马鞭草科马马鞭草(Stachytarpheta jamaicensis (L) Vahl)叶中的三萜熊果酸(3 - β -3羟基-ur -12-烯-8-oic- Acid)的抗糖尿病和抗炎活性

Uchenna Estella Odoh, Payare L. Sangwan, Chinenye Cynthia Odo
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引用次数: 0

摘要

背景:熊果酸是广泛存在于药用植物中的一种五环萜类羧酸,据报道具有多种生物活性,如抗炎、抗癌、抗糖尿病和抗氧化活性。目的:研究马鞭草科马蹄草(Stachytarpheta jamiacensis (L) Vahl)叶二氯甲烷甲醇提取物熊果酸对四氧嘧啶诱导的糖尿病大鼠的抗糖尿病和抗炎作用。方法:采用冷浸法制备二氯甲烷:甲醇(1:1)提取物。从二氯甲烷甲醇萃取物中得到二氯甲烷馏分,用不同极性递增的溶剂进行柱层析和洗脱,分离出生物活性化合物。分离化合物的结构通过IR、1HNMR、13CNMR、MS等光谱技术进行了鉴定。按照标准程序对分离物进行植物化学分析和急性毒性研究。通过测定25和50 mg/kg剂量的高血糖大鼠的空腹血糖水平,观察其抗糖尿病潜力,为期14天。以10和20 mg/kg体重的鸡蛋白蛋白诱导大鼠足跖水肿小鼠为实验对象,研究了分离化合物的抗炎活性。结果:与糖尿病对照组相比,从甘蔗水青树二氯甲烷甲醇提取物中分离得到的熊果酸(3- β -3羟基-熊-12-烯-8-酸)在25和50 mg/kg剂量下可显著降低糖尿病动物的空腹血糖水平(72.79和79.77%)。标准药物(格列苯脲)降低77.77%。20 mg/kg熊果酸对卡拉胶诱导的小鼠耳部水肿的抑制作用最大(75.00%,p<0.05)。萜类化合物呈阳性。在高达5000 mg/kg剂量的急性毒性试验中没有死亡记录。 结论:从牙买加水芋二氯甲烷甲醇提取物中分离得到的熊果酸具有明显的抗糖尿病和抗炎活性。
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Antidiabetic and Antiinflammatory Activities of Ursolic Acid (3 - beta-3hyrdoxy-urs-12-ene -8-oic-acid), a Triterpenoid from Leaves of Stachytarpheta jamaicensis (L) Vahl (Verbennaceae)
Background: Ursolic acid, a pentacyclic terpenoid carboxylic acid widely found in medicinal plants has been reported to have multifarious biological activities such as antiinflammatory, anticancer, antidiabetic, and antioxidant activities. Aim: To evaluate the antidiabetic and antiinflammatory activities of Ursolic acid isolated from dichloromethane: methanol extract of leaves of Stachytarpheta jamiacensis (L) Vahl (Verbenaceae) in alloxan-induced diabetic rats. Methods: A dichloromethane: methanol (1:1) leaves extract was prepared by cold maceration. Dichloromethane fraction obtained from the dichloromethane: methanol extract was subjected to column chromatography and eluted with different solvents of increasing polarity to isolate the bioactive compounds. The structure of the isolated compound was elucidated using spectroscopic techniques (IR, 1HNMR, 13CNMR, MS). Phytochemical analysis of the isolate and acute toxicity study was done following standard procedures. The anti-diabetic potential was assessed by determining fasting blood glucose level on hyperglycemic rats at the dose of 25 and 50 mg/kg for a period of 14days. The isolated compounds’ antiinflammatory activity was investigated using egg albumin-induced rat paw edema in mice at dose of 10 and 20 mg/kg body weight. Results: Ursolic acid (3-beta-3hyrdoxy-urs-12-ene -8- oic-acid) isolated from dichloromethane: methanol extract of Stachytarpheta jamaicensis showed significant (p<0.05) reduction (72.79 and 79.77%) in fasting blood glucose levels at the dose of 25 and 50 mg/kg respectively in treated diabetic animals when compared with the diabetic control. A 77.77 % reduction was observed for standard drug (glibenclamide). Ursolic acid at 20 mg/kg exhibited a maximum inhibition (75.00%, p<0.05) of carrageenan-induced ear edema in mice. It showed positive for terpenoids. There was no death recorded in the acute toxicity test at doses of up to 5000 mg/kg. Conclusion: The results demonstrate that ursolic acid isolated from dichloromethane: methanol extract of Stachytarpheta jamaicensis (L) Vahl possesses significant anti-diabetic and anti-inflammatory activity.
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