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Natural products are an abundant and environmentally friendly source for controlling plant pathogens and insect pests. Toward the development of new natural product-based pesticides, here, a series of osthole-based isoxazoline derivatives were prepared by [3 + 2] annulation and evaluated for their insecticidal activities and toxicities. The structures of all osthole-based isoxazoline derivatives were characterized by various spectral analyses, and derivative

To improve the insecticidal activity of (+)-nootkatone, a series of 42 (+)-nootkatone thioethers containing 1,3,4-oxadiazole/thiadiazole moieties were prepared to evaluate their insecticidal activities against

Natural products (NPs) are very important sources for the development of new drugs. Merrillianone and cycloparvifloralone, isolated from the roots, stems, and fruits of Illicium henryi Diels, are two natural sesquiterpene compounds. In continuation of our effort to discovery more effective neurotrophic compounds from NPs, a series of novel merrillianone/cycloparviforalone based esters 2a-i, 3a-g and 3i-q were prepared and their structures were characterized by 1H NMR, 13C NMR and IR spectral analyses. Furthermore, the spatial structure of compound 2h was unambiguously confirmed by X-ray crystallography. The neurite outgrowth-promoting activity results indicated that most of the target derivatives exhibited more potent neurite outgrowth-promoting activity than merrillianone and cycloparviforalone. Among all target derivatives, the neurite outgrowth-promoting activity of compounds 2a, 3a and 3b was about 2-fold stronger than that of their precursors merrillianone and cycloparviforalone, respectively. Besides, compounds 2a and 3a displayed relatively low cytotoxicity to normal GES-1 cells. Moreover, these derivatives had good hydrolytic stability. Finally, some interesting results of the structure-activity relationships (SARs) were also discussed. This work will pave the way for the development of merrillianone/cycloparviforalone derivatives as potential neurotrophic agents.

The perfluorooctanoic acid (PFOA) poses a high risk for aquatic organisms. Nevertheless, the current toxicity studies rarely report how PFOA affects different cell populations during the embryonic development of fish. Here, the zebrafish embryos at 2-30 hpf were exposed to 1-100 μg/L PFOA. The heartbeat and locomotor behavior were significantly decreased after ≥ 25 μg/L PFOA exposure. The single-cell RNA sequencing showed that PFOA exposure influenced nine cell populations, including heart cells, hatching gland cells, macrophages, lens cells, ionocytes, melanoblasts, optic cup cells, periderm cells, and differentiating neurons cells. Among them, heart cells were the most affected cell population. Functions of cardiac muscle contraction, actin cytoskeleton and oxygen binding were significantly changed in the heart cells, which were involved in the altered expressions of tnni2a.4, acta1a, atp1a1a.2, mylpfa, and so on. Besides, the changes of apoptotic process, innate immune response, and translation in lens cells, hatching gland cells, macrophages and ionocytes should also be of concern. Our study indicates that 2-30 hpf of embryonic development is the sensitivity window for the PFOA exposure. Identification of the target cell population provides clear information of the toxic endpoint of PFOA, which sheds new light on the risk assessment of PFOA on aquatic organisms.