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。研究结果表明，从埃及、土耳其等地治疗哮喘的民间药材Nigella sativa种子中分离得到了新的一元苯二萜类生物碱，分别为Nigella胺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、褐藻或苔类植物中分离出了几种dollar - ellane型二萜。然而，从高等植物中分离到该类二萜的报道很少。此外，原产地中海地区的日本烹饪草本鼠粪叶对橄榄油负荷小鼠血清甘油三酯升高有显著抑制作用。利用对胰脂肪酶活性的抑制作用，通过生物测定指导分离，从活性组分中分离出更多的鼠尾草酸类化合物。鼠尾草酸（5 mg/kg/d, p.o）可降低高脂饮食小鼠2周后的体重增加和附睾脂肪重量积累。在埃及传统药物中用作泻药和抗糖尿病药的西葫芦（Citrullus colocynthis）的果实被发现对口服蔗糖负荷大鼠血清葡萄糖水平的升高有抑制作用，对小鼠耳被动皮肤过敏反应（PCA）有抗过敏作用。通过生物测定引导分离，发现主要的葫芦烷型三萜苷葫芦素e2 - o -β- d -葡萄糖吡喃苷具有抗过敏活性，并分离到新的葫芦烷型三萜苷番荔枝苷A和B。此外，从分布于撒哈拉-阿拉伯沙漠地区的阿纳塔卡（Anastatica hierochuntica）全株中分离出新的骨黄酮A和B，以及新的木脂素A- c。Anastatins A和B显示出较强的肝保护活性。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