Pal R, Rizvi S Y, Kundu B, Mathur K B, Katiyar J C
Division of Parasitology, Central Drug Research Institute, Lucknow, India.
Experientia. 1991 May 15;47(5):486-90. doi: 10.1007/BF01959951.
Several glycopeptides structurally related to muramyl dipeptide (MDP) have been synthesized and evaluated for their ability to stimulate the non-specific resistance of hamsters against L. donovani infection. These compounds have been named CDRI compounds. The synthetic procedure used for compounds 86/448 and 84/212 is described. MDP and its synthetic congeners were administered as immunostimulants at a prophylactic dose of 3 mg/kg at two weeks interval. The challenge infection (1 x 10(7) amastigotes i.c./hamster) was given in between two doses of the compounds. One of the glycopeptides, CDRI comp. 86/448, has been found to be significantly more potent than MDP, effecting 92% inhibition of the challenge dose, whereas MDP produced only 26.5% inhibition. The effect of comp. 86/448 lasted until day 7 of challenge. The efficacy of sodium stibogluconate was appreciably improved in hamsters treated with comp. 86/448.
已合成了几种与胞壁酰二肽(MDP)结构相关的糖肽,并评估了它们刺激仓鼠对杜氏利什曼原虫感染的非特异性抵抗力的能力。这些化合物被命名为CDRI化合物。描述了用于化合物86/448和84/212的合成过程。MDP及其合成同系物作为免疫刺激剂,以3mg/kg的预防剂量每隔两周给药一次。在两次化合物给药之间进行激发感染(每只仓鼠脑内接种1×10⁷无鞭毛体)。已发现其中一种糖肽CDRI化合物86/448比MDP的效力显著更高,对激发剂量的抑制率达92%,而MDP仅产生26.5%的抑制率。化合物86/448的作用持续到激发后的第7天。在用化合物86/448治疗的仓鼠中,葡萄糖酸锑钠的疗效明显提高。