Vinblastine sulfate is a cytotoxic alkaloid [1]. Vinblastine sulfate inhibits the proliferation of cancer cells by inhibiting the polymerization of tubulin (nAChR: IC50 = 8.9μM) and interfering with the formation of the spindle during cell division [2-3]. Vinblastine sulfate is used to treat several types of cancer (Hodgkin's lymphoma, non-small cell lung cancer, bladder cancer, brain cancer, melanoma, and testicular cancer) [4].
In human acute promyelocytic leukaemia (NB4) cells, Vinblastine sulfate (50μM; 19h) reduced NB4 cell viability in a time- and concentration-dependent manner and concurrently promoted apoptosis and cell cycle arrest [5]. In Caco-2 cells, completion of culture medium with Vinblastine sulfate (10nM; 19d) increased the P-gp mRNA and the expression at protein level [6]. In Hela cells, Vinblastine sulfate (1, 10, 100, 1000, 10000µg/mL; 24h, 48h) treatment inhibits the proliferation of HeLa cells, and its inhibitory effect increases in a dose-dependent manner [7].
In fibrosarcoma mouse model, Vinblastine sulfate (0.25, 0.5, 1.0, 2.0mg/kg; ip; single injection) treatment reduces the incidence of DNA strand breaks in fibrosarcomas, blood leukocytes, and bone marrow cells in mice in a dose-dependent manner [8]. In Swiss mice, Vinblastine sulfate (0.5, 1.0, 1.5mg/kg; ip; single injection) is clastogenic in mouse bone marrow [9].
References:
[1]. McKay DB, Burkman AM. Nicotinic and nonnicotinic receptor-mediated actions of vinblastine. Proceedings of the Society for Experimental Biology and Medicine. 1993 Jul; 203(3): 372-376.
[2]. Pandya P, Agarwal LK, Gupta N, et al. Molecular recognition pattern of cytotoxic alkaloid vinblastine with multiple targets. Journal of Molecular Graphics and Modelling. 2014 Nov 1; 54: 1-9.
[3]. Sui M, Fan W. Combination of γ-radiation antagonizes the cytotoxic effects of vincristine and vinblastine on both mitotic arrest and apoptosis. International Journal of Radiation Oncology* Biology* Physics. 2005 Mar 15; 61(4): 1151-1158.
[4]. Du GH, Zhang YW, Kong XY, et al. Vinblastine and vincristine. Natural Small Molecule Drugs from Plants. 2018: 551-557.
[5]. Calviño E, Tejedor MC, Sancho P, et al. JNK and NFκB dependence of apoptosis induced by vinblastine in human acute promyelocytic leukaemia cells. Cell Biochemistry and Function. 2015 Jun; 33(4): 211-219.
[6]. Hellinger É, Bakk ML, Pócza P, et al. Drug penetration model of vinblastine-treated Caco-2 cultures. European journal of pharmaceutical sciences. 2010 Sep 11; 41(1): 96-106.
[7]. Yasin YS, Jumaa AH, Jabbar S, et al. Effect of laetrile vinblastine combination on the proliferation of the hela cancer cell line. Asian Pacific Journal of Cancer Prevention: APJCP. 2023; 24(12): 4329.
[8]. Rajagopalan R, Ranjan SK, Nair CK. Effect of vinblastine sulfate on γ-radiation-induced DNA single-strand breaks in murine tissues. Mutation Research/Genetic Toxicology and Environmental Mutagenesis. 2003 Apr 20; 536(1-2): 15-25.
[9]. Choudhury RC, Palo AK, Padhy A. Cytogenetic consequences of vinblastine treatment in mouse bone marrow. Chemotherapy. 2004 Oct 29; 50(4): 171-177.
Vinblastine sulfate是一种细胞毒性生物碱 [1]。Vinblastine sulfate通过抑制微管蛋白聚合（nAChR：IC50 = 8.9μM）并干扰细胞分裂过程中纺锤体的形成来抑制癌细胞增殖 [2-3]。Vinblastine sulfate用于治疗多种癌症（霍奇金淋巴瘤、非小细胞肺癌、膀胱癌、脑癌、黑色素瘤和睾丸癌） [4]。
在人急性早幼粒细胞白血病（NB4）细胞中，Vinblastine sulfate（50μM；19h）以时间和浓度依赖性方式降低NB4细胞活力，同时促进细胞凋亡和细胞周期停滞 [5]。在Caco-2细胞中，用Vinblastine sulfate（10nM；19d）完成培养基培养可增加P-gp mRNA和蛋白质水平的表达 [6]。在HeLa细胞中，Vinblastine sulfate（1、10、100、1000、10000µg/mL；24h、48h）处理可抑制HeLa细胞增殖，且其抑制作用呈剂量依赖性增强 [7]。
在小鼠纤维肉瘤模型中，Vinblastine sulfate（0.25、0.5、1.0、2.0mg/kg；ip；单次注射）处理可剂量依赖性地降低小鼠纤维肉瘤、血液白细胞和骨髓细胞中DNA链断裂的发生率 [8]。在瑞士小鼠中，Vinblastine sulfate（0.5、1.0、1.5mg/kg；ip；单次注射）在小鼠骨髓中具有致染色体断裂作用 [9]。