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.

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.

<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.

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.

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.

<i>Annonaa muricata </i>Linn Leaf Induce Apoptosis in Cancer Cause Virus

Introduction: Now many studies conducted on the drug substance from nature that can serve as an anticancer agent as a potential chemoprevention agent, such as Annona muricata Linn leaf escort chemotherapy, which was flaring. The cancer cell in humans was included the loss of p53 protein function due to mutations in the protein gene. Other causes are that the p53 proteins are not functioning due to an increase in protein misfolding event chaperones and degradation events ubiquitous as binding by viral protein. Method: Cytotoxicity assay performed on 24 well plate micro-cultures. HeLa cells are as 2 × 104 cells in 100 mL in RPMI media. Created control is RPMI and solvent DMSO 0.25%. Cytotoxic Test performed by the method of calculation tryphan blue dye exclusion. Being fasted for 24 hours in the culture medium, then the cells are grown in micro-plate with media plus samples with a non-lethal concentration (LC50) of partition and fractionation Annona muricata Linn leaf. Sampling is performed at 24 hours. Each of these wells is calculated the number of living cells and made the curve of cell number and incubation time. Result: The results showed that HeLa cells are being LC50 partition of leaves Annona muricata Linn in ethyl acetate his cell death rate was higher (2000 μg/ml have 131.89%;15.625 μg/ml have 11.37%) and in ethanol-distillate water his cell death rate was lower (2000 μg/ml have 35.80%;15.625 μg/ml have 3.97%). Another results showed that HeLa cells are being LC50 fractionation of leaves Annona muricata Linn in chloroform his cell death rate was higher (2000 μg/ml have 91.86%;15.625 μg/ml have 2.68%) and in ethyl acetate, his cell death rate was lower (2000 μg/ml have 23.79%;15.625

Phytocompounds of Anonna muricata leaves extract and cytotoxic effects on breast cancer cells

Objective: To identify the phytochemical compounds from Annona muricata(A. muricata) and to determine their in vitro anti-proliferative activities against breast cancer cells, MCF7 and MDA-MB-231. Methods: A. muricata leaves were successively extracted by soxhlet method using n-hexane, ethyl acetate and methanol, and decocted with water. Each extract was analysed by gas chromatography mass spectrometry(GCMS) and characterized with Wiley and NIST library searches. Anti-proliferative activity of each extract was evaluated on MCF7 and MDA-MB-231 breast cancer cells using MTT assay. Results: The GCMS analysis of different solvent extracts of A. muricata leaves showed presence of different chemical groups of compounds such as steroids, terpenoids, phenolic compounds, sugars, sugars alcohol and others including vitamin E. Ethyl acetate leaves extract exhibited the lowest IC_(50) value on the MDA-MB-231 breast cancer cell and n-hexane leaves extract showed the the lowest IC_(50) value on the MCF-7 breast cancer cell. Conclusion: Steroids and phenolic compounds were the main phytocompound groups identified from all A. muricata leaves extracts. The antiproliferative activity of n-hexane and ethyl acetate extract towards breast cancer MCF7 and MDA-MB-231 respectively might be due to the presence of biologically active compounds in the extracts, hence, providing some scientific evidences of the effectiveness of its traditional usages.

Palm Red Mite Management with Soursop Seed Plant Residue Extracts

Raoiella indica Hirst, 1924 (Prostigmata: Tenuipalpidae), is one of the leading pest mites in palm and banana trees, however, there are few control methods available for this pest species. Therefore, this work aimed to evaluate the acaricidal effect of soursop seed extract (Annona muricata L.) on R. indica adults. The experiment was conducted in a completely randomized design using soursop seed extract with 7 replicates and 12 individuals of R. indica per replicate. The experimental units consisted of discs of coconut palm leaves (4 cm in diameter), with cotton moistened at the bottom of the Petri dish (10.0 × 1.2 cm) and around the disc to maintain turgor and prevent mites from escaping. The application was performed using an airbrush, connected to a calibrated compressor with a constant pressure of 1.3 psi and 1 mL of solution per repeat plate. The acaricidal effect was evaluated 24, 48, and 72 hours after spraying. Mortality data were corrected and submitted to Probit analysis (p ≤ 0.05) using the statistical program R, with the LC50 and LC90 calculated for the extract. At the maximum concentration (15%), the soursop seed extract showed mortality of 70% of individuals of R. indica, and the LC50 was 6.58%. It was concluded that the soursop seed extract showed acaricidal potential on R. indica in the laboratory.

