Paniculacin,a new coumarin derivative from Murraya paniculata

Paniculacin (1), a new coumarin derivative, has been isolated from the ethyl acetate soluble fraction of the ethanolic extract of Murraya paniculata along with umbelliferone, scopoletin, 4-hydroxybenzoic acid, trans-cinnamic acid, and β-sitosterol. Their structures were elucidated on the basis of spectral data.     

Inhibition of α-Glucosidase by Andrographis paniculata. Ethanol Extract in Rats

Abstract

In the current study, we investigated the effect of ethanol extract of Andrographis paniculata. (Burm.f.) Nees (Acanthaceae) (AP) on α.-glucosidase (EC 3.2.1.20) inhibition in both normal and streptozotocin-induced diabetic rats. Oral carbohydrate tolerance tests were performed in 18-h fasted rats with starch (3 g/kg), sucrose (4 g/kg), and glucose (2 g/kg) separately, in both normal and diabetic rats, 10 min after administration of 250 (D1), 500 (D2), 1000 (D3) mg/kg ethanol extract of AP, vehicle (control), and acarbose (Acar) 10 mg/kg, respectively. Blood samples were analyzed for blood glucose at 0, 30, 60, and 120 min after respective treatments and the peak blood glucose (PBG) and area under the curve (AUC) determined. Our results demonstrate that 500 mg, 1000 mg/kg ethanol extract of AP reduces and prolongs the PBG concentration, simultaneously decreasing AUC after starch and sucrose loading in normal and diabetic rats. Similarly, acarbose also reduced sucrose and starch induced blood glucose excursions, whereas it had no peak blood glucose suppressive effect after exogenous glucose load in both normal and streptozotocin-induced diabetic rats. The results suggest the possibility that the ethanol extract of AP may have PBG suppressive effect, post–carbohydrate challenge as evidenced by reduced PBG and AUC, which can be used effectively as a safer alternative to control postprandial hyperglycemia (PPH), especially in diabetic patients and borderline patients not properly controlled on diet alone.     

穿心莲质量标准研究

目的对穿心莲药材的有效成分进行定性定量鉴别,对水分、总灰分、酸不溶性灰分、浸出物及重金属含量进行定量测定,进一步完善穿心莲药材的质量标准。方法采用薄层色谱法对穿心莲中的穿心莲内酯和脱水穿心莲内酯进行定性鉴别,高效液相色谱法进行定量测定,常规检查项目按2010年版《中华人民共和国药典》(一部)附录Ⅸ A杂质检查法、Ⅸ H水分测定法中的烘干法、附录Ⅸ K灰分测定法、附录Ⅹ A浸出物测定法及Ⅸ E重金属检查法测定。结果10批穿心莲样品中穿心莲内酯和脱水穿心莲内酯及醇溶性浸出物含量均符合我国药典规定的标准。结论所建立的方法简便、准确,能作为质量标准以控制穿心莲药材的质量。     

布渣叶水煎液对非酒精性脂肪肝大鼠血脂及炎症反应影响研究

目的：观察布渣叶水煎液对非酒精性脂肪肝大鼠血脂、炎症反应的影响。方法：采用高脂饮食法制备大鼠模型,将48只Wistar雄性大鼠随机分为正常对照组、模型对照组、非诺贝特组、布渣叶水煎液组,分别灌服生理盐水、非诺贝特溶液、布渣叶水煎液。结果：布渣叶水煎液可降低非酒精性脂肪肝大鼠血清和肝组织TC、TG及肝指数,降低肝组织TNF-α、MCP-1和NF-κB等炎症因子的表达。结论：布渣叶水煎液对非酒精性脂肪肝大鼠血脂、炎症反应具有改善作用。     

基于网络药理学探讨穿心莲抗癌的作用机制

【目的】基于网络药理学探讨穿心莲抗癌的潜在作用机制。【方法】应用中药系统药理学技术平台(TCMSP)筛选穿心莲的潜在活性化学物质,借助GeneCards数据库、OMIM数据库平台筛选治疗癌症的作用靶点,利用Cytoscape 3.7.2软件构建“药物-活性化学物质-疾病-作用靶点”网络图,借助String数据库平台构建蛋白质相互作用(PPI)网络。最后应用Bioconductor平台和R语言进行基因本体论(GO)富集分析和京都基因与基因组百科全书(KEGG)通路分析。【结果】通过筛选得到穿心莲的潜在活性成分24个,涉及71个疾病作用靶点,其中与癌症相关作用靶点31个。主要活性成分为汉黄芩素、mono-O-methylwightin、quercetin tetramethyl(3’,4’,5,7)ether、千层纸素A等。主要通过调控AR、ERS1、IL-6等靶点基因及p53信号通路、甲状腺激素信号通路、催乳素信号通路等发挥抗肿瘤作用。主要抗癌病种为乳腺癌与前列腺癌。【结论】应用网络药理学的方法预测出穿心莲治疗癌症的可能作用机制,为其进一步研究提供新的思路与线索。     

圆锥石头花中两个具有α-葡萄糖苷酶抑制活性的新三萜皂苷(英文)

