title: Pharmacological evaluation of total alkaloids from nux vomica: effect of reducing strychnine contents.
abstract: The aim of the study was to investigate the possibility of improving the therapeutic efficacy of the total alkaloid fraction (TAF) extracted from processed nux vomica by reducing the strychnine contents. Most strychnine was removed from TAF to obtain the modified total alkaloid fraction (MTAF). The toxicity and pharmacokinetics of TAF and MTAF were further investigated and compared besides their antitumor, analgesic and anti-inflammatory activities. The results showed that the ratios of brucine to strychnine were 1:2.05 and 2.2:1 for TAF and MTAF, respectively, and the toxicity of TAF was about 3.17-fold higher than that of MTAF. Compared to brucine alone, the elimination of brucine was found to be inhibited by other alkaloids in TAF or MTAF except strychnine. Significantly increased pharmacological activities when administered by the oral route were obtained with MTAF in comparison to TAF and nux vomica powder (NVP). In summary, MTAF might replace NVP and TAF in the clinical application of Chinese medicine to obtain much higher efficacy.
authors.affiliation: Engineering Center of State Ministry of Education for Standardization of Chinese Medicine Processing, Nanjing University of Chinese Medicine, Nanjing 210023, China.
authors.forename: Jun
authors.initials: J
authors.lastname: Chen
authors.affiliation: Engineering Center of State Ministry of Education for Standardization of Chinese Medicine Processing, Nanjing University of Chinese Medicine, Nanjing 210023, China.
authors.forename: Yange
authors.initials: Y
authors.lastname: Qu
authors.affiliation: Engineering Center of State Ministry of Education for Standardization of Chinese Medicine Processing, Nanjing University of Chinese Medicine, Nanjing 210023, China.
authors.forename: Dongyue
authors.initials: D
authors.lastname: Wang
authors.affiliation: Engineering Center of State Ministry of Education for Standardization of Chinese Medicine Processing, Nanjing University of Chinese Medicine, Nanjing 210023, China.
authors.forename: Pei
authors.initials: P
authors.lastname: Peng
authors.affiliation: Engineering Center of State Ministry of Education for Standardization of Chinese Medicine Processing, Nanjing University of Chinese Medicine, Nanjing 210023, China.
authors.forename: Hao
authors.initials: H
authors.lastname: Cai
authors.affiliation: Engineering Center of State Ministry of Education for Standardization of Chinese Medicine Processing, Nanjing University of Chinese Medicine, Nanjing 210023, China.
authors.forename: Ying
authors.initials: Y
authors.lastname: Gao
authors.affiliation: Engineering Center of State Ministry of Education for Standardization of Chinese Medicine Processing, Nanjing University of Chinese Medicine, Nanjing 210023, China.
authors.forename: Zhipeng
authors.initials: Z
authors.lastname: Chen
authors.affiliation: Engineering Center of State Ministry of Education for Standardization of Chinese Medicine Processing, Nanjing University of Chinese Medicine, Nanjing 210023, China. bccai@126.com.
authors.forename: Baochang
authors.initials: B
authors.lastname: Cai
mesh_terms: D000700:Analgesics / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D019540:Area Under Curve; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D006207:Half-Life; D006801:Humans; D007928:Lethal Dose 50; D051379:Mice; D010936:Plant Extracts / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D012639:Seeds / Q000737:chemistry; D013331:Strychnine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D031461:Strychnos nux-vomica / Q000737:chemistry*
chemical_list: D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D000972:Antineoplastic Agents, Phytogenic; D010936:Plant Extracts; C083806:brucine; D013331:Strychnine
references.citation: J Forensic Sci. 1985 Oct;30(4):1248-55
references.pmid: 4067548
references.citation: Behav Brain Res. 2007 Mar 12;178(1):70-81
references.pmid: 17207866
references.citation: J Pharm Biomed Anal. 2009 Feb 20;49(2):487-91
references.pmid: 19062219
references.citation: Isr Med Assoc J. 2008 Feb;10(2):142-5
references.pmid: 18432030
references.citation: J Ethnopharmacol. 2003 Oct;88(2-3):205-14
references.pmid: 12963144
references.citation: Zhongguo Zhong Yao Za Zhi. 2012 Jul;37(14):2160-3
references.pmid: 23126206
references.citation: J Mater Sci Mater Med. 2009 Oct;20(10):2075-84
references.pmid: 19459034
references.citation: J Ethnopharmacol. 2012 Jan 6;139(1):181-8
references.pmid: 22094056
references.citation: J Control Release. 2012 Sep 28;162(3):628-35
references.pmid: 22967750
references.citation: J Ethnopharmacol. 2004 Jul;93(1):109-12
references.pmid: 15182914
references.citation: J Toxicol Environ Health. 1977 Dec;3(5-6):797-809
references.pmid: 599579
references.citation: Lloydia. 1976 Sep-Oct;39(5):263-325
references.pmid: 14294
references.citation: Acta Pharmacol Sin. 2007 Nov;28(11):1851-8
references.pmid: 17959038
references.citation: J Ethnopharmacol. 1992 Jan;35(3):295-7
references.pmid: 1347799
references.citation: Zhongguo Yao Li Xue Bao. 1998 Sep;19(5):425-8
references.pmid: 10375801
references.citation: J Ethnopharmacol. 2006 Jun 30;106(2):179-86
references.pmid: 16442763
references.citation: Neurotoxicol Teratol. 2005 Nov-Dec;27(6):855-9
references.pmid: 16171972
references.citation: Fitoterapia. 2011 Dec;82(8):1302-8
references.pmid: 21958965