Hayashi T, Asano S, Mizutani M, Takeguchi N, Kojima T, Okamura K, Morita N
Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University, Japan.
J Nat Prod. 1991 May-Jun;54(3):802-9. doi: 10.1021/np50075a008.
A new tetracyclic diterpenoid, scopadulciol [3], together with 6-methoxybenzoxazolinone, glutinol, and acacetin, was isolated from the 70% EtOH extract of Scoparia dulcis collected in Taiwan. Its structure was elucidated to be 6 beta-benzoyl-12-methyl-13-oxo-9(12)a,9(12)b-dihomo-18-podocarpanol on the basis of spectral data. It mildly inhibited hog gastric H+, K(+)-ATPase. Examination of the inhibitory activities of derivatives of scopadulcic acid B [2], including 3, revealed that methylation of the carboxyl group and introduction of an acetyl group or oxime at C-13 or C-18 markedly enhanced the inhibitory activity, while debenzoylation reduced the activity. Among the 30 compounds tested, compound 12, a methyl ester of scopadulcic acid B [2], showed the most potent activity.
从采自台湾的甜地丁70%乙醇提取物中分离得到一种新的四环二萜类化合物——甜地丁醇[3]，以及6-甲氧基苯并恶唑啉酮、谷甾醇和刺槐素。根据光谱数据确定其结构为6β-苯甲酰基-12-甲基-13-氧代-9(12)a,9(12)b-二高-18-罗汉松醇。它对猪胃H⁺,K⁺-ATP酶有轻度抑制作用。对甜地丁酸B[2]的衍生物（包括化合物3）的抑制活性进行研究发现，羧基甲基化以及在C-13或C-18位引入乙酰基或肟基可显著增强抑制活性，而去苯甲酰化则会降低活性。在所测试的30种化合物中，甜地丁酸B[2]的甲酯化合物12表现出最强的活性。
