RESUMEN
Elemene, derived from Curcuma wenyujin, one of the "8 famous genuine medicinal materials of Zhejiang province," exhibits remarkable antitumor activity. It has gained wide recognition in clinical practice for effectiveness on tumors. Dr. XIE Tian, introduced the innovative concept of "molecular compatibility theory" by combining Chinese medicine principles, specifically the "monarch, minister, assistant, and envoy" theory, with modern biomedical technology. This groundbreaking approach, along with a systematic analysis of Chinese medicine and modern biomedical knowledge, led to the development of elemene nanoliposome formulations. These novel formulations offer numerous advantages, including low toxicity, well-defined composition, synergistic effects on multiple targets, and excellent biocompatibility. Following the principles of the "molecular compatibility theory", further exploration of cancer treatment strategies and methods based on elemene was undertaken. This comprehensive review consolidates the current understanding of elemene's potential antitumor mechanisms, recent clinical investigations, advancements in drug delivery systems, and structural modifications. The ultimate goal of this review is to establish a solid theoretical foundation for researchers, empowering them to develop more effective antitumor drugs based on the principles of "molecular compatibility theory".
Asunto(s)
Humanos , Estudios Retrospectivos , Antineoplásicos/uso terapéutico , Neoplasias/tratamiento farmacológico , Medicamentos Herbarios Chinos/uso terapéutico , Sesquiterpenos/uso terapéuticoRESUMEN
In the present study, a series of 13-β-elemene ester derivatives were designed and prepared, and their antioxidant activity was investigated in the H2O2-treated human umbilical vein endothelial cells (HUVECs). Among the test compounds, the dimer compounds 5v and 5w exhibited the most potent antioxidant activity with significant ROS suppression being observed. Both compounds markedly inhibited the H2O2-induced changes in various biochemical substances, such as superoxide dismutase (SOD), malonyldialdehyde (MDA), nitric oxide (NO), and lactic dehydrogenase (LDH), which were superior to that of the positive control vitamin E. Further more, they did not produce any obvious cytotoxicity, but increased the viability of HUVECs injured by H2O2 in a dose-dependent manner. Additionally, compound 5w, designed as a prodrug-like compound, showed improved stability relative to compound 4 in vitro.
Asunto(s)
Humanos , Antioxidantes , Metabolismo , Farmacología , Células Cultivadas , Curcuma , Química , Estabilidad de Medicamentos , Medicamentos Herbarios Chinos , Química , Farmacología , Endotelio Vascular , Biología Celular , Metabolismo , Células Endoteliales de la Vena Umbilical Humana , Peróxido de Hidrógeno , Metabolismo , Malondialdehído , Metabolismo , Óxido Nítrico , Metabolismo , Oxidación-Reducción , Estrés Oxidativo , Ácidos Ftálicos , Farmacología , Sesquiterpenos , Farmacología , Succinatos , Farmacología , Superóxido Dismutasa , MetabolismoRESUMEN
Natural products have been an important source of new drugs, which also played a dominant role in the discovery and research of new drugs for the treatment of hypertension. This review article reviews the recent progress in the research and development of natural lead compounds with antihypertensive activity, including alkaloids, diterpenes, coumarins, flavonoids, and peptides. We summarized their structures, sources, as well as the antihypertensive mechanisms. These information provides instructive reference for the following structural modifications and optimization.
Asunto(s)
Humanos , Antihipertensivos , Farmacología , Usos Terapéuticos , Productos Biológicos , Farmacología , Usos Terapéuticos , Hipertensión , Quimioterapia , Magnoliopsida , Química , Péptidos , Farmacología , Usos Terapéuticos , Fitoquímicos , Farmacología , Usos Terapéuticos , Fitoterapia , Extractos Vegetales , Farmacología , Usos TerapéuticosRESUMEN
AIM@#In a search for new cardiovascular drug candidates, a