Search

Penicamins A-L ( 1 - 12 ), 12 highly oxygenated novel diterpenes, were obtained from the fungus Penicillium camemberti JSB-7212. Compounds 1 - 12 share the same 7/6/5 tricyclic skeleton as valparane-type diterpenes but differ in the absolute configurations at C-7, C-11, and C-14, as well as in the oxidation levels at C-6 and C-8, which were determined through extensive spectroscopic data interpretation. Stereochemical assignments of compounds 1 , 2 , and 4 - 12 were established by single-crystal X-ray diffraction, and the absolute configuration of 3 was determined by analysis of the NOESY data and biogenetic consideration. Compounds 2 and 3 were immunosuppressive against lipopolysaccharide (LPS)-induced B cells, with IC 50 values of 3.0 and 7.9 μM, respectively. They also moderately suppressed concanavalin A (ConA)-induced T cell proliferation, with IC 50 values of 19 and 20 μM, respectively.

Benign prostatic hyperplasia(BPH) is a common disease of the male urinary system, and its incidence rate in China is increasing. However, the mechanism underlying the pathogenesis of BPH remains unclear. Some studies demonstrated that the incidence of BPH was related to the change in the levels of steroid hormones. Too high content of dihydrotestosterone(DHT) in the body may cause BPH and other related diseases. Testosterone(T) is converted to DHT by 5α-reductase(SRD5A). By inhibiting the activity of this enzyme, the production of DHT can be reduced, and then the incidence of BPH can be lowered. Therefore, it has drawn great attention to screen and discover safer and more effective 5α-reductase inhibitors from natural medicines to treat prostatic hyperplasia without affecting the physiological function of men. This review summarizes the characteristics and tissue distribution of 5α-reductase, the discovery of 5α-reductase inhibitors in traditional Chinese medicine and natural medicines, 5α-reductase inhibitors commonly used in clinical practice and their side effects, as well as the animal models of prostatic hyperplasia and common detection indicators, aiming to provide a reference for more in-depth understanding and research about BPH and development of drugs.

Twelve new austalide meroterpenoids ( 1 - 12 ) were isolated from the endophytic fungus Diaporthe sp. XC1211. Their structures were elucidated by extensive spectroscopic analysis. The absolute configurations of compounds 1 , 3 , 4 , and 6 were established by single-crystal X-ray diffraction, whereas those for the others were established by experimental electronic circular dichroism (ECD) data analysis. Compounds 1 - 12 represent a rare class of austalides with a 24α-CH 3 . Compounds 2 and 5 demonstrated potent proliferation inhibitory effects against LPS-induced B cells with IC 50 values of 6.7 (SI = 3.6) and 3.8 (SI > 13) μM, respectively. Compounds 2 and 5 decreased the secretion of IL-6 in LPS-induced B cells in a dose-dependent manner.

Peniandranoids A-E ( 1 - 5 ), five new meroterpenoids, together with three known analogues ( 6 - 8 ), were isolated from the fermentation of a soil-derived fungus, Penicillium sp.sb62. Their structures including absolute configurations were determined by extensive spectroscopic analysis, and the absolute configurations of compounds 1 and 5 were further elucidated by single-crystal X-ray diffraction. Peniandranoids A-E belong to a rare class of andrastin-type meroterpenoids incorporating an extra polyketide unit (a C 10 polyketide unit for 1 and 2 , a C 9 polyketide unit for 3 and 4 , and a furancarboxylic acid unit for 5 ). Compounds 1 and 6 exhibited favorable inhibitory activities against influenza virus A (H1N1) with EC 50 values of 19 and 14 μg/mL, respectively. Compounds 3 - 8 exhibited potent immunosuppressive activities against concanavalin A-induced T cell proliferation with EC 50 values ranging from 4.3 to 27 μM and lipopolysaccharide-induced B cell proliferation with EC 50 values ranging from 7.5 to 23 μM, respectively.