Banno Norihiro, Akihisa Toshihiro, Tokuda Harukuni, Yasukawa Ken, Higashihara Hiroshi, Ukiya Motohiko, Watanabe Kenji, Kimura Yumiko, Hasegawa Jun-Ichi, Nishino Hoyoku
Ichimaru Pharcos Company Ltd., Gifu, Japan.
Biosci Biotechnol Biochem. 2004 Jan;68(1):85-90. doi: 10.1271/bbb.68.85.
Nine triterpene acids, viz., six of the ursane type, ursolic acid (1), corosolic acid (2), 3-epicorosolic acid (3), pomolic acid (4), tormentic acid (5) and hyptadienic acid (6), and three of the oleanane type, oleanolic acid (7), augustic acid (8) and 3-epimaslinic acid (9), among which 1 constituted the most predominant triterpene acid, were isolated and identified from ethanol extracts of the leaves of red perilla [Perilla frutescens (L.) Britton var. acuta Kudo] and green perilla [P. frutescens (L.) Britton var. acuta Kudo forma viridis Makino]. These eight compounds, 1, 2, 4-9, were evaluated for their inhibitory effects on 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation (1 microg/ear) in mice. All the compounds tested showed a marked anti-inflammatory effect, with a 50% inhibitory dose (ID50) of 0.09-0.3 mg per ear. In addition, an evaluation against the Epstein-Barr virus early antigen (EBV-EA) activation induced by TPA showed five compounds, 1-3, 5 and 9, with a potent inhibitory effect on EBV-EA induction (91-93% inhibition at 1x10(3) mol ratio/TPA). Furthermore, compound 5 exhibited strong antitumor-promoting activity in an in vivo two-stage carcinogenesis test of mouse tumor by using 7,12-dimethylbenz(a)anthracene (DMBA) as an initiator and TPA as a promoter.
从紫苏叶[Perilla frutescens (L.) Britton var. acuta Kudo]和绿叶紫苏[P. frutescens (L.) Britton var. acuta Kudo forma viridis Makino]的乙醇提取物中分离并鉴定出9种三萜酸，即乌苏烷型的6种，熊果酸(1)、科罗索酸(2)、3-表科罗索酸(3)、坡模酸(4)、 tormentic酸(5)和次亚麻酸(6)，以及齐墩果烷型的3种，齐墩果酸(7)、奥古斯汀酸(8)和3-表马斯里酸(9)，其中1是最主要的三萜酸。对这8种化合物1、2、4 - 9进行了对12 - O -十四烷酰佛波醇-13-乙酸酯(TPA)诱导的小鼠炎症(1微克/耳)的抑制作用评估。所有测试化合物均显示出显著的抗炎作用，每耳50%抑制剂量(ID50)为0.09 - 0.3毫克。此外，对TPA诱导的爱泼斯坦-巴尔病毒早期抗原(EBV - EA)激活的评估显示，5种化合物1 - 3、5和9对EBV - EA诱导具有强效抑制作用(在1×10³摩尔比/TPA时抑制率为91 - 93%)。此外，在以7,12 -二甲基苯并(a)蒽(DMBA)为启动剂、TPA为促进剂的小鼠肿瘤体内两阶段致癌试验中，化合物5表现出很强的抗肿瘤促进活性。
