SEARCH FOR NEW ANTIDIABETOGENIC AND ANTI-OBESE SEED COMPOUNDS FROM THE TRADITIONAL EGYPTIAN MEDICINES

我们通过生物测定筛选，从埃及传统药物中寻找抗糖尿病和抗肥胖的种子化合物。结果从民间治疗哮喘、埃及和土耳其食用的黑种草种子中分离得到新的多拉贝烷型二萜生物碱：黑种草碱A_1-A_5、B_1-B_3、C和D。这些成分被发现具有促进脂质代谢的活性。以前，从海洋软珊瑚、褐藻或地钱中分离出几种多拉贝烷型二萜。然而，从高等植物中分离到这种类型的二萜类化合物的报道非常罕见。此外，产于地中海地区、在日本被称为食用药的丹参叶对橄榄油负载小鼠的血清甘油三酯升高具有显著的抑制作用。通过生物测定指导分离使用对胰腺脂肪酶活性的抑制活性，abietan型双…从活性部位中分离到更多的内酯类化合物(鼠尾草酸)。鼠尾草酸(5 mg/kg/d，P.O.)降低高脂饲料喂养2周后小鼠的体重增长和附睾脂的蓄积。埃及传统药物中用作通便和抗糖尿病药物的西瓜果实对口服蔗糖负荷的大鼠血糖水平的升高具有抑制作用，对小鼠耳部被动皮肤过敏反应(PCA)具有抗过敏作用。通过生物测定分离，发现主要的葫芦烷型三萜糖苷-葫芦素E2-O-β-D-吡喃葡萄糖苷具有抗过敏活性，并分离出新的葫芦烷型三萜苷类化合物coocinthoside A和B。此外，从分布于撒哈拉-阿拉伯沙漠中的新骨架黄烷酮类化合物anastatins A和B以及新木脂素A-C中分离得到新的木脂素A-C。Anastatins A和B具有较强的保肝活性。较少

We have searched antidiabetogenic and anti-obese seed compounds from traditional Egyptian medicines through bioassay screening. As the results, new dolabellane-type diterpene alkaloids, nigellamines A_1-A_5, B_1-B_3, C and D, were isolated from seeds of Nigella sativa, which is prescribed in folk medicines for treatment of asthma and used as a food in Egypt and Turkey. These constituents were found to show lipid metabolism promoting activity. Previously, several dolabellane-type diterpenes were isolated from the marine soft coral, brown algae, or liverwort. However, the isolation reports of this type of diterpenes from higher plants were very rare.In addition, the leaves of Salvia officinalis, which is originated from Mediterranean area and known as a culinary herb in Japan, showed significant inhibitory effect on serum triglyceride elevation in olive oil-loaded mice. Through bioassay-guided separation using the inhibitory activity against pancreatic lipase activity, abietan-type diter … More penes (carnosic acid) were isolated from the active fraction. Carnosic acid (5 mg/kg/d, p.o.) reduced the gain of body weight and the accumulation of epididymal fat weight in high fat diet-fed mice after 2 weeks.The fruit of Citrullus colocynthis, which is used as an catharsis and anti-diabetic agents in traditional Egyptian medicines, was found to show inhibitory effects on increase in serum glucose levels in oral sucrose-loaded rats and an antiallergic effect on ear passive cutaneous anaphylaxis (PCA) reaction in mice. Through bioassay-guided separation, the principal cucurbitane-type triterpene glycoside, cucurbitacin E 2-O-β-D-glucopyranoside, was found to exhibit antiallergic activity and new cucurbitane-type triterpene glycosides, colocinthosides A and B, were isolated.Furthermore, new skeletal flavanones, anastatins A and B and new lignans, hierochin A-C, were isolated from the whole plants of Anastatica hierochuntica, which is distributed in the Sahara-Arabian deserts and used by women as a charm for child birth. Anastatins A and B showed potent hepatoprotective activity. Less