Study On Quality Standard Of Castor Oil And The Synthesis And Activity Of Indeno [1,2-b] Pyridine Derivatives

This paper describes the synthesis and anticancer activity study of indeno[1,2-b]- pyridine derivatives in order to find potential antitumor drug candidates as well as the revision of the pharmacopoeial standard of castor oil based on the Chinese Pharmacopoeia (2005).To the revision of quality standard of castor oil, the harvest time of castor oil was not showed in C.P. 2005. So far, there is no report on the relation between the quality of castor oil and its harvest time. Castor oil is widely distributed all over the country and harvested in autumn. The quality standard is established from a comprehensive study of 6 samples of castor oil from three different factories that SFDA has approved .We recheck castor oil's relative density, refractive index, acid value, saponification value and iodine value according to appendix of C.P. 2005. It states that the date is suitable; It is the first time to set up a preliminary and best development system of TLC (thin layer chromatography) for castor oil. The results Indicate that: petroleun ether(60-90℃)-ethyl ether-formic acid(11:4.5:0.5)is the best mobile phase. The spot which sprays with iodine is clear, the color is obvious and Rf is suitable; The content of ricinoleic acid in castor oil is determined by GC. It contains not less than 48.0% of ricinoleic acid; Through the experiments, the quality standard of castor oil was established. Compared to C.P. 2005, TLC identification and content determination are added to make the standard more perfect. Besides, we primarily establish the GC and GC/MS fingerprint of castor oil from different factories, and the common model of fingerprint is built.To indeno[l,2-b]pyridine derivatives, a large number of compounds containing indone show good biological activity. Indeno[l,2-b]pyridine is an important structure. Its derivatives are used in medicine widely, such as anti-tumor, anti-inflammatory/anti- allergic, anti-cardiova-scular sclerosis, bactericidal and so on. In order to search for potential antitumor candidates, we design and synthesize indeno[l,2-b]pyridine derivatives in several steps starting from 1-indanone.It was reported by Hajime Katayama that the novel heterocyclic-ium triflate derivatives have strong cytotoxic activity against cancer cells. Based on the above study, the target compounds are synthesized by reacting Indeno[l,2-b]pyridine intermediates with methyl trifluoromethanesulfonate and 4-(dimethylamino)benzaldehyde. Their structures are confirmed by IR,NMR,MS. And their antitumor activities against cancer cell lines HEP-2 and K562 are tested by the MTT method in vitro. They exhibite potent antitumor activity.The paper has revised the quality standard of castor oil. It provides technical support for the revision of C. P. 2010 and makes the clinical use of castor oil safer and more effective. Indeno[l,2-b]pyridine derivatives have been synthesized and show good anticancer activity. The result provides the rationale for further research on antitumor drugs.