多籽钩叶藤中苯甲酰基酯型 clerodane 二萜衍生物的体内活性。

In vivo activity of benzoyl ester clerodane diterpenoid derivatives from Dodonaea polyandra.

机构信息

Sansom Institute for Health Research, University of South Australia, Frome Road, Adelaide, 5000, South Australia.

出版信息

J Nat Prod. 2011 Apr 25;74(4):650-7. doi: 10.1021/np100701s. Epub 2011 Mar 7.

Abstract

Four new benzoyl ester clerodane diterpenoids, 15,16-epoxy-8α-(benzoyloxy)methylcleroda-3,13(16),14-trien-18-oic acid (1), 15,16-epoxy-8α-(benzoyloxy)methyl-2α-hydroxycleroda-3,13(16),14-trien-18-oic acid (2), 15,16-epoxy-8α-(benzoyloxy)methyl-2-oxocleroda-3,13(16),14-trien-18-oic acid (3), and 15,16-epoxy-2α-benzoyloxycleroda-3,13(16),14-trien-18-oic acid (4), have been isolated from the leaves and stems of Dodonaea polyandra. The anti-inflammatory activities of compounds 1, 2, and 4 were evaluated by means of 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced mouse ear edema. Compounds 2 and 4 exhibited maximum inhibition of inflammation (70-76%) at doses of 0.22 and 0.9 μmol/ear, respectively. Modest activity (~45% inhibition) was maintained at nanomole/ear doses.

摘要

从 Dodonaea polyandra 的叶和茎中分离得到了四个新的苯甲酰酯 clerodane 二萜类化合物，分别为 15,16-环氧-8α-(苯甲酰氧基)甲基 cleroda-3,13(16),14-三烯-18-酸（1）、15,16-环氧-8α-(苯甲酰氧基)甲基-2α-羟基 cleroda-3,13(16),14-三烯-18-酸（2）、15,16-环氧-8α-(苯甲酰氧基)甲基-2-氧代 cleroda-3,13(16),14-三烯-18-酸（3）和 15,16-环氧-2α-苯甲酰氧基 cleroda-3,13(16),14-三烯-18-酸（4）。化合物 1、2 和 4 通过 12-O-十四烷酰佛波醇-13-醋酸酯（TPA）诱导的小鼠耳肿胀实验评估了抗炎活性。化合物 2 和 4 在 0.22 和 0.9 μmol/耳剂量下表现出最大的抗炎抑制作用（70-76%）。在纳摩尔/耳剂量下仍保持适度的活性（~45%抑制）。