Luo Xiaodong research team of Kunming Institute of Botany, Chinese Academy of Sciences: Study on novel structure and pharmacological activity of plant alkaloids

Lead alkaloids have complex structures and significant physiological activities, which have attracted the attention of organic chemists and pharmacists for a long time Luo Xiaodong research team of Kunming Institute of Botany, Chinese Academy of Sciences has been committed to the research of novel structure, efficacy and new drug creation of alkaloids in medicinal plants for a long time In this research direction, more than 60 papers have been published, 11 of which have been published in organic letters 13 novel / active alkaloids reported by the research team have been introduced as hot molecules by Nat Prod Rep In recent years, the team has isolated three complex units (org Lett 2018, 20, 4116-4120) and multiple heterocycles (org Lett 2018, 20, 2702-2706), as well as isoquinoline alkaloids (org Lett 2018, 20, 1647-1650), which have a unique framework of benzofuranolactone substituted by dimethyl group Luo Xiaodong's research team is mainly based on the discovery of novel and diverse alkaloids and natural products of limonoids, enriching the structural types of natural products Based on the structural characteristics of compounds and the knowledge of folk medicine, through the comprehensive evaluation of the mechanism of action and drug-forming ability, the research team used modern methods to interpret traditional drugs and develop innovative drugs Every year, the research group has postdoctoral, doctoral and master's candidates We welcome students who are interested in pharmaceutical chemistry to join the research group Luo Xiaodong received his Bachelor of engineering degree from the Department of chemistry, East China University of science and technology in 1991, and his doctor of Science degree from Kunming Institute of Botany, Chinese Academy of Sciences in 1999 Later, he engaged in postdoctoral and visiting research at the City University of New York and Oxford University Currently, he is the "core backbone of specially hired researchers" of the Chinese Academy of Sciences, the winner of the national fund for Distinguished Young Scholars, the leader of the "ten thousand talents plan" of the Central Organization Department, and the "leader of young and middle-aged technological innovation" of the Ministry of science and technology It is mainly engaged in the research on the structure and function of natural products and the creation of new drugs (pesticides) It has formed the characteristics from systematic basic research to the creation of new drugs (pesticides) in the field of indole alkaloids and limonoids At present, as the first / corresponding author, he has published more than 120 SCI papers in Chem Rev., org Lett The research results enrich the structural types of natural products, and the basic research has been selected into the 2012 annual report of NSFC Under the support of "major new drug creation" and "863 Plan", researcher Luo Xiaodong further expanded the basic research results of indole alkaloids, limonoids and induced phytochemistry to the application fields: 1 Presided over and completed the preclinical research of new drug "dengtaiye alkali", and obtained the approval document for clinical trials of drugs issued by CFDA, and now is in the process of II Phase II clinical trial; 2 The development of neem limononin obtained the temporary pesticide registration certificate and was approved to be used in AA (organic) grade green food production pesticides (NY / t393-2013); 3 The cooperation with Yunnan Institute of ecological agriculture to induce and cultivate purple root water hyacinth, excavate the active substances of cyanobacteria inhibition, and get demonstration and promotion in the purification of polluted water Researcher Luo is now the executive editor of natural products & bioprosecting, the editorial board member of China natural medicine, the outstanding scholar of "light of the west" of the Chinese Organization Department and the Chinese Academy of Sciences, the outstanding contribution award of the western scholar of the Chinese Academy of Sciences, and the outstanding graduate guidance teacher of the Chinese Academy of Sciences The results of advanced scientific research (1) the multiple drug resistance and side effects caused by the abuse of Paeonia like indole alkaloid antibiotics, which have potential antibacterial activity, are seriously threatening human health, and the natural small molecules derived from plant antibacterial and antifungal have been concerned by scientists Luo Xiaodong's research team combined with the original research background and focused on the current research focus, selected traditional medicinal materials rich in monoterpene indole alkaloids to carry out relevant research, and made some research progress Ervatamia chinensis is mainly used to treat sore throat and furuncle and other diseases in the folk Luo Xiaodong's research team found the pitcher like indole alkaloids erchinines A and B from this medicine The unique structure of Ervatamia chinensis has the complex unit fragments of diazoproxazolidine and three hemiacetaldehyde amines Erchinines A and B showed a potential inhibitory activity (MIC: 0.78 μ g / ml) to Bacillus subtilis, while erchinine B showed a potential inhibitory activity (MIC: 6.25 μ g / ml) to Trichophyton rubrum, which was similar to that of griseofulvin The potential inhibition of erchinines A and B on Bacillus subtilis (source: org Lett 2018, 20, 4116-4120) The research results were published online on or g lett (org Lett 2018, 20, 4116-4120) under the title of "Nepenthes like indole alkaloids with antimicrobial activity from Ervatamia China" （2） Voacanga Africana, a complex ring indole alkaloid with potential antibacterial activity, was isolated from the African horsebell fruit and mainly used in the folk for the treatment of malaria, dysentery, ulcer and other diseases Luo Xiaodong's research team isolated the indole alkaloids voacafarines A and B from the plant, and their structural units contain pyrrole / pyridine / pyrrole/ Piperidine / furan fused heterocyclic system The results of antibacterial activity study showed that voacafarines A and B showed potential inhibitory activity against Staphylococcus aureus and Salmonella typhi, and the results were better than those of berberine and rattan The potential inhibition of voacafarines A and B on Staphylococcus aureus and Salmonella typhi (source: org Lett 2018, 20, 2702-2706) The research results are published in org Lett (org Lett 2018, 20, 20, 2702-2706） 。
（3） Dactylicapnos scandens, a potential anti-inflammatory alkaloid, was found in zijinlong, which is a famous traditional medicine in Yunnan Province, rich in isoquinoline alkaloids It is widely used in anti-inflammatory and analgesic In the early stage, researchers developed the listed drugs of anti adrenergic and analgesic, isoclonidine hydrochloride tablets and myopic eye drops from zijinlong Recently, a new aporphine alkaloid dactylacetone a was found in zijinlong by Dr Wang Bei and his partners The compound has a unique framework of gemodimethyl substituted benzofuranolactone, which is a double broken and recombined aporphine structure Preliminary pharmacological study showed that dactylacetone a had better inhibitory effect on IL-1 β and PGE2 released by RAW264.7 cells stimulated by LPS at the concentration of 2.4-12 μ m compared with dexamethasone (20.0 μ m) in the control group The results enrich the diversity of AIQ alkaloids and provide the possibility for the discovery of natural non steroidal anti-inflammatory lead compounds The inhibitory effect of dactylactone a on IL-1 β and PGE2 (source: org Lett 2018, 20, 1647-1650) The above research results were published in org Lett (org Lett 2018, 20, 1647-1650) under the title of "anti inflamatoryisoquinoline with BIS seco aporphine skeleton from Dactylicapnos scandens" While exploring the beauty of novel alkaloid structure in nature, the research team also evaluated its biological activity, making these novel skeleton compounds possible to become the leading compounds in modern drug development Nowadays, people and scientific research have been paid more and more attention in the economic life China has ushered in the "node of science and technology explosion" Behind the progress of science and technology is the work of countless scientists In the field of chemistry, in the context of the pursuit of innovation driven, international cooperation has been strengthened, the influence of Returned Scholars in the field of R & D has become increasingly prominent, and many excellent research groups have emerged in China For this reason, CBG information adopts the 1 + X reporting mechanism CBG information, chembeangoapp, chembeango official microblog, CBG wechat subscription number and other platforms jointly launch the column of "people and scientific research", approach the domestic representative research group, pay attention to their research, listen to their stories, record their demeanor, and explore their scientific research spirit.