The Millettia Yunnan's Chemical Composition And Compound Millettia Preparation Preparation Technology And Quality Standards

Fufang Jixueteng Gao, a traditional Chinese patent medicine, is made up of the powder of Dian Jixueteng Gao, Radix Cyathulae, Radix Dipsaci, Flos Carthami and Semen Glycine. It's mainly used for the treatment of blood deficiency, numb hands and feet, painful aching of the joints and irregular menstruation. As the foundational research of Fufang Jixueteng Gao is very limited, there was no characteristic method to estimate and control its quality effectively. In order to establish the quality standards of Fufang Jixueteng preparations, the chemical constituents of Caulis Kadsurae was investigated first of all. The procedure of the traditional preparation was also improved.Dian Jixueteng Gao is the water extract of Caulis Kadsurae, the stems Kadsura interior A. C. Smith and K. heteroclita (Roxb.) Craib. Previous studies indicated that the dibenzocyclooctene-type lignans were principal bioactive constituents of K. interior and K. heteroclita, which showed various biological activities, such as anti-lipid peroxidation, antitumor-promoting effect and calcium antagonism. No chemical study of Caulis Kadsurae has been reported yet. Our current investigation on the chemical constituents of the EtOAc soluble extract of Caulis Kadsurae led to the isolation and identification of 17 lignans, kadsutherins A~C, diankadsutherin, diankadsurinone, kadsurin, interiotherin C, heteroclitin C, schisanlignone A, binankadsurin A, gomisin U, heterocltin D, interiorin, schiarisanrin C, heteroclitein G, meso-dihydroguaiaretic acid, together with ganwuweizic acid, mawuweizic acid and P-sitosterol. Kadsutherins A~C and diankadsutherin were new compounds. Kadsutherin C is the first dibenzocyclooctene lignan without oxygen-containing substitute at C (2). Diankadsurinone was a new natural compound. Heteroclitin D was isolated from Caulis Kadsurae with a high yield, which showed significant anti-lipid peroxidative effect and inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) activation and on platelets aggregation induced by ADP and PAR Heteroclitin D can be used as the chemical marker for quality control of Fufang Jixueteng preparations.The procedure of Fufang Jixueteng Gao was improved on the basis of the contents of bioactive lignans and the main activities of the preparations. Caulis Kadsurae was extracted with water and ethanol, respectively. The content of total lignans in the ethanolic extract was much higher than that of the water extract, as well as the activity to promote tiny blood circulation of mesentery. It suggested that the bioactive lignans couldn't be extracted completely by water. It's more reasonable to extract Caulis Kadsurae with ethanol to prepare Fufang Jixueteng Gao. The procedure was optimized by orthogonal designs. 54.69g of the ethanolic extracted Fufang Jixueteng Gao was equivalent to 218.75g of the water extract on the activity. Fufang Jixueteng Gao was transformed to capsules and granules. The two new preparations were more convenient for taking than the original Fufang Jixueteng Gao.HPLC-DAD was used for quantitative determination of eight lignans, heteroclitin G, gomisin A, interiorin, interiorin B, heteroclitin D, kadsurin, deoxyschisandrin and schisandrin C, in Caulis Kadsurae and its preparations. The method was stable and feasible. All of the eight lignans could be determined exactly in the ethanolic extract of Caulis Kadsurae, Fufang Jixueteng capsules and its intermediate products. Seven of the lignans could be determined exactly in Caulis Kadsurae and Fufang Jixueteng granules. The content of heteroclitin D was higer than that of any other lignans in Fufang Jixueteng capsules and granules. And there was no significant difference among three batchs of capsules or granules on the content of Heterocltin D. Thus, heteroclitin D was taken as the chemical marker of the Fufang Jixueteng preparations. Additionally, TLC methods were established to identify Caulis Kadsurae, Radix Cyathulae and Radix Dipsaci in Fufang Jixueteng preparations.Based on the above conclusions, the quality standards of Fufang Jixueteng capsules and granules were established. The quality of the traditional Fufang Jixueteng preparations can be controlled effectively by the above characteristic TLC identification and quantitative determination.