A therapeutic potentiality and toxicity concern of nutrient plant Annona squamosa Linn.

Annona squamosa Linn.fruit is famous for its nutritional value with a long history of medicinal benefits due to the presence of many phytochemicals,including alkaloids,diterpenes,essential oil,phytopeptides,etc.Several studies envisaged that Annona squamosa possesses cytotoxic,diuretic,antiurolithiatic,antitumor,anti-psoriatic,antioxidant,and hepatoprotective properties.This plant is traditionally used for the treatment of wound infection,dysentery,seizure,tumors,fever,vomiting,parasitic infections,hypertension,thyroid,toothache,acne,heart disease,inflammation,diabetes,hair loss,dandruff,hemorrhage,maggot-infected sores,abortifacient,and cough.However,some chemical constituents isolated from the plant have shown specific toxic effects in human and animal models,such as acute oral toxic effects,genotoxic,neurotoxic,and ocular toxic.The plant has diverse pharmacological actions,the seeds of this plant possess a genotoxic effect but on the contrary,the bark of the plant shows genoprotective activity.A large number of ethnobotanical studies reported the seed of this plant is used to induce abortion in humans,but a scientific study carried out in pregnant rats reported aqueous seed extract of the plant did not interfere with reproductive performance.The presented review summarized the traditional uses,pharmacological,and toxicological activities of the isolated compounds from this plant.Additionally,some patents and commercial products related to Annona squamosa are also brought up in this article to explore its application which would attract the scientific community to search out its hidden side.

Anti-proliferative effect of Annona extracts on breast cancer cells

Backgorund:Fruits and seed extracts of Annona montana have significant cytotoxic potential in several cancer cells.This study evaluates the effect of A.montana leaves hexane extract on several signaling cascades and gene expression in metastatic breast cancer cells upon insulin-like growth factor-1(IGF-1)stimulation.Methods:MTT assay was performed to determine the proliferation of cancer cells.Propidium iodide staining and flow cytometry analysis of Annexin V binding was utilized to measure the progression of the cell cycle and the induction of apoptosis.Protein expression and phosphorylation were determined by western blotting analysis to examine the underlying cellular mechanism triggered upon treatment with A.montana leaves hexane extract.Results:A.montana leaves hexane(subfraction V)blocked the constitutive stimulation of the PI3K/mTOR signaling pathways.This inhibitory effect was associated with apoptosis induction as evidenced by the positivity with Annexin V and terminal deoxynucleotidyl transferase dUTP nick end labeling(TUNNEL)staining,activation of caspase-3,and cleavage of PPAR.It also limited the expression of various downstream genes that regulate proliferation,survival,metastasis,and angiogenesis(i.e.,cyclin D1,survivin,COX-2,and VEGF).It increased the expression of p53 and p21.Interestingly,we also observed that this extract blocked the activation of AKT and ERK without affecting the phosphorylation of the IGF-1 receptor and activation of Ras upon IGF-1 stimulation.Conclusion:Our study indicates that A.montana leaves(sub-fraction V)extract exhibits a selective anti-proliferative and proapoptotic effect on the metastatic MDA-MB-231 breast cancer cells through the involvement of PI3K/AKT/mTOR/S6K1 pathways.

Evaluation of the Nutritional Value and Acute Toxicity of the Seeds of the Fruit of Annona muricata L. (Sursop) Consumed in Kinshasa

In this paper, the author aimed to determine the nutritional value of soursop (Annona muricata L. fruit) consumed in Kinshasa as well as the study of the acute toxicity of its seeds. The fruit of Annona muricata L. was sampled according to the ISO 7002 standard for agricultural and food products. The selected fruits were ripe, without physical damage. The usual analytical methods allowed the determination of the nutritional value of the fruit pulp of Annona muricata L. The water content was measured by the method of loss of mass on drying. The total amount of ash was determined by incineration in the oven at 550°C. The mineral elements were determined by inductively coupled plasma spectrometry (ICP0). The determination of acute toxicity was carried out on 25 female mice of the NMRI SUISSE species according to OECD 425 guidelines. For 100 grams of fresh material from the fruit pulp, we noted a very high water content of 84% ± 6%. We also note a particularly high amount of carbohydrates with a rate of 12.2% ± 2%. Protein and lipid content were relatively low at 1% ± 0.01% and 0.7% ± 0.3% respectively. The dietary fiber content was 0.8% ± 0.2%. An energy value of 49.3 Kcal per 100 grams of pulp was determined. The LD 50 obtained was 3320 mg/kg, indicating slight toxicity of soursop seeds. The results of this study show that the white pulp of the fruit of Annona muricata L. consumed in Kinshasa is rich in carbohydrates when we compare it to others biomolecules. It also contains dietary fiber and mineral salts making soursop an excellent constituent of a weight loss diet with a low energy intake.

