Department of Pharmacology, Faculty of Medicine, Tehran University of Medical Sciences, Tehran, Iran.
Phytother Res. 2012 Jul;26(7):1023-8. doi: 10.1002/ptr.3678. Epub 2011 Dec 20.
Dracocephalum kotschyi Boiss. has been used as part of an ethnobotanical remedy against many forms of human cancer in Iran. It has been demonstrated that a flavonoid named xanthomicrol from D. kotschyi contributes to its preferential antiproliferative activity against malignant cells. In the present study, the antiproliferative activity of its flavonoid fraction was further characterized. Using liquid-liquid extraction and a semi-preparative reversed-phase HPLC method, eight flavonoid aglycones were isolated from the aerial parts of the plant and their identities were confirmed through MS and NMR analyses as luteolin, naringenin, apigenin, isokaempferide, cirsimaritin, penduletin, xanthomicrol and calycopterin. The in vitro antiproliferative activity of each compound was evaluated against a panel of established normal and malignant cell lines using the MTT assay and some structure-activity relationships were observed. The hydroxyflavones (luteolin, apigenin and isokaempferide) exerted comparable antiproliferative activities against malignant and normal cells, while the methoxylated hydroxyflavones (cirsimaritin, penduletin, xanthomicrol and calycopterin) showed preferential activities against tumor cells. This activity may be of value in treating tumors as it would exert few side effects in normal tissues. Xanthomicrol selectively inhibited the growth of human gastric adenocarcinoma, while calycopterin selectively prevented human acute promyelocytic leukemia and human colon carcinoma cells proliferation.
藏夏枯草（Dracocephalum kotschyi Boiss.）已被伊朗人用作治疗多种人类癌症的民间药物。已证实，藏夏枯草中的一种名为黄木樨草素的类黄酮化合物对恶性细胞具有优先的抗增殖活性。在本研究中，进一步研究了其类黄酮部分的抗增殖活性。通过液液萃取和半制备反相 HPLC 方法，从该植物的地上部分分离出八种类黄酮苷元，并通过 MS 和 NMR 分析确定其为木樨草素、柚皮素、芹菜素、异凯因、圣草酚、 Pendulatin、黄木樨草素和金莲花素。通过 MTT 测定法评估了每种化合物对一系列已建立的正常和恶性细胞系的体外增殖活性，并观察到一些结构-活性关系。羟基黄酮（木樨草素、芹菜素和异凯因）对恶性和正常细胞均具有相当的抗增殖活性，而甲氧基化羟基黄酮（圣草酚、 Pendulatin、黄木樨草素和金莲花素）对肿瘤细胞表现出优先的活性。这种活性在治疗肿瘤方面可能具有价值，因为它在正常组织中几乎没有副作用。黄木樨草素选择性地抑制人胃腺癌的生长，而金莲花素选择性地阻止人急性早幼粒细胞白血病和人结肠癌细胞的增殖。
