Polyketides with Anti-Inflammatory Activity from Trichoderma koningiopsis, a Rhizosphere Fungus from the Medicinal Plant Polygonum paleaceum.

Twelve new fungal polyketides, koningiopisins I-P (1-8) and trichoketides C-F (9-12), together with six known congeners (13-18), were isolated from Trichoderma koningiopsis, a rhizosphere fungus obtained from the medicinal plant Polygonum paleaceum. Their structures and absolute configurations were established by spectroscopic analysis, single-crystal X-ray diffraction, the modified Mosher's method, chemical derivatization, the octant rule, and 13C NMR and ECD calculations. Compounds 1-5 are tricyclic polyketides possessing an octahydrochromene framework with a 6,8-dioxabicyclo[3.2.1]octane core. Compounds 7 and 8 contain a unique ketone carbonyl group at C-7 and differ from other members of this group of compounds with the ketone carbonyl group at C-1. Compounds 1, 2, and 13 showed inhibitory activity on LPS-induced BV-2 cells on NO production with IC50 values of 14 ± 1, 3.0 ± 0.5, and 8.9 ± 2.7 µM, respectively.

Collective synthesis of aspulvinone and its analogues by vinylogous aldol condensation of substituted tetronic acids with aldehydes.

A mild, modular and efficient synthetic method with broad substrate scope was developed for aspulvinones. Nine natural aspulvinones were synthesized, six of which were for the first time. The aldol condensation delivered Z-configuration products predominantly in MeCN. Meanwhile, alkoxy exchange occurred in MeOH and EtOH. Aspulvinone O and E, and substrate 49, 50, and 51 exhibited modest anti-SARS-CoV-2 activity in a high-throughput screening and enzyme kinetics assay.

Attitudes and Practice Regarding Disposal for Unwanted Medications among Young Adults and Elderly People in China from an Ecopharmacovigilance Perspective.

Due to the expensive cost and uncertain effectiveness of environmental management options in eliminating pharmaceutical residues, recently, decreasing the emission of pharmaceutical pollutants from a drug administration perspective has been considered a hot area of research. As a kind of drug administration for the environment, ecopharmacovigilance (EPV) emphasizes the source control of pharmaceutical pollutants. Disposal of unwanted medicines has been considered as the easiest target for source control of pharmaceutical contamination. Here, we focused on public attitudes and practice regarding disposal of unwanted medicines from the EPV perspective among 365 Chinese university young adults and 206 elderly retirement home residents. The results showed that the majority of respondents had positive attitudes, but exhibited inadequate awareness and poor practice. In addition, the young-adult respondents were found to pay more attention to the environmental problems posed by pharmaceutical residues, and be more supportive of the EPV intervention predominantly performed by pharmaceutical industries and pharmacists. Therefore, it is urgent to establish the standard medicine disposal protocols and educate the general public on the best way for medication disposal under the principle of EPV in China, and efforts on environmentally-preferred drug disposal under EPV should target for the specific demographics.