The anti-diabetic effect and possible mechanism of the Annona muricata L.root extract in type 2 diabetic mice

Objective:To investigate the anti-diabetic effect of the root extract of Annona muricata(AME)in streptozotocin-nicotinamide-induced type 2 diabetic(T2DM)mice.Methods:After 4 weeks of high-fat diet,ICR mice were given 1 g/kg nicotine and 120 mg/kg streptozotocin(STZ)orally to construct a T2DM model.The T2DM mice were randomly divided into five groups:model group,200 mg/kg metformin group and 50,100,200 mg/kg AME groups.Drugs were oral administered continuously for 4 weeks.Fasting blood glucose and body weight were measured weekly.Oral glucose tolerance test(OGTT)and detection of serum glycated hemoglobin(HbA1c)level were performed one week before the end of the experiment.At the end of drug administration,serum total cholesterol(TG),triglycerides(TC),low-density lipoprotein levels(LDL-C)and insulin levels were tested by lipid detection kits;homeostasis model assessment-estimated insulin resistance(HOMA-IR)and HOMA-βindexes were calculated.Liver and kidney tissues were weighed to calculate organ indices and pathological tests were performed.Western blot was performed in the liver to detect adenosine monophosphate-activated protein kinase(AMPK),acetyl coenzyme A carboxylase(ACC),glucose-6-phosphate carboxylase(G6Pase),and phosphoenolpyruvate carboxykinase(PCK1)protein expression.Results:with 200 mg/kg AME significantly reduced fasting blood glucose,HbA1c,TG and LDL-C levels,protected liver and kindey in diabetic mice,decreased the area under the OGTT curve,inhibited ACC and G6Pase protein expressions,and activated AMPK protein expression.Conclusion:AME showed good therapeutic activity against T2DM,and the mechanism may be related to the activation of AMPK and inhibition of ACC and G6Pase proteins.

Ethanol extract of Annona muricata Linn fruit perform antidiabetic effect on type 2 diabetic mice through α-glucosidase inhibition

Objective:To explore the anti-diabetic effects and its underlying mechanism of Annona muricata Linn fruit ethanol extract(AME).Methods:Streptozotocin-induced type 2 diabetic(T2DM)mouse model was constructed.Those diabetic mice were randomly grouped and given 50 mg/kg acarbose or AME(200 mg/kg,100 mg/kg or 50 mg/kg)for four weeks.The body weight,postprandial blood glucose and glycosylated hemoglobin levels were measured during the administration.After the administration,a glucose tolerance test was performed,and the levels of triglycerides,cholesterol and low-density lipoproteins in mice were detected by biochemical test kits.The inhibitory activity of AME onα-glucosidase in vivo and in vitro was determined by enzyme inhibition tests.Results:AME significantly reduced weight gain,postprandial blood glucose,glycosylated hemoglobin and low-density lipoprotein levels in T2DM mice;enhanced glucose tolerance and pancreaticβ-cell function of T2DM mice;inhibitedα-glucosidase activity in mouse intestine in an noncompetitive manner.Conclusion:AME may noncompetitive inhibitα-glucosidase activity and reduce postprandial glucose intake to achieve a therapeutic and regulatory effect on type 2 diabetes.

基于理化分析和机器学习研究低温气调对采后番荔枝冷害的影响

本文旨在探究气调包装对番荔枝冷害的影响,并通过机器学习解析各指标与冷害的关系。以室温(RT,25℃)、低温(LT,10℃)和低温气调包装(CA,10℃)贮藏条件下的果实为试验材料,测定7 d内果肉硬度、冷害指数(CI)、总酚、相对电导率(EC)、苯丙氨酸裂解酶(PAL)活性等理化指标。结果表明,低温贮藏有效延缓番荔枝后熟,抑制软化,但易造成冷害现象,表现为果肉出现水浸状损伤,细胞膜透性增加,丙二醛积累。在此基础上,建立多种机器学习算法,筛选出预测CI的最优模型为Ridge回归。解释性分析(SHapley Additive exPlanations,SHAP)显示,贮藏时间、可溶性固形物、失重率、可溶性蛋白和总酚对模型贡献较大,与低温胁迫紧密联系。低温结合气调通过增加可溶性物质和酚类含量,提高机体渗透调节和清除活性氧能力,从而维持膜结构完整性以缓解低温冷害。

