Study On The Chemical Constituents Of Vaccariae Semen And The Influence Of Processing

Vaccariae Semen, recorded in the first rank of Shennong Bencao Jing, is the dry mature seed of Vaccaria segetalis (Neck.) Garcke, family Caryophyllaceae. It is able to invigorate the circulation of blood, promote the menstrual flow and the flow of milk, and cause the subsidence of swelling, for agalactia, amenorrhea, dysmenorrhea, mastitis with swelling and pain of the breas in human medicine.Processing plays an important role in the improvement of medicine effect. In history, vaccariae semen has a variety of processing approaches, such as firing to charcoal, steaming, steaming with alcohol, and frying, etc. Nowadays, in terms of Chinese Pharmacopoeia, vaccariae semen can be used in crude or in fried, but usually in fried in clinic. Generally, after fried, the active constituents of vaccariae semen with loose texture will be extracted more easily, and then will have an improved effect. Chemical constituent is the material basis of medicine effect. The change of medicine effect after processing must result from the change of the material basis, namely the change of the chemical constituent. However, there is absent research on the influence of processing on the material basis of vaccariae semen. To explore the processing mechanism of vaccariae semen, this paper will firstly research on the chemical constituents of vaccariae semen, and then explore the influence of processing on the content and dissolution rate of those chemical constituents.This paper includes these sections:The first section has a review on the research advancement of the chemical constituents, pharmacological effects and processing of vaccariae semen. Its chemical constituents includes triterpenoid saponins, cyclic peptides, flavonoids and others; the pharmacological effects includes galactopoietic activity, antitumor activity, effect on the blood and vessel, antioxidant activity, ameliorative effect on osteopenia and others; the processing part includes its history and its mechanism.The second section researches the chemical constituents of vaccariae semen with the help of lots of modern chromatographic separation technology, such as macroporous adsorptive resins, silica gel and LH-20. The result gives 18 compounds, two of which are novel ones and four of which are isolated from vaccariae semen for the first time. These 18 compounds are listed as followed:apigenin 6-C-[α-L-arabinopyranosyl-(1’"→2")-β-D-glucopyranosyl]-7-O-β-D-glucopyranoside (1), apigenin 6-C-[α-L-arabinopyranosyl-(1"’→2")-β-D-glucopyranosyl]-7-O-(6""-O-dihydroferuloyl)-β-D-glucopyranoside (2), apigenin 6-C-β-D-glucopyranosyl-7-O-(6""-O-dihydroferuloyl)-β-D-glucopyranoside (3), isovitexin-2"-Oarabinoside (4), saponarin (5), vitexin (6), segetalin A (7), segetalin B (8), segetalin C (9), segetalin D (10), segetalin E (11), Stigmast-7,22-dien-3-ol-3β-0-(β-D-glucopyranoside) (12), segetoside A (13), allantoin (14), hypaphorine (15), adenosine (16), guanosine (17), sucrose (18). Their chemical structures see Figure I. Rotational isomers appear in compound 1～5.Besides, it is found that the chemical structure of vaccarin was identified incorrectly before and should be corrected the same as compound 1.The third section explores the influence of processing on the content and dissolution rate of the main chemical constituents. Segetalins A、B、E, hypaphorine, vaccarin, saponarin, isovitexin-2"-O-arabinoside and vaccarin H were chosen as agents.After processing, few changes appeared on the content of segetalins A、B、E, suggesting processing has little effect on the content of segetalins. However, the dissolution rates of these three compounds in fried vaccariae semen were higher than those in crude vaccariae semen. Their improvement was 15.5%,5.7%,14.3% respectively. Hence, processing is able to improve the dissolution rates of segetalin A、 B, E.After processing, different changes appeared on the content of hypaphorine, vaccarin, saponarin, isovitexin-2"-O-arabinoside and vaccarin H. The content of isovitexin-2"-O-arabinoside improved 92.2%, but that of vaccarin, hypaphorine, saponarin and vaccarin H decreased 25.7%,7.7%、11.1%and 17.3%, respectively. However, the dissolution rates of these five compounds were higher than those in crude vaccariae semen. Their improvement was 7.7%、9.3%、12.4%、12.4%、18.4% respectively. Therefore, processing is able to improve the dissolution rates of these five compounds.