizoma Paridis. [Results] The content of total saponins decreased after fermentation,while the content of total flavonoids increased. [Conclusions]The content of total saponins decreased after fermentation and the content of total flavonoids increased. The fermentation process of Monascus purpureus Went. needs further optimization.

Gecko Active Components Regulates Endoplasmic Reticulum Stress to Induce the Apoptosis of KYSE150 Cells through PERK Pathway

Objective: Gecko active components (GACs), extracted from the powder of whole Gecko, have been reported to be effective against esophageal squamous cell carcinoma (ESCC). Endoplasmic reticulum stress (ERs) has been regarded as an important cause for pathogenesis of esophageal squamous cell carcinoma (ESCC). In this paper, we aimed to study the effect of GACS on apoptosis of human esophageal carcinoma KYSE150 cells and to analyze the underlying signaling pathway. Methods: MTT assay was used to detect the viability of KYSE150 cells, and Flow cytometry was applied to detect reactive oxygen species (ROS), calcium generation, and the level of mitochondrial membrane potential (MMP). Western blot analysis was applied to observe the expression of apoptosis-related proteins and endoplasmic reticulum stress (ERs)-related proteins in KYSE150 cells. Results: The results showed that GACs inhibited KYSE150 cell vitality in a dose- and time-dependent manner. Not only that, GACs could up-regulated ERs-related and apoptosis-related proteins expression, and the content of ROS and calcium were significantly increased, and also, the level of MMP was significantly decreased. Conclusion: The results of this report suggested that induction of apoptosis occurs through the ERs dependent signaling pathways.

Biological Active Components of Selected Medical Fungi

According to official data, about 2000 mushrooms belong to the category of medical mushrooms, while over 600 have already confirmed medical properties. The aim and task of this work were to collect, analyze and process scientific and expert data of biologically active components of selected Basidiomycetes fungi: Letinula edodes, Ganoderma Lucidum, Grifola frondosa, Trametes versicolor and Inonotus obliquus. Areas of fungi therapy and the search for new immunomodulatory agents are far from being restricted to these species alone, however, these five may serve as typical representatives of widespread medicinal fungi used in both traditional medicine and modern biomedical research. Their biologically active components have different pharmacological effects, and beta-glucan polysaccharides, which are recognized as immunomodulators, are of particular importance. Many of the fungal beta-glucans tested have switched to pharmaceuticals such as Lentinan, Sonifilan, Krestin and GanoPoly, which speaks to their pharmacological and research potential. Citing the results of scientific advances in the last two decades, the results of preclinical tests and the results of clinical studies can confirm that supplementation with medical fungi can increase treatment success or mitigate the negative side effects of different therapies. A long-term weakened immune system is a risk factor for malignancies, so it can be concluded that disease prevention is beneficial for each individual and deserves the same attention paid to treating the disease.

Effects of Different Cultivation Media and Periods on the Content of Main Active Components of Cordyceps militaris Strain QC04

In this study,Cordyceps militaris strain QC04 was cultivated in oat,rice,and wheat media for different time periods.We studied the effects of different cultivation media and periods on the fruiting body biomass and active components of C.militaris,aiming to provide reference for the production and utilization of C.militaris QC04.The results showed that the dry weight of the fruiting body of C.militaris was the highest in the wheat medium,moderate in the oat medium,and the lowest in the rice medium.The content of cordycepin and adenosine in the fruiting body and residual medium was higher in the oat and rice media than in the rice medium.The content of cordycepin and adenosine in fruiting body and residual medium peaked on day 55.Furthermore,the content of cordycepin in the fruiting body was lower than that in the residual medium,while the content of adenosine showed an opposite trend.The content of cordycepic acid in the rice medium was generally higher than that in the oat and wheat media.As the cultivation period extended,the fruiting body biomass declined and the content of cordycepic acid in the fruiting body increased slightly.