AP番荔枝在广西崇左的引种表现及栽培技术

为了调优热带水果品种比例,于2016年自湛江引入优良品种AP番荔枝进行试种。经过7年的引种栽培试验,AP番荔枝在广西崇左生长结果表现良好,果实大小中等、均匀。果实性状方面,AP番荔枝平均单果重297.8g,比普通番荔枝品种(CK)的181.6g增加64.0%,差异达极显著;可食率66%,比CK的57%增加15.8%,可溶性固形物24.5%,比CK的20.5%提高19.5%,这两项指标差异达显著;单果种子28粒,比CK的45粒减少37.8%,差异达极显著;可溶性糖18.3%,比CK的16.8%提高8.90%,平均株产量比CK高4.2%~10.5%,两项指标差异不显著。AP番荔枝具有早结丰产特性,其果实大、品质好、可食率高、可溶性固形物高,适合广西崇左发展种植。

A New Cytotoxic Acetogenin from the Seeds of Annona squamosa

A new Annonaceous acetogenin, squamostolide (1), was isolated from the seeds of Annona squamosa. Its structure was elucidated based on spectroscopic methods and comparison with known compounds. It is the first example of Annonaceous acetogenin with each of the two ends of the aliphatic chain bearing a g-lactone. The new compound exhibited cytotoxic activity in vitro against bel-7402 and CNE2 human tumor cell lines.

Evaluation of the acute and sub acute toxicity of Annona senegalensis root bark extracts

Objective:To investigate the safety profile of Annona senegalensis（A.senegalensis）.Methods: Dried powdered root-bark of A.senegalensis was prepared by Sohxlet extraction using methanolmethylene chloride（1:1） solution and concentrated to obtain the methanol-methylene chloride extract（MME）.MME was fractionated to obtain the n-hexane（HF）,ethylacetate（EF） and methanol（MF） fractions.Acute toxicity(LD50) test was performed with MME,HF,EF and MF in mice by oral route.The sub acute toxicity studies were performed in rats after 14 days of MME administration while haemalological and biochemical parameters were monitored.Results: Medium lethal（LD-（50）） values of 1 296.3 808.1 265 and 2 154 mg/kg were obtained for the MME.MF, HF and EF,respectively.The sub-acute toxicity studies indicated a significant（P【0.05） increase in the body weight of both the treated rats and the control.The haematological tests indicated no change in the packed cell volume values but a significant（P【0.05） increase in the total WBC count at 100 and 400 mg/kg doses.The differential analysis showed a decrease in the nutrophils and a non-significant increase in the lymphocyte counts.The liver transaminase enzymes, alanin transaminase and aspartate transaminase showed no significant increase compared to the control.Histopathological examination of the liver sections also indicted no obvious signs of hepatotoxicity except with the 400 mg/kg dose that showed degeneration and necrosis of the hepatocytes.Conclusions:These results indicated that the root bark extracts of A.Senegalensis are safe at the lower doses tested,and calls for caution in use at higher doses in treatment.

Annona muricata:Is the natural therapy to most disease conditions including cancer growing in our backyard?A systematic review of its research history and future prospects

Annona muricata(A.muricata)is a tropical plant species belonging to family Annonaceae and known for its many medicinal uses.This review focuses on the research history of its traditional uses,phytochemicals,pharmacological activities,toxicological aspects of the extracts and isolated compounds,as well as the in vitro propagation studies with the objective of stimulating further studies on this plant for human consumption and treatment.A.muricata extracts have been identified in tropical regions to traditionally treat diverse conditions ranging from fever to diabetes and cancer.More than 200 chemical compounds have been identified and isolated from this plant,the most important being alkaloids,phenols and acetogenins.Using in vitro studies,its extracts and phytochemicals have been characterized as antioxidant,anti-microbial,anti-inflammatory,insecticidal,larvicidal,and cytotoxic to cancer cells.In vivo studies have revealed anxiolytic,antistress,anti-inflammatory,immunomodulatory,antimalarial,antidepressant,gastro protective,wound healing,hepato-protective,hypoglycemic,anticancer and anti-tumoral activities.In silico studies have also been reported.In addition,clinical studies support the hypoglycemic as well as some anticancer activities.Mechanisms of action of some pharmacological activities have been elucidated.However,some phytochemical compounds isolated from A.muricata have shown a neurotoxic effect in vitro and in vivo,and therefore,these crude extracts and isolated compounds need to be further investigated to define the magnitude of the effects,optimal dosage,and mechanisms of action,long-term safety,and potential side effects.Additionally,more clinical studies are necessary to support the therapeutic potential of this plant.Some studies were also found to have successfully regenerated the plant in vitro,but with limited success.The reported toxicity notwithstanding,A.muricata extracts seem to be some of the safest and promising therapeutic agents of the 21st century and beyond that need to be studied further for better medicinal formulations and diseases management.