刺果番荔枝根提取物改善2型糖尿病药效和作用机制研究

目的:研究刺果番荔枝根提物(AME)对2型糖尿病(T2DM)ICR小鼠的作用效果,探究其作用机制。方法:4周高脂饮食后,给予ICR小鼠口服1 g/kg烟酰胺和120 mg/kg链脲佐菌素(STZ)构建T2DM模型。按照模型组、200 mg/kg二甲双胍组和50、100、200 mg/kg AME组将T2DM鼠随机分为5组,连续给药4周。每周测空腹血糖和体重。实验结束前一周进行口服糖耐量实验(OGTT)并检测糖化血红蛋白(HbA1c)水平。给药结束后血清学检测总胆固醇(TG)、甘油三酯(TC)、低密度脂蛋白水平(LDL-C)和胰岛素水平;计算稳态评估模型HOMA-IR和HOMA-%β。Western blot法检测肝脏中单磷酸腺苷活化蛋白激酶(AMPK)、乙酰辅酶A羧化酶(ACC)、葡萄糖-6-磷酸羧化酶(G6Pase)和磷酸烯醇丙酮酸羧激酶(PCK1)表达量。结果:200 mg/kg AME明显降低了TT2DM小鼠空腹血糖、HbA1c、TG和LDL-C水平;明显降低了HOMA-IR和HOMA-%β指数;降低了OGTT曲线下面积;抑制了ACC和G6Pase蛋白表达水平,并激活了AMPK蛋白表达。结果:AME表现出了对T2DM良好的治疗活性,其机制可能与激活AMPK蛋白,抑制ACC和G6Pase蛋白表达有关。

刺果番荔枝果实乙醇提取物抑制α⁃葡萄糖苷酶治疗2型糖尿病的实验研究

目的:研究95%乙醇回流提取的刺果番荔枝果实提取物(AME)治疗2型糖尿病作用以及可能的机制。方法:利用链脲佐菌素诱发ICR小鼠建立2型糖尿病,随机分组,分别给予50 mg/kg阿卡波糖或者AME(200、100和50 mg/kg),连续给药4周。每周测定小鼠体重、餐后血糖水平。第3周测定糖化血红蛋白水平。给药结束后进行OGTT实验,检测血清生化指标。通过酶抑制实验测定AME对体内外α⁃葡萄糖苷酶抑制活性和选择性。结果:AME能控制2型糖尿病小鼠的体重增长,显著降低餐后血糖、糖化血红蛋白及低密度脂蛋白水平,增强小鼠机体糖耐受的能力;非竞争性抑制小鼠肠道内α⁃葡萄糖苷酶活性。结论:AME可能非竞争性抑制α⁃葡萄糖苷酶活性以控制机体对餐后葡萄糖摄入,发挥2型糖尿病治疗作用。

刺果番荔枝化学成分的研究

从番荔枝科番荔枝属植物刺果番荔枝（Ａｎｎｏｎａｍｕｒｉｃａｔａ）的种子分得五种番荔素类成分，经光谱分析，鉴定其中两种为新化合物，命名为：ｍｕｒｉｃａｔａｌｉｃｉｎ（Ｉ）和ｍｕｒｉｃａｔａｌｉｎ（ＶＩ），另三种为已知化合物：ａｎｎｏｎａｃｉｎ（Ｉ），ａｎｎｏｎａｃｉｎＡ（ＩＩ）和ａｎｎｏｎａｃｉｎ１０ｏｎｅ（ＩＶ）。在制备酸酯（ｍｅｓｉｔｏａｔｅ）衍生物过程中，又得到一新番荔素的酸酯Ｖｂ，与模型化合物比较，确认Ｖｂ是ｃｉｓＴＨＦａｎｎｏｎａｃｉｎＡｍｅｓｉｔｏａｔｅ。Ｖｂ的原化合物定名为ａｎｎｏｎａｃｉｎＢ。

刺果番荔枝种子中的新环肽──刺果番荔枝环肽A

从刺果番荔枝种子中得到１个新环肽，命名为刺果番荔枝环肽Ａ（ａｎｎｏｍｕｒｉｃａｔｉｎＡ）通过多种２Ｄ－ＮＭＲ技术、ｐｏｓ．ＦＡＢ－ＭＳ和氨基酸分析，其结构确定为坏（脯－苯丙－缬－丝－丙－甘），是１个环六肽。

