Ptp1b Inhibitors From Chinese Herbal Medicine To Find

Pseudorix kaempferi Gord. is widely distributed in the east and southeast of China. The root and trunk barks were popularly known as traditional Chinese medicine "Tu-Jin-Pi", which had been widely used for treatment of skin diseases caused by fungal infections in China. It showed actions with antifungal, antitumor, antifertility in morden pharmacological laboratory experiment. Under the high througth put screening technology, we discovered the extracting solution had inhibitory effect on PTP1B enzyme in vitro, active test. By bioactivity-guided we isolated the water-solubility components.Through our research work, 20 compounds were isolated from the 70% ethanol extract of the trunk barks of Pseudorix kaempferi Gord, of which structures of 16 comounds have been elucidated as 2,6-dihydroxyterephthalic acid (PK-1), gallic acid (PK-2), p-benzoic acid (PK-3), isovanillic acid (PK-4), syringic acid (PK-5), l-C-(4-hydroxyphenyl)-glycerol (PK-6), p-hydroxy benzaldehyde (PK-7), syringic aldehyde (PK-8), 4-hydroxyphenyl-β-D-allopyranoside (PK-9), oleanolic acid (PK-10), 3β-acetyloleanolic acid (PK-11), oleanolic acid 3-O-β-D-glucuronyl-6'-ethyl ester (PK-12), dammar-24(25)-ene-3β, 6α, 12β, 20(S)-tetraol-20-O-β-D-pyranoglucoside (PK-13), ellagic acid (PK-14), osthole (PK-15), uracil (PK-16).Among them, compound PK-9 and PK-12 were novel compounds. Compound PK-1 was a new natural product as well as compounds (PK-2～PK-8, PK-10～PK-11 and PK-13～PK-16) isolated from Pseudorix genus for the first time.The pharmacological inhibitory bioactivities of all these compounds on PTP1B enzymic were evaluated. The results showed that compounds PK-9, PK-10, PK-11, PK-12, PK-13 and PK-14 could inhibited the PTP1B enzymic.Amebia enchroma (Royle) Johnst. is widely distributed in Xinjiang Province, northwest of China. The rhizome of it had been widely used as traditional Chinese medicine and it showed pharmacological actions with antifungal, antitumor, anti-immune deficiency. We discovered the extracting solution had inhibitory effect on PTP1B enzyme in vitro, active test. By bioactivity-guided we isolated the lipid soluble components.Through our research work, 8 compounds were isolated from the 70% ethanol extract of the rhizome of Amebia enchroma, of which structures of 6 comounds have been elucidated as deoxyshikonin (AE-1), shikonin (AE-2), quercetin (AE-3), kaempferol (AE-4), acacetin (AE-5),β-sitosterol (AE-6). Among them, acacetin (AE-5) isolated from Amebia genus for the first time.The pharmacological inhibitory bioactivities of all these compounds on PTP1B enzymic were evaluated. The results showed that compounds AE-1, AE-2, AE-3 and AE-5 could inhibited the PTP1B enzymic.