Studies On The Chemical Constituents In Herb Of Hedyotis Diffusa

Bai-Hua-She-She-Cao Hedyotis diffusa Willd. (Rubiaceae) is a medicinal herb.It is widely distributed in subtropical regions, including Guangdong, Guangxi, Fujian,Hunan, Sichuan, Guizhou, Yunnan, etc. In traditional Chinese medicine, it has theeffect of“clearing away heat and toxic material, relieving stranguria by diuresis,promoting blood circulation and removing blood stasis”. It is a well-known Chinesefolk-medicine orally used for the treatment of appendicitis, hepatitis, urinary tractinfections, bronchitis, enteritis, bleeding, sore throat, and malignant tumor, andexternally used for the treatment of venomous snake bite, mumps, acne, furunculosis,seborrhea dermatitis, etc. In recent years, it is extensively used for the treatment ofvarious types of cancers.The chemical constituents of Bai-Hua-She-She-Cao were studied by multiplechromatographical techniques (such as silica gel chromatography, Sephadex LH-20and PHPLC etc.). On the basis of physicochemical evidence and spectral analysis(lD,2D-NMR, MS etc.), 25 compounds were obtained from its 95% ethanol extract, andthe structures of 20 compounds among them were identified as deacetylasperulo-sidic acid methyl ester (HD-1), scandoside methyl ester (HD-2), 6?-O-(2-hydroxy-propyl)geniposide (HD-3), 6?-O-(2-hydroxy-propyl)geniposide (HD-4), 6?-O-(1-hydroxymethyl-ethyl)geniposide (HD-5), 6?-O(1-hydroxymethyl-ethyl)geniposide(HD-6), 6?-O-ethylgeniposide (HD-7), 6?-O-ethylgeniposide (HD-8), 10-dehydro-geniposide (HD-9), 6?-O-p-trans-coumaroylgeniposide (HD-10), quercetin 3-O-[2?-O-(6(?)-O-E-sinapoyl)-?-D-glucopyranosyl]-?-D-glucopyranoside (HD-11), quercetin3-O-[2?-O-(E-6(?)-O-feruloyl)-?-D-glucopyranosyl]-?-D-glucopyranoside (HD-12),quercetin 3-O-[2?-O-(E-6(?)-O-feruloyl)-?-D-glucopyranosyl]-?-D-galactopyranoside (HD-13), kaempferol (HD-14). quercetin (HD-15), p-coumaric acid (HD-16),4-methoxycinnamic acid (HD-17), 2-formyl-5-hydroxylmethyl-furan (HD-18), 2-hydroxy-3-methylanthraquinone (HD-19), stigmasterol (HD-20).Among them, compounds HD-3?8 were 6 new iridoids compounds and theywere 3 pairs of epimer; compounds HD-1, 17, 18 were isolated from Hedyotisdiffusa for the first time, compound HD-9 as iridoids was isolated from genusHedyotis for the first time.The chemical constituents of the Hedyotis diffusa, pharmacological effects andidentification of the authenticity of the research progress were reviewed by use ofdocuments and our research work.