番荔枝属3个资源树种的核型分析

应用改良去壁低渗-火焰干燥法制片,镜检,分析比较番荔枝属3个资源的核型。结果表明,阿蒂莫耶番荔枝、刺番荔枝为2倍体,而圆滑番荔枝为4倍体,阿蒂莫耶番荔枝、圆滑番荔枝有随体。核型公式分别为:阿蒂莫耶番荔枝2n=2x=14=14m;刺番荔枝2n=2x=14=12m+2sm;圆滑番荔枝2n=4x=28=14m+14sm。刺番荔枝属于1A核型,阿蒂莫耶番荔枝属于1B核型,光叶番荔枝属于2B核型。

刺果番荔枝中的番荔枝内酯（3）

刺果番荔枝中的番荔枝内酯（３）杨仁洲，吴淑君（中国科学院华南植物研究所，广州５１０６５０）关键词刺果番荔枝，番荔枝内酯ＡＮＮＯＮＡＣＥＯＵＳＡＣＥＴＯＧＥＮＩＮＳＦＲＯＭＡＮＮＯＮＡＭＵＲＩＣＡＴＡ（Ⅲ）￥ＹＡＮＧＲｅｎ－Ｚｈｏｕ；ＷＵＳｈｕ－Ｊｕｎ...

刺果番荔枝中的番荔枝内酯（2）

从刺果番荔枝（ＡｎｎｏｎａｍｕｒｉｃａｔａＬ．）的种子中分离了３个具有酮基的单四氢呋喃环型的番荔枝内酯Ｓ＿７，Ｓ＿８和Ｓ＿（１０），根据它们的［α］＿Ｄ、１ＨＮＭＲ，１３＿ＣＮＭＲ，ＭＳ及ＩＲ谱分析，分别推定为新－异阿诺纳辛－１０－酮（Ｓ＿７）、新阿诺纳辛－１０－酮（Ｓ＿８）和异－新阿诺纳辛－１０－酮（Ｓ＿（１０））。

刺果番荔枝根化学成分研究

目的研究刺果番荔枝(Annona muricata L.)根皮的化学成分。方法采用硅胶柱色谱、Sephadex LH-20柱色谱、高效液相色谱分离根皮乙醇提取物中的化合物,根据理化性质和波谱技术分析确定所得化合物的结构。结果从提取物中分离得到6个化合物,分别鉴定为annomontine(山番荔枝辛,1)、methoxyannomontine(2)、Isohemigossylic acid lactone-2-methyl ether(3)、1-(4'-Met hoxybenzyl)-5,6,7-trimethoxyisoquinoli(4)、thalimicrinone(5)、liriodenine(鹅掌楸碱,6)。结论化合物1~6均为首次从该植物中分离得到。

刺果番荔枝中的番荔枝内酯

从刺果番荔枝（Ａｎｎｏｎａ ｍ ｕｒｉｃａｔａ Ｌ．）的种子中分离到３ 个单四氢呋喃型番荔枝内酯类化合物，用波谱方法鉴定为海南哥纳香甲素（ｈｏｗ ｉｉｃｉｎ Ａ， Ｓ１３）、乙素（ｈｏｗ ｉｉｃｉｎ Ｂ， Ｓ５）和新化合物４－去氧海南哥纳香乙素（４－ｄｅｓｏｘｙｈｏｗ ｉｉｃｉｎ Ｂ， Ｓ２）。

番荔枝科两种植物花器官形态发生

用扫描电镜观察了囊瓣木(Saccopetalum prolificum)和刺果番荔枝(Annona muricata)花器官的形态发生过程。刺果番荔枝和囊瓣木花被片均为3轮,其中刺果番荔枝内轮花被片数目为3枚、5枚或7枚。囊瓣木花原基最初为圆锥形,最外轮3枚花被片很快发生,之后中、内轮花被片原基连续发生,3轮花被片互生。此时花原基为六边形。花被片分化完成时,圆球形雄蕊原基沿六边形花原基的6个边螺旋向心发生,最终近轮状排列于花原基上。刺果番荔枝的雄蕊较多(约1000枚),首先在中轮花被片所对的花原基边缘发生,之后大量雄蕊螺旋状发生。心皮分化的早期阶段,与雄蕊原基很相似,当心皮数目逐渐增多时,不能分辩出发生的顺序。成熟花中,心皮和雄蕊全都被毛覆盖,毛具有粘住传粉滴的作用。

Muricatin A和Muricatin B刺果番荔枝中的两个新番荔枝内酯

从刺果番荔枝(Annona muricata)的种子分离得到两个新成分,此两成分及其衍生化物经光谱分析,鉴定为两个新番荔枝肉酯,命名为Muricatin A和Muricatin B。它们属无THF环番荔枝内酯。