SEARCH FOR ANTI-METASTATIC AND DIFFERENTIATION-INDUCING ACTIVE COMPOUNDS FROM MEDICINAL PLANTS AND FOODS

在本研究中，我们研究了具有抗侵袭、基质金属蛋白酶（MMPs）产生抑制、分化诱导活性的药用植物的活性成分，这些药用植物已用于抗癌和长寿。1.传统泰国药物的MeOH提取物和EtOAc可溶性部分，丁茎（旋花科）在体外能抑制HT 1080细胞通过Matrigel膜的侵袭和人成纤维细胞的增殖（HT 1080）和人白血病细胞（U937）细胞。通过生物活性导向分离，从乙酸乙酯萃取物中分离出4种主要的类鱼藤素[鱼藤素（1）、茶黄素（2）、鱼藤酮（3）、12 α-羟基鱼藤酮（4）]以及各种异黄酮和紫檀烷。其中1-4在3-30 μM浓度下孵育24 h后对HT 1080细胞的侵袭有抑制作用，孵育48 h后对HT 1080和人白血病U937细胞的增殖也有抑制作用。关于其作用机制，1-4（1-10 μM） ...更多信息 使用明胶酶谱法抑制培养基中proMMP-9的释放。NBT还原实验表明，化合物1和2（10 μM）对HL-60细胞有诱导分化作用。2.在体外抗肿瘤实验中，研究了短茎芦醇提物及其生物碱组分对U937、小鼠黑色素瘤细胞（B16 F10）和HT 1080的细胞毒作用。具有6-羟基的二聚倍半萜硫代生物碱（6-hydroxythiobinupharidine，6，6 '-dihydroxythiobinupharidine，6-hydroxythionuphlutine B）在10 μM浓度下显示出显著的细胞毒活性，并阐明了活性的几个结构要求。6-羟基硫代比努法利定处理U937细胞后1 h内即可观察到细胞凋亡，并通过caspase-8途径参与细胞凋亡。3.从黑种草子中分离得到一种新的二萜生物碱--黑种草胺，并对其化学结构进行了鉴定。发现1'S-1 '-Acetoxychavicol acetate和各种相关化合物抑制NF-κB的活化，表明具有抗肿瘤活性。少

In the present study, we investigated the active constituents with anti-invasive, matrix metalloproteases (MMPs) production inhibitory, differentiation-inducing activities from medicinal plants that have been used for anti-cancer and longevity.1.The MeOH extract and EtOAc-soluble fraction traditional Thai medicine, the stems of Erycibe expansa (Convolvulaceae) were found to inhibit invasion of HT1080 cells through Matrigel-coated filters in vitro and proliferation of human fibroblast (HT1080) and human leukemia cell (U937) cells. Through bioassay-guided separation, four principal rotenoids [deguelin (1), tephrosin (2), rotenone (3), 12a-hydroxyrotenone (4)] together with various isoflavones and pterocarpanes were isolated from the EtOAc fraction. Among them, 1-4 inhibited the invasion of HT1080 cells at 3-30 μM after 24 h incubation, and they also inhibited proliferation of HT1080 and human leukemia U937 cells after 48 h incubation. With regard to their action mechanism, 1-4 (1-10 μM) … More inhibited release of proMMP-9 in the medium using a gelatin zymography. Furthermore, compounds 1 and 2 (10 μM) induced the differentiation of HL-60 cells using NBT reduction test.2.The methanolic extract and its alkaloid fraction from the rhizomes of Nuphar pumilum were found show cytotoxic effects on U937, mouse melanoma cell (B16F10), and HT1080 in the experiments of their anti-invasion. Dimeric sesquiterpene thioalkaloids with the 6-hydroxyl group (6-hydroxythiobinupharidine, 6,6'-dihydroxythiobinupharidine, 6-hydroxythionuphlutine B) showed substantial cytotoxic activity at a concentration of 10 μM, and several structural requiremwnts for the activity were clarified. Apoptosis of U937 was immediately observed within 1 h after treatment of 6-hydroxythiobinupharidine and pathway via caspase-8 was found to be involved.3.Furthermore, new diterpene alkaloids, nigellamines were isolated from the seeds of Nigella sativa that have been used for cancer treatment and their chemical structures were determined. 1'S-1'-Acetoxychavicol acetate and various related compounds were found to inhibit activation of NF-κB, suggesting antitumor activity. Less