Anti-lipid droplets accumulation effect of Annona montana(mountain soursop)leaves extract on differentiation of preadipocytes

The Annona genus is a member of Annonaceae,one of the largest families of plants across tropical and subtropical regions.This family has been used in several ethnomedicinal practices to treat a multitude of human diseases.However,the molecular mechanism underlying its effect on the lipid droplet formation and on the expression of adipogenic markers of this plant remain to be investigated.In this study,we examined whether the extracts from the aerial part of Annona montana affect in vitro differentiation of preadipocytes.For our investigations,both mouse embryo fibroblast 3T3-L1 and normal human primary subcutaneous preadipocytes were incubated with Annona montana extracts(-and its subfractions-)and then analyzed on preadipocyte differentiation,lipid content,lipid droplet size and number,the expression of adipogenic-specific transcriptional factors,as well as cell survival.From our examinations,we found the Annona montana ethyl acetate extract to exhibit a potent inhibitory effect on adipogenesis,without affecting cell survival,in a dose-dependent manner.Such inhibitory effects included a significant decrease in the accumulation of lipid content by both a dramatic reduction of size and number of lipid droplets.This extract strongly attenuated the expression of PPARγand HMGB2.It also inhibited the expression of CEBPα,FAS,and Akt without influencing Erk1/2 activities.Our findings suggest that specifically,the Annona montana ethyl acetate extract has a prominent inhibitory effect in cellular pathways of adipocyte differentiation by modulating specific gene expression,which is known to perform a pivotal role during adipogenesis.

SQUAMOSTATIN-B, A NEW POLYKETIDE FROM ANNONA SQUAMOSA (ANNONACEAE)

Squamostatin-B (1), a new polyketide or acetogenin, has been isolated from Annona squamosa L. (Annonaceae). Its structure and relative atereochemistry were elucidated on the basis of the spectral analyses of 1 and its derivatives, the acetate (2) and mesitoate (3).

Quantitative analysis of trigonelline in some Annona species by proton NMR spectroscopy

A quantitative ^(1)H NMR method(qHNMR)was used to measure the trigonelline content in the leaves of six species of the Annona genus.The methodology employed compared the intensities of the signals at δ9.14(H-2)andδ0.00,the internal standard TSP-d_(4).This measuring method was able to establish the concentration of trigonelline in the range from 0.67 to 10.04 mg·g^(-1) depending on the investigated extract.

<i>In Vitro</i>Clonal Propagation from Juvenile and Different Explant Types of Two Edible <i>Annonaceae</i>Species: <i>Annona muricata</i>L. and <i>Annona squamosa</i>L.

Annona muricata L. and Annona squamosa L. are tropical species whose fleshy fruit is edible. They offer real possibilities for socio-economic use, particularly in the fields of medicine, nutrition, ecosystem conservation and the poverty alleviation. This study was set up to evaluate different methods of micropropagation from juvenile material for the regeneration of these species. Thus, MS medium supplemented with [BAP 2 mg·L-1] i.e. M2 produced 2.87 newly formed shoots from the cotyledonary nodes of A. muricata. For the terminal apices of A. squamosa, it was MMS medium supplemented with [BAP 2 mg·L-1] i.e. MM2 that was most conducive to new shoot formation (3.12). The addition of 0.1 and 0.2 mg·L-1 of NAA in the M2 medium, made it possible to have the best elongations and average number of nodes for the new shoots from cotyledonary nodes of A. muricata (9.11 cm for 5.62 nodes). With A. squamosa, MM7 medium [MMS + BAP 1 mg·L-1 + KIN 1 mg·L-1] resulted in an average length of 9.05 cm with 5.62 nodes on average for the apical shoots. A 3-day rhizogenic induction period in the dark with [IBA 50 mg·L-1] and 2 g·L-1 of activated charcoal gave a rooting rate of 66.67% for shoots originating from the cotyledonary nodes of A. squamosa;while with vitroplants from cotyledonary nodes of A. muricata, a better rooting rate (83.33%) was obtained following a 5-day rhizogenic induction. After 30 days of acclimatization, the survival rate reached 83.33% for plants from the tips of A. muricata, whereas for A. squamosa, it was plants grown from cotyledonary nodes that had the same survival rate.

