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Dimeric Acylphloroglucinol Derivatives with New Skeletons from Leptospermum scoparium |
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| Authors: | Kai Xia Ji-Hong Gu Xiao-Xue Fu Ni-Ping Li Mu Chen Qian Huang Wen-Jing Wang Wen-Cai Ye Lei Wang |
| Affiliation: | 1. Center for Bioactive Natural Molecules and Innovative Drugs Research, College of Pharmacy, Jinan University, Guangzhou, 510632 P. R. China Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, Jinan University, Guangzhou, 510632 P. R. China These authors contributed equally to this work.;2. Center for Bioactive Natural Molecules and Innovative Drugs Research, College of Pharmacy, Jinan University, Guangzhou, 510632 P. R. China Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, Jinan University, Guangzhou, 510632 P. R. China Science and Technology Innovation Center, Guangzhou University of Chinese Medicine, Guangzhou, 510405 P. R. China These authors contributed equally to this work.;3. Center for Bioactive Natural Molecules and Innovative Drugs Research, College of Pharmacy, Jinan University, Guangzhou, 510632 P. R. China Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, Jinan University, Guangzhou, 510632 P. R. China;4. Center for Bioactive Natural Molecules and Innovative Drugs Research, College of Pharmacy, Jinan University, Guangzhou, 510632 P. R. China |
| Abstract: | Leptosparones A–F ( 1 – 6 ), six new dimeric acylphloroglucinol derivatives with unprecedented skeletons, were isolated from Leptospermum scoparium. Compounds 1–3 and 5–6 are phenylpropanoyl-phloroglucinol dimers, while 4 is a phenylpropanoylphloroglucinol-isovalerylphloroglucinol hybrid. Structurally, these compounds represent the first examples of dimeric phloroglucinols with unprecedented C(7′)−C(8) linkage between the phloroglucinol core and the acyl side chain. Their structures were elucidated by comprehensive analyses of spectroscopic data, single crystal X-ray diffraction and chemical calculations. In addition, all compounds showed inhibitory effects against α-glucosidase with IC50 values ranging from 39.5 to 186.8 μM. |
| Keywords: | Leptospermum scoparium acylphloroglucinol dimer α-glucosidase inhibitory activity |