Studies On The Chemical Constituents Inthe Chloroformfraction Of Sarcococcaruscifoliastapf Study On The Synthesis And Molluscicidal Activity Of6-sub Salicylic Acid With Different Chain Length

Sarcococca ruscifolia Stapf, as a member of the genus Sarcococca of the Buxaceae family, is often found in forest ditches on mountains at the altitudes of1200to2600meters in various regions of Yunnan Province, including Kunming, Dali, Zhongdian, Wenshan, Honghe, Dayao, and Wuding. In China, it is widely used by the folks for the treatments of stomach pain, bruises, traumatic, dizziness, palpitation, sore throat and so on. Modern pharmacology and phytochemistry researches have elucidated that S. ruscifolia can promote gastrointestinal peristalsis and anti-ulcer. Alkaloids, the main compounds isolated from this plant, show good cholinesterase inhibitory activity and cytotoxicity activity. Based on the experiments of anti-tumor activity screening, we found that the ethanol extract of S. ruscifolia has the inhibitory activity of lung and skin cancers. Therefore, for the purpose of searching for effective anti-cancer monomers, this research made further separation and purification to the alkaloids-rich chloroform franction. Seven compounds were isolated and six of them were elucidated as Sarcorucinine E [(20S)-20-(N-Methylamino)-3-[(3-methylbut-2-enoyl), amino]-5α-pregnane-2-ene-4-one](SRI), Sarcorucinine F [(20S)-20-(N-Methylamino)-3-[(3-methylbut-2-enoyl)amino]-5a-pregnane-2,16-diene-4-one](SR2), Sarcorucinine G [(20S)-20-(N,N-Dimethylamino)-3β-(benzamido)-5α-pregnane-16-ene](SR3), Epipachysamine D (SR4), Pachysamine M (SR5), and Sarcovagine D (SR6) on the basis of physico-chemical properties and spectroscopic analyses. Among them, SRI, SR2and SR3were totally new compounds and SR5was separated from this plant for the first time.Ginkgolic acids (GAs) are a group of6-alkylsalicylic acids, extracted from the sarcotesta and leaves of Ginkgo biloba L, and show good molluscicidal activities. The side chain lengths of GAs are more than13. In order to understand the structure-activity relationship for GAs analogues and their molluscicidal activity, in this study14Z/E isomers of GA analogues(GA-8a. GA-9a to GA-8g, GA-9g) with different chain lengths (5-13carbon atoms) and phenyl rings based on one added inside double bond have been synthesized. All of them are new compounds. The structures were elucidated by spectroscopic analyses. Their molluscicidal effects against the host snail Oncomelania hupensis were evaluated. The results revealed that the E-isomers were better molluscicidal agents than their respective Z-isomers. Activity was found to decrease regularly with the shortening of the alkyl chain lengths.