源自丁香酚的苯并恶嗪和氨甲基化合物的抗癌活性。
anticancer activity of benzoxazine and aminomethyl compounds derived from eugenol.
作者信息
Rudyanto Marcellino, Ekowati Juni, Widiandani Tri, Syahrani Achmad
机构信息
Department of Pharmaceutical Sciences, Faculty of Pharmacy, Universitas Airlangga, Surabaya, Indonesia.
Institute of Tropical Disease, Universitas Airlangga, Surabaya, Indonesia.
出版信息
J Public Health Afr. 2023 Mar 16;14(Suppl 1):2511. doi: 10.4081/jphia.2023.2511. eCollection 2023 Mar 30.
BACKGROUND
Indonesia is the world's primary producer of clove. In order to find new utilization for clove and new biologically active compounds, eugenol, the main constituent of clove, has been converted to its derivatives.
OBJECTIVE
This study aims to examine anticancer activity of benzoxazine and aminomethyl compounds derived from eugenol.
METHODS
Fibrosarcoma was induced by injection of benzo(a)pyrene solution. The test compounds were given per oral at 20, 40, and 80 mg/Kg body weight, once a day for 30 days.
RESULTS
As a result, all the tested compounds showed activity in reducing the cancer incidence rate. All the tested compounds were also found to reduce tumor weight. Benzoxazine derivatives gave slightly better activity compared to aminomethyl derivatives. The strongest activity was exhibited by 6-allyl-3-(furan-2- ylmethyl)-8-methoxy-3,4-dihydro-2H-benzo(e)(1,3)oxazine.
CONCLUSIONS
All four benzoxazine and aminomethyl compounds derived from eugenol that were tested exhibited anticancer activity in mice fibrosarcoma.
背景
印度尼西亚是世界主要的丁香生产国。为了寻找丁香的新用途和新的生物活性化合物，丁香的主要成分丁香酚已被转化为其衍生物。
目的
本研究旨在检测丁香酚衍生的苯并恶嗪和氨甲基化合物的抗癌活性。
方法
通过注射苯并(a)芘溶液诱导纤维肉瘤。受试化合物按20、40和80毫克/千克体重口服给药，每天一次，共30天。
结果
结果显示，所有受试化合物均具有降低癌症发病率的活性。还发现所有受试化合物均能减轻肿瘤重量。与氨甲基衍生物相比，苯并恶嗪衍生物的活性略好。6-烯丙基-3-(呋喃-2-基甲基)-8-甲氧基-3,4-二氢-2H-苯并(e)(1,3)恶嗪表现出最强的活性。
结论
所测试的四种源自丁香酚的苯并恶嗪和氨甲基化合物在小鼠纤维肉瘤中均表现出抗癌活性。
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