Spiro Meroterpenoids from Ganoderma applanatum.

Spiroapplanatumines A-Q (1-12, 14-16, 18, and 20), new spiro meroterpenoids respectively bearing a 6/5/7 or 6/5/5 ring system, along with three known compounds, spirolingzhines A, B, and D, were isolated from the fruiting bodies of the fungus Ganoderma applanatum. Their structures including absolute configurations were assigned by using spectroscopic methods, ECD and 13C NMR calculations, and single-crystal X-ray diffraction analysis. Biological evaluation of all the compounds disclosed that compounds 7 and 8 inhibited JAK3 kinase with IC50 values of 7.0 ± 3.2 and 34.8 ± 21.1 µM, respectively.

Dihydrothiophene-condensed chromones from a marine-derived fungus Penicillium oxalicum and their structure-bioactivity relationship.

Four dihydrothiophene-condensed chromones including two new compounds oxalicumones D-E (1-2) and known oxalicumones A-B (3-4), along with five other known chromones were isolated from a culture broth of the marine gorgonian-associated fungus Penicillium oxalicum SCSGAF 0023. The structures of 1-2 were elucidated by spectroscopic analysis. Eleven derivatives 3a-3i and 4a-4b were obtained from the acylation of 3 and 4, respectively. Compounds 1-4, 3a-3e, 3g-3h, and 4b showed significant cytotoxicity against several carcinoma cell lines with IC50 ≤ 10 µM. And their structure-bioactivity relationship was discussed.

[Protective effect of morphine hypoxic preconditioning on liver against acute hypoxic-reoxygenation injury in rabbits].

OBJECTIVE: To investigate the protective effect of morphine hypoxic preconditioning on hepatic hypoxic/reoxygenation injury in rabbits and the mechanisms involved. METHODS: Hypoxic/reoxygenation injury was induced with inhalation of 8% O2 for 3 hours followed by air for 3 hours. Thirty male white New Zealand rabbits were randomly divided into 3 groups: normal control group (N group), hypoxic/reoxgenation group (H/R group) and morphine hypoxic preconditioning group (MO + H/R group). Animals in the H/R and MO + H/R groups received 5 mL of saline or 3 mg/kg of morphine respectively before the induction of hypoxic injury. Hepatic apoptosis was determined quantitatively by terminal deoxynucleotidyl transferase-mediated dUTP nick-end labeling (TUNEL) methods. The activity of superoxide dismulase (SOD) in liver tissues was measured at the end of reoxgygenation. RESULTS: A large number of TUNEL positive cells [(9.50 +/- 1.00)%] were observed in hepatic tissues of rabbits in the H/R group. The administration of morphine exerted a significant anti-apoptotic effect, as evidenced by reduced TUNEL-positive staining [(2.20 +/- 0.40)%, P < 0.05 vs. H/R group]. Compared with the H/R group, treatment with morphine increased SOD activity significantly [(85.57 +/- 19.37) vs. (48.35 +/- 15.84), P < 0.05)]. CONCLUSION: Morphine hypoxic preconditioning can protect rabbits against acute hepatic hypoxic/ reoxygenation injury by increasing SOD activity and reducing hepatic apoptosis.

Compounds from Polyphaga plancyi and their inhibitory activities against JAK3 and DDR1 kinases.

Plancyamides A (1) and B (3), plancypyrazine A (2), and plancyols A (4) and B (5), five new compounds (1-5), and three known ones (6-8), were isolated from the whole bodies of Polyphaga plancyi Bolivar. Their structures were elucidated by a combination of spectroscopic analyses including 1D and 2D NMR, and HRESIMS. Among them, compound 3 is racemic, chiral HPLC separation afforded its respective enantiomers. The absolute configuration of 1 was assigned by computational methods. Biological evaluation of all the compounds with exception of 7 and 8 discloses that compounds 2 and 4 could inhibit JAK3 kinase with IC50 values of 12.6 and 5.0µM, respectively. In addition, compound 4 exhibit inhibitory activity towards DDR1 kinase with IC50 value of 4.87µM.