1.Effects of Ivermectin on Migration and Invasion of Human Gastric Cancer Cells BGC- 823 and MGC- 803 and Its Mechanism
Yanjiao XIE ; Shaoyi KUANG ; Huiming DENG ; Daorui YU ; Haofei FAN ; Hao JIA ; Qiang LIU
China Pharmacy 2019;30(5):621-627
OBJECTIVE: To study the effects of ivermectin on the migration and invasion of human gastric cancer cell lines BGC-823 and MGC-803 and its mechanism. METHODS: After treated with 0, 2.5, 5, 10, 20, 40 μmol/L ivermectin for 24 h, inhibitory rate of human gastric cancer cell lines BGC-823 and MGC-803 were detected by MTT assay. Effects of 5 μmol/L ivermectin and phosphate buffercontaining 0.67‰ dimethyl sulfoxide (control group) for 24 h on the migration and invasion of` gastric cancer cells BGC-823 and MGC-803 were observed by Transwell chamber invasion assay.Western blot assay was used to detect the protein expression of TGF-β1, TGF-βR, Smad2 and Smad3 in epithelial-mesenchymal transition (EMT) markers E-cadherin, N-cadherin, Vimentin, Snail and EMT transduction pathway TGF-β/smad of BGC-823 and MGC-803 cells after treated with 5, 10 μmol/L ivermectin and phosphate buffercontaining 0.67‰ dimethyl sulfoxide (control group) for 24 h. RESULTS: Ivermectin could inhibit the growth of BGC-823 and MGC-803, inhibitory rate of it was positively correlated with its concentration. Compared with control group, the number of migration and invasion BGC-823 and MGC-803 cells were decreased significantly after treated with 5 μmol/L ivermectin (P<0.01 or P<0.001); the expression of E-cadherin protein was enhanced significantly in BGC-823 and MGC-803 cells after treated with 5 and 10 μmol/L ivermectin (P<0.05 or P<0.01 or P<0.001); the protein expression of N-cadherin, Vimentin, Snail, TGF-βR, Smad2 and Smad3 were decreased significantly (P<0.05, P<0.01 or P<0.001); protein expression of TGF-β1 was decreased significantly after treated with 10 μmol/L ivermectin (P<0.05). CONCLUSIONS: Ivermectin can significantly inhibit the migration and invasion of gastric cancer cells BGC-823 and MGC-803, and inhibiting the biological activity of EMT by reducing the expression of TGF-β/smad pathway is one of the mechanisms that inhibit the migration and invasion of gastric cancer cells.
2.Antimicrobial indole alkaloids from Tabernaemontana corymbosa.
Kun FAN ; Lanchun ZHANG ; Bangyin TAN ; Guy S S NJATENG ; Malong QIN ; Ruirong GUO ; Xiaojuan HUANG ; Cai-Feng DING ; Weimin GAO ; Rongping ZHANG ; Haofei YU
Chinese Journal of Natural Medicines (English Ed.) 2023;21(2):146-153
Four unreported monoterpene indole alkaloids, tabernaecorymines B-E (1-4), together with twenty-one known indole alkaloids (5-25) were obtained from the stem bark of Tabernaemontana corymbosa. Their structures and absolute configurations were elucidated by extensive spectroscopy, quantum chemical calculations, DP4+ probability analyses and Mo2(OAc)4-induced electronic circular dichroism experiment. The antibacterial and antifungal activities of these compounds were evaluated and some of them showed significant activity against Staphylococcus aureus,Bacillus subtilis, Streptococcus dysgalactiae and Candida albicans.
Tabernaemontana
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Anti-Infective Agents
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Antifungal Agents
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Anti-Bacterial Agents
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Indole Alkaloids