目的:研究圆锥石头花根中的化学成分。方法:用75%乙醇回流提取、乙酸乙酯和正丁醇依次萃取,采用硅胶、Sephadex LH-20、Rp-C18柱色谱法和制备液相色谱等方法分离纯化,根据光谱数据(一维、二维的核磁共振谱和质谱)及酸水解鉴定了化合物的结构并进行了-葡萄糖苷酶抑制活性测定。结果:从圆锥石头花根中分离得到2个新三萜多糖皂苷——圆锥石头花皂苷A(1)和B(2),两者均具有较强的α-葡萄糖苷酶抑制活性。结论:化合物1和2是首次从该植物中分离得到的新化合物,其结构中的对甲氧基-桂皮酰基可能为决定相关活性的关键基团。     

金钮扣不同提取物止咳化痰作用研究

目的:研究金钮扣不同提取物的止咳、化痰作用。方法:金钮扣用95%乙醇回流提取得到醇提取物,加水溶解后依次用石油醚、氯仿、乙酸乙酯、正丁醇萃取,浓缩得相应的萃取物和水相溶解部位。采用豚鼠枸橼酸引咳法、小鼠气管酚红法,观察金钮扣不同提取物的止咳、化痰作用。结果:金钮扣醇提取物组、乙酸乙酯组、正丁醇组和空白对照组的咳嗽潜伏期分别为133.5、138.4、137.1、87.8s,咳嗽次数分别为7、8、8和16次,酚红分泌量分别为1.031、1.014、1.262、0.656μg;醇提取物组、乙酸乙酯组和正丁醇组的咳嗽潜伏期延长、咳嗽次数减少、酚红分泌量增加,与空白对照组比较均具有显著性差异(P<0.01或P<0.05)。石油醚组、氯仿组和水溶部分组的咳嗽潜伏期、咳嗽次数及酚红分泌量,与空白对照组比较均无显著性差异。结论:金钮扣醇提取物止咳和化痰作用的有效成分主要集中在乙酸乙酯和正丁醇萃取部位。     

A biochemical study on the gastroprotective effect of hydroalcoholic extract of Andrographis paniculata in rats

Aim:

The aim of the present study is to evaluate the gastroprotective effect of hydroalcoholic extract of Andrographis paniculata (HAEAP) in male albino wistar rats.

Materials and Methods:

Rats were pretreated with HAEAP (100,200,500mg/kg b. wt for 30 days) and then gastric ulcers were induced by ethanol, aspirin, pylorus ligation and cold restraint stress models. Ulcer score was determined in all the ulcer models. pH, gastric volume, titrable acidity, pepsin, mucin, myeloperoxidase, H⁺K⁺ATPase, thiobarbituric acid reacting substances (TBARS) and antioxidant enzyme activities were assayed in ethanol-administered rats.

Results:

The ulcer score was found to be low in HAEAP-pretreated rats. Among the doses studied, 200 mg/kg b.wt was found to be optimum for significant ulcer reduction. The test drug significantly reduced the acidity, pepsin concentration, myeloperoxidase and H⁺K⁺ATPase activities in ethanol-administered rats. The elevated TBARS and decreased glutathione (GSH) and mucin levels observed during ulcerogenesis were found to be altered in HAEAP-received animals.

Conclusions:

The ulcer preventing effect of HAEAP may partly be due to its regulating effect on H⁺K⁺ATPase activity and /or mucin preserving effects. The flavonoids present in the HAEAP might be responsible for the gastroprotective action probably by maintaining the antioxidants and thiol status in the gastrointestinal tract.     

穿心莲药材指纹图谱提取方法研究

目的以建立指纹图谱为目标,研究不同提取方法对穿心莲药材化学成分提取效果的影响。方法采用不同提取方式、提取时间、提取溶剂及提取温度对穿心莲药材化学成分进行提取,并对提取物进行高效液相色谱法检测比较。结果以75%甲醇水溶液作为提取溶剂,80℃水浴回流2h的提取条件下获得的指纹图谱信息较为丰富,响应值较高。结论此方法简便、重现性好,可作为构建穿心莲药材HPLC指纹图谱的供试品溶液制备方法。     

A biochemical study on the gastroprotective effect of andrographolide in rats induced with gastric ulcer

The major objective of the study was to evaluate the gastroprotective property of andrographolide, a chief component of the leaves of Andrographis paniculata in terms of the ulcer preventive effect in rats. An acute toxicity test was conducted with different concentrations of andrographolide to determine the LD(50) value. The dose responsive study was conducted in rats pretreated with andrographolide (1, 3 and 5 mg/kg) for a period of 30 days, prior to ulcer induction by administering ethanol, aspirin or by pyloric ligation. The ulcer protective efficacy was tested by determining the ulcer score, pH, pepsin, titrable acidity, gastric mucin, lipid peroxides, reduced glutathione, and enzymatic antioxidants superoxide dismutase, catalase and glutathione peroxidase in gastric tissue. The activities of H(+)-K(+) ATPase and myeloperoxidase were also determined in gastric tissue. The LD(50) value was found to be 48 mg/kg b. wt and the effective dose was found to be 3 mg/kg. We have observed a significant reduction in the ulcer score in rats pretreated with 3 mg of andrographolide/kg body weight. A favourable increase in the pH and decrease in titrable acidity were observed in the gastric fluid of rats pretreated with the test drug. The gastric tissue H(+)-K(+) ATPase and myeloperoxidase activities were elevated in ulcer-induced animals. The elevation in the enzyme activity was significantly minimized in the andrographolide received animals. The antioxidants and mucin levels were significantly maintained in the gastric tissue of drug-pretreated animals. Andrographolide did not produce any toxic effects in normal rats. This study reveals that the ulcer preventive efficacy of andrographolide may probably due to its antioxidant, cytoprotective and antiacid secretory effects.