Discovery of Novel (+)-Nootkatone-Based Amine Derivatives as Potential Insecticide Candidates.

To discover novel natural product-based insecticides, a series of (+)-nootkatone-based amine derivatives were prepared and evaluated for their insecticidal activities against Walker, Sulzer, and Linnaeus. Insecticidal assays showed that most of the title (+)-nootkatone derivatives exhibited stronger insecticidal activities against three insect pests than the precursor (+)-nootkatone after the introduction of amine groups on the parent (+)-nootkatone. Compounds , , , , , , and displayed more promising growth inhibitory (GI) effect against than the commercially available botanical insecticide toosendanin.

Preparation and Biological Evaluation of Novel Osthole-Derived -Benzoylthioureas as Insecticide Candidates.

To discover novel natural-product-based insecticide candidates, herein, a variety of osthole-derived -benzoylthioureas were synthesized and assessed for their insecticidal activities against three insect pests. An insecticidal assay showed that most of the target osthole-derived -benzoylthioureas displayed a more potent and broad-spectrum insecticidal effect than the parent osthole after the introduction of -benzoylthioureas on the C-3' position of osthole. Compound displayed the most potent growth inhibitory (GI) effect on Walker, with a final corrected mortality rate of 82.

Eupalinolide A induces autophagy via the ROS/ERK signaling pathway in hepatocellular carcinoma cells and .

Hepatocellular carcinoma is the most common primary malignancy of the liver. The current systemic drugs used to treat hepatocellular carcinoma result in low overall survival time. It has therefore been suggested that new small‑molecule drugs should be developed for treating hepatocellular carcinoma.

Eupalinolide B inhibits hepatic carcinoma by inducing ferroptosis and ROS-ER-JNK pathway.

Primary hepatic carcinoma is a common malignant tumor. The classic molecular targeted drug sorafenib is costly and is only effective for some patients. Therefore, it is of great clinical significance to search for new molecular targeted drugs.

Design, Synthesis, and Biological Evaluation of Novel Osthole-Based Isoxazoline Derivatives as Insecticide Candidates.

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 was further confirmed by X-ray crystallography.

Development of Novel (+)-Nootkatone Thioethers Containing 1,3,4-Oxadiazole/Thiadiazole Moieties as Insecticide Candidates against Three Species of Insect Pests.

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 Walker, Sulzer, and Linnaeus. Insecticidal evaluation revealed that most of the title derivatives exhibited more potent insecticidal activities than the precursor (+)-nootkatone after the introduction of 1,3,4-oxadiazole/thiadiazole on (+)-nootkatone. Among all of the (+)-nootkatone derivatives, compound (1 mg/mL) exhibited the best growth inhibitory (GI) activity against with a final corrected mortality rate (CMR) of 71.

Discovery of Natural Product-Based Fungicides (III): Semisynthesis and Biological Activity of N-Phenylpyrazole Sarisan Hybrids as Antifungal Agents.

Many phytopathogenic fungi can easily infect crops, resulting in crop yield reductions. In continuation of our efforts to develop natural product (NP)-based antifungal agents, a series of N-phenylpyrazole sarisan hybrids 6a-v were prepared via I -mediated oxidative cyclization, and their structures were determined by various spectral analyses including IR, H-NMR and ESI-MS. Among all N-phenylpyrazole sarisan hybrids, compounds 6a, 6b, 6e, 6i, 6j and 6r exhibited more encouraging antifungal action against at least two phytopathogenic fungi than the reference fungicide hymexazol.

Development of Membrane-Active Honokiol/Magnolol Amphiphiles as Potent Antibacterial Agents against Methicillin-Resistant (MRSA).

Currently, infections caused by drug-resistant bacteria have become a new challenge in anti-infective treatment, seriously endangering public health. In our continuous effort to develop new antimicrobials, a series of novel honokiol/magnolol amphiphiles were prepared by mimicking the chemical structures and antibacterial properties of cationic antimicrobial peptides. Among them, compound showed excellent antibacterial activity against Gram-positive bacteria and clinical MRSA isolates (minimum inhibitory concentrations (MICs) = 0.