Li S Y, Ling L H, Teh B S, Seow W K, Thong Y H
Department of Child Health, University of Queensland, Mater Children's Hospital, South Brisbane, Australia.
Int J Immunopharmacol. 1989;11(4):395-401. doi: 10.1016/0192-0561(89)90086-6.
Tetrandrine and berbamine are two naturally occurring analogues with a bis-benzylisoquinoline structure. Comparative in vitro studies show that tetrandrine has significantly greater suppressive effects on adherence, locomotion and 3H-deoxyglucose uptake of neutrophils, as well as the mitogen-induced lymphocyte responses and mixed lymphocyte reactions. Also, tetrandrine displayed anti-oxidant activity while berbamine did not. By contrast, berbamine demonstrated a significantly greater capacity for inhibition of NK cell cytotoxicity. These results show that tetrandrine is superior to berbamine in most aspects of anti-inflammatory and immunosuppressive activity. Since these two alkaloids differ by only one substitution in the side chain of one of the benzene rings, these findings may provide further insight into structure-activity relationships and clues to the synthesis and development of active analogues of this promising class of drugs for the treatment of chronic inflammatory diseases.
粉防己碱和小檗胺是两种具有双苄基异喹啉结构的天然类似物。体外比较研究表明，粉防己碱对中性粒细胞的黏附、运动及3H-脱氧葡萄糖摄取具有显著更强的抑制作用，对丝裂原诱导的淋巴细胞反应和混合淋巴细胞反应也有显著更强的抑制作用。此外，粉防己碱具有抗氧化活性，而小檗胺则没有。相比之下，小檗胺对NK细胞细胞毒性的抑制能力显著更强。这些结果表明，在抗炎和免疫抑制活性的大多数方面，粉防己碱优于小檗胺。由于这两种生物碱仅在其中一个苯环侧链上有一个取代基不同，这些发现可能为结构-活性关系提供进一步的见解，并为这类有前景的治疗慢性炎症性疾病的药物活性类似物的合成与开发提供线索。