Evaluation of the anticonvulsant and muscle relaxant effects of the methanol root bark extracts of Annona senegalensis

Objective:To investigate the potentials of the root bark of Annona（A.） senegalensis in the control of seizure and related hypnotic and motor incoordination effects in mice using experimental models.Methods:The methanol extract（ME） of the root bark of A.senegalensis was studied in mice using pentylenetetrazole（PTZ） induced convulsions,phenobarbitone induced sleeping time and motor coordination test on rota-rod performance.Acute toxicity and lethality（LD50） lest as well as phytochemical analysis were also carried out.Results:The extract（200,400,800 mg/ kg） exhibited a non- dose dependent significant（P【0.05） delay in the onset of both tonic and clonic phases of seizure induced by PTZ（60 mg/kg,s.c.） as well as offered a 100%protection （200 mg/kg） in mice from PTZ induced seizures.The extract significantly（P【0.05） decreased the latency and increased the duration of phenobarbitone induced sleeping time.At 200 mg/kg, the extract exhibited a significant（P【0.05） motor incoordination.The acute toxicity test revealed an oral LD50 of 1 2%mg/kg,while the phytochemical studies showed the presence of alkaloids, resins,glycosides,carbohydrate,reducing sugar,flavonoids,terpenoids,saponins and tannins. Conclusion:The extract of A senegalensis possessed anticonvulsant activity with pronounced hypnotic and muscle relaxant effects.

Muricatenol, a Linear Acetogenin from Annona muricata (Annonaceae)

Muricatenol 1, a new acetogenin, has been isolated from the seeds of Annona muricata L.. Compound 1 is a C-37 acetogenin without any THF rings. with four hydroxyls and one double bond in the long aliphatic chain. The hydroxyls of 1 are located at C-4, C-10, C-18 and C-19. respectively. The vicinal diet at C-18/C-19 is threo-configuration, and the double bond at C-14/C-15 is cis-configuration.

Squamin-A,Novel Cyclopeptide from Annona squamosa

A novel cyclopeptide, squamin-A has been isolated from the seeds of Annona squamosa Linn.. The structure was elucidated by extensive 2D-NMR, FABMS and amino acid analysis in combination with Marfey's reagents as cyclo-[l-prolyl-l-(S-oxo)-methionyl-l-tyrosyl-l-glycyl-tythreonyl-l-valyl-l-alanyl-l-isoleucyl].

Anticancer activity test of ethyl acetate extract of endophytic fungi isolated from soursop leaf(Annona muricata L.)

Objective: To analyze anticancer activity of an ethyl acetate extract of endophytic fungi isolated from soursop leaf(Annona muricata L.). Methods: Anticancer activity of fungal extracts was determined by observing its toxicity against MCF-7(Michigan Cancer Foundation-7) cells in vitro by using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT) assay method. At an extract concentration of 100 μg/m L, 4 isolates out of 12 showed high activity against the cancer cell growth. The four isolates were then selected for further IC50 determination, by measuring the inhibition of cancer cell proliferation at extract concentration of 25 μg/m L, 50 μg/m L, 100 μg/m L, 200 μg/m L and 400 μg/m L. Results: Results showed that isolate Sir-G5 had the highest anticancer activity with an IC50 of 19.20 μg/m L. The best isolates were screened again using a normal cell(Chang cells) to determine its toxicity against normal cells. Results indicated that the extracts do not affect the proliferation of normal cells. Molecular identification showed that the fungal isolate Sir-G5 has a close relationship with Phomopsis sp. Conclusions: The endophytic fungi isolated from soursop leaf has the potential to be used as a source of anticancer agents.

Research Progress of Main Pests in Sweetsop ( Annona squamosa L. ) and Its Insecticide Activity

The research progress on pests and insecticide activity of Annona squamosa L. is summarized in the paper, including symptom, occurrence regularity and control methods. Furthermore, the comprehensive technique for controlling pests of A. squamosa in the future is preliminarily discussed.

A New Diterpenoid Dimer from Annona glabra

A new diterpenoid dimer annonebinide A has been isolated from the stems of Annona glabra. Its structure was determined to be ent-16a-hydroxykauran-17-yl ent-16b-kauran-17-oate on the basis of spectroscopic and chemical evidence.