Effective components of Semen Ziziphi Spinosae for sedative-hypnotic based on receptor ligand binding assay / 中国药理学通报

ABSTRACT

Aim To determine the effective compo-nents of Semen Ziziphi Spinosae for sedative-hypnotic and its mechanism. Methods The extraction of Se-men Ziziphi Spinosae and the rat brain homogenates were prepared. High concentrations of Diazepam com-petitively replaced the ligand compounds of Semen Ziz-iphi Spinosae combining BDZ receptor in brain tissue, and all the compounds with sedative and hypnotic effects were collected and identified by HPLC and LC-MS technique, as the compounds extracted from the brain tissue were administered with Semen Ziziphi Spi-nosae. The brain tissue was administered with Diaze-pam, and with Semen Ziziphi Spinosae and Diazepam. Results The HPLC chromatograms show that the peak time of BDZ receptor ligand compounds was 2. 71 min and 46. 87min, when compared with Diazepam. And the LC-MS chromatograms display the relative molecu-lar weight of the ligand compounds was 274. 28 m/z, 453. 34 m/z,496. 34 m/z and 608. 38 m/z respective-ly. According to the fingerprint of Semen Ziziphi Spi-nosae, these compounds may be fatty acid substances and lupine pill triterpene compounds. Conclusions On the basis of the principle of receptor ligand bind-ing, we established a way to quickly analyze and iden-tify the role of natural products in the same drug target compounds. The method not only can clearly define the effective components of natural products, but also clar-ify the mechanism of action of the compounds. The ac-tive ingredient of calm hypnosis in Semen Ziziphi Spi-nosae may be fatty acid substances Palmitic acid ( C16 H32 O2 ) and lupine pill triterpene compounds Alphitolic acid( C30 H48 O4 ) and Spinosin( C28 H32 O15 ) . They exert their sedative and hypnotic effects by combining with BDZ receptor, and the research has laid a theoretical foundation for the further study about mechanism of Se-men Ziziphi Spinosae.