Protective Effects of Annona Muricata Linn. (Annonaceae) Leaf Aqueous Extract on Serum Lipid Profiles and Oxidative Stress in Hepatocytes of Streptozotocin-Treated Diabetic Rats

Extracts from various morphological parts of Annona muricata Linn. (Annonaceae) are widely used medicinally in many parts of the world for the management, control and/or treatment of a plethora of human ailments, including diabetes mellitus (DM). The present study was undertaken to investigate the possible protective effects of A. muricata leaf aqueous extract (AME) in rat experimental paradigms of DM. The animals used were broadly divided into four (A, B, C and D) experimental groups. Group A rats served as ‘control’ animals and received distilled water in quantities equivalent to the administered volumes of AME and reference drugs'' solutions intraperitoneally. Diabetes mellitus was induced in Groups B and C rats by intraperitoneal injections of streptozotocin (STZ, 70 mg kg⁻¹). Group C rats were additionally treated with AME (100 mg kg⁻¹ day⁻¹, p.o.) as from day 3 post STZ injection, for four consecutive weeks. Group D rats received AME (100 mg kg⁻¹ day⁻¹ p.o.) only for four weeks. Post-euthanization, hepatic tissues were excised and processed biochemically for antioxidant enzymes and lipid profiles, such as catalase (CAT), reactive oxygen species (ROS), glutathione (GSH), superoxide dismutase (SOD), glutathione peroxidase (GSH-Px), thiobarbituric acid reactive substances (TBARS), triglycerides (TG), total cholesterol (TC), high density lipoprotein (HDL) and low density lipoprotein (LDL), respectively. Treatment of Groups B and C rats with STZ (70 mg kg⁻¹ i. p.) resulted in hyperglycaemia, hypoinsulinaemia, and increased TBARS, ROS, TC, TG and LDL levels. STZ treatment also significantly decreased (p<0.05) CAT, GSH, SOD, GSH-Px activities, and HDL levels. AME-treated Groups C and D rats showed significant decrease (p<0.05) in elevated blood glucose, ROS, TBARS, TC, TG and LDL. Furthermore, AME treatment significantly increased (p<0.05) antioxidant enzymes'' activities, as well as serum insulin levels. The findings of this laboratory animal study suggest that A. muricata extract has a protective, beneficial effect on hepatic tissues subjected to STZ-induced oxidative stress, possibly by decreasing lipid peroxidation and indirectly enhancing production of insulin and endogenous antioxidants.     

番荔枝子中4个新的邻双四氢呋喃型番荔枝内酯

目的 研究番荔枝Annona squamosa种子的化学成分。方法 通过多种现代色谱技术对番荔枝子超临界CO₂提取物的化学成分进行分离纯化,并根据理化性质和谱学数据确定其结构。结果 从番荔枝子中分离得到7个化合物,分别鉴定为3-[12-[5-[5-(1-羟基十二烷基)-2-四氢呋喃基]-2-四氢呋喃基]-9,12-二羟基十二烷基]-5-甲基-2(5H)-呋喃酮（1）、3-[11-[5-[5-(1-羟基癸烷基)-2-四氢呋喃基]-2-四氢呋喃基]-8,11-二羟基十一烷基]-5-甲基-2(5H)-呋喃酮（2）、3-[9-[5-[5-(1,3-二羟基十四烷基)-2-四氢呋喃基]-2-四氢呋喃基]-9-羟基壬烷基]-5-甲基-2(5H)-呋喃酮（3）、3-[8-[5-[5-(1-羟基十四烷基)-2-四氢呋喃基]-2-四氢呋喃基]-2,8-二羟基辛烷基]-5-甲基-2(5H)-呋喃酮（4）、阿诺西林甲（5）、annosquacin A（6）和乙酰紫玉盘素（7）。结论 化合物1～4为4个未见报道的新邻双四氢呋喃型番荔枝内酯类化合物,分别命名为顺式-11-羟基鳞状辛素丙（1）、10-羟基鳞状辛素（2）、鳞状亭素戊（3）和鳞状亭素己（4）。     

超临界CO2萃取番荔枝种子中布拉他辛的工艺研究

目的:筛选超临界CO2流体萃取番荔枝种子中布拉他辛的最佳工艺条件。方法:用HPLC法测定布拉他辛的含量,并采用正交试验优化超临界CO2流体萃取布拉他辛的工艺条件。结果:超临界CO2流体萃取布拉他辛的最佳工艺条件为:萃取压力为30MPa,萃取温度为35℃,萃取时间为2h,夹带剂(无水乙醇)用量为0.3mL/g。结论:超临界CO2流体萃取法可有效提取番荔枝种子中的布拉他辛,该方法切实可行。     

番荔枝种子的化学成分研究

目的 研究番荔枝Annona squamosa种子的化学成分。方法 利用色谱分离纯化,根据化合物的理化性质和波谱数据进行结构鉴定。结果 分离鉴定了26个化合物,其中10个为双四氢呋喃环型番荔枝内酯类化合物,分别为泡番荔枝辛（1）、番荔辛（2）、去乙酰紫玉盘素（3）、去乙酰异紫玉盘素（4）、大花紫玉盘素A（5）、motrilin（6）、番荔枝塔亭丁（7）、番荔枝塔亭戊（8）、番荔枝塔亭甲（9）、12, 15-顺式番荔枝塔亭甲（10）。结论 化合物4和10为首次从番荔枝种子中分离得到。     

