Studies On The Bioactive Constituents Of Styrax Perkinsiae And Rabdosia Coetsa

In this work, the bioactive components in two plants, Styrax perkinsiae Rehd and Rabdosia coetsa (Bach.-Ham.ex D. Don) Hara, were studied. 1. Five new compounds together with eighteen known compounds were isolated from the 95% ethanol extracts of the seeds of S. perkinsiae Rehd for the first time. Their structures were elucidated on the basis of spectral and chemical evidence. The new compounds isolated were determined as follows: 5-(3-hydroxypropyl)-7-methoxy-2-[2,3-dihydro-3-hydroxymethyl-7-methoxy-2-(3-methoxy-4-hydroxylphenyl)-benzofuran-5-yl] benzofuran (1), (E)-5-(3-oxopropenyl)-7-methoxy-2-(3,4-methylenedioxyphenyl) benzofuran (2), 5-(3-butanoyloxypropyl)-7-methoxy-2-(3,4-methylenedioxyphenyl) benzofuran (egonol butanate, 3), 5-(3-hydroxypropyl)-7-hydroxyl-2-(3,4-methylenedioxyphenyl) benzofuran (demethyl egonol, 4), and 5-(3-hydroxypropyl)-2,3-dihydro-3-hydroxymethyl-2-(3-methoxy-4-hydroxylphenyl)-benzofuran (demethoxy dihydrodehydrodiconiferyl alcohol, 5), and the known compounds were egonol (6), demethoxyl egonol (7), egonol acetate (8), demethoxyl egonol acetate (9), egonol glucoside (10), egonol gentiobioside (11), egonol gentiotrioside (12), lariciresinol (13), dihydrodehydrodiconiferyl alcohol (14), pinoresinol (15), succinic acid (16), (2S,3S,4R,10E)-2[(2'R)-2'-hydroxytetracosanoyl amino]-10-octadecene-1,3,4-triol (17), β-sitosterol (18), β-daucosterol (19), pentacosanoic acid (20), heneicosoic acid (21), stearic acid (22), glyceroyl monopalmitate (23), respectively. In vitro test, compounds 4, 11 and 12 promote the synthesis of estrogen E2 in ovarian granule cells of mice, 3T3-L1 adipose cells of mice, and ROS1728 osteoblasts of rats, and the mean yields of estrogen E2 were 80.80%, 212.16% and 278.28% higher than those of blank control at a concentration of 100 μg/ml, respectively. Compounds 6 (a high content in the seeds of S. perkinsiae) and 12 were tested in vivo on ovariectomized mice, the results showed that the E2 level in the serum of mice could be elevated by compound 12, but not by compound 6. On the other hand, Compounds 1 and 4 exhibited cytotoxic activity in vitro on two breast cancer cell lines MCF-7 and MDA-MB-231 with a mean GI50 value of 4.63 and 14.39 μg/mL, respectively. 2. Bioassay-guided isolation of the 95% ethanol extract of the whole plants of R. coetsa led to 7 compounds. They were identified as ethyl caffeate (24), rosmarinic acid (25), methyl rosmarinate (26), betulinic acid (27), uvaol (28), 2α,3β-dihydroxyursolic acid (29) and ursolic acid (30) by spectral analysis. Rosmarinic acid (25), methyl rosmarinate (26), and ethyl caffeate (24) inhibited ACE by 103.89%, 76.36% and 54.81% at a concentration of 100 μg/ml, respectively. 3. The research on aromatase in recent years was summarized.