光叶番荔枝提取物抗肿瘤作用的实验研究

研究光叶番荔枝提取物对小鼠移植性肉瘤S180瘤体生长的抑制作用。定量称取光叶番荔枝提取物。用1％CMC-Na研磨配制成所需浓度的混悬液。将制备的肿瘤细胞悬液，以0.2ml／只接种于小鼠右前肢腋部皮下．24h后将其随机分为模型组、环磷酰胺组及光叶番荔枝组．并开始用药。各组均连续给药7d．停药后处死小鼠。剥取瘤块称重．计算抑瘤率。结果：光叶番荔枝提取物对小鼠移植性肉瘤S180有明显的抗肿瘤作用．抑瘤率可达64％-68％。     

番荔枝酰胺的全合成研究

番荔枝(Annona squamosa)是番荔枝科番荔枝属植物,有抗菌和抗肿瘤作用。番荔枝酰胺(squamosamide)是从该植物中提取得到的一个新化合物。为进一步探明该化合物的药理活性,进行了全合成研究工作。经七步反应首次制得天然目标物,总收率14%。     

Studies On The Use Of “Slimax”, A Chinese Herbal Mixture,In The Treatment Of Human Obesity

A phytochemical preparation known as “Slimax” was administered orally to human volunteers for a six week period, using a double-blind experimental method. This preparation is an aqueous extract of the Chinese medicinal plants Hordeum vulgare , Polygonatum multiflorum , Dimocarpus longan , Ligusticum sinense , Lilium brownii and Zingiber officinale . Treatment with Slimax resulted in a significant decrease in parameters such as body weight, waist and hip circumference, and Body Mass Index (BMI), in all subjects tested. The basis of action was shown to be through modification of lipid metabolism, with significant effects on both the accumulation and the release of lipid from adipose tissue. The experimental results indicate a great potential for the use of this herbal preparation in treatment of human obesity.     

HPLC法测定番荔枝种子中泡番荔枝辛的含量

目的：采用HPLC法测定番荔枝种子中泡番荔枝辛的含量。方法：采用HPLC法测定。色谱柱：HederaODS-3（250 mm×4.6 mm,5μm）,流动相为甲醇-水（90∶10）,流速为1.0 mL·min^-1;检测波长为220 nm,柱温25℃。结果：进样量在2.01～20.1μg范围内时,其质量与色谱峰面积的线性关系良好（r=0.999 8）。泡番荔枝辛平均回收率为99.7%,RSD为2.2%（n=6）。测得2008年和2009年采收的番荔枝种子中泡番荔枝辛的含量分别为1.09%和1.42%。结论：本法简便,灵敏,分离度良好,可用于番荔枝种子中泡番荔枝辛的含量测定。     

番荔枝种子的化学成分研究

目的研究番荔枝Annona squamosa种子的化学成分。方法利用色谱分离纯化,根据化合物的理化性质和波谱数据进行结构鉴定。结果分离鉴定了26个化合物,其中10个为双四氢呋喃环型番荔枝内酯类化合物,分别为泡番荔枝辛(1)、番荔辛(2)、去乙酰紫玉盘素(3)、去乙酰异紫玉盘素(4)、大花紫玉盘素A(5)、motrilin(6)、番荔枝塔亭丁(7)、番荔枝塔亭戊(8)、番荔枝塔亭甲(9)、12,15-顺式番荔枝塔亭甲(10)。结论化合物4和10为首次从番荔枝种子中分离得到。     

Anticonvulsant effect of Annona diversifolia Saff. and palmitone on penicillin-induced convulsive activity. A behavioral and EEG study in rats

PURPOSE: To evaluate hypnotic and anticonvulsant activities of Annona diversifolia Saff. and palmitone by using behavior and electroencephalographic (EEG) analysis in an experimental model of focal seizures in rats. METHODS: For hypnotic assessment, EEG analysis of polysomnographic slow-wave sleep (SWS) and rapid eye movement (REM) sleep for a 1 h period were performed after vehicle, A. diversifolia extract or palmitone, administration. For anticonvulsant effect, 60 minutes after treatments, EEG and behavior were analyzed during penicillin-induced seizures. Latency to the onset of the first paroxystic spike, first seizure and frequency, as well as seizure severity using Racine's scale, were determined. RESULTS: Palmitone, but not A. diversifolia extract, produced a delay in the latency to the SWS phase. In addition, both palmitone and extract decreased SWS duration and accumulated REM sleep phase. With regard to the seizures, both the extract and palmitone increased the latency to the onset of spikes and seizures, but also decreased the duration of penicillin-induced seizures. This reduction in the EEG recordings was associated with an attenuation in the severity of behavioral seizures. CONCLUSIONS: A. diversifolia and palmitone did not produce a sedative-hypnotic effect although both of them were effective in reducing the severity of behavioral and EEG seizures induced by penicillin in rats, suggesting that the diminution in the paroxystic activity by A. diversifolia is likely produced by palmitone through GABAergic neurotransmission. This study justifies and reinforces the traditional use of this plant in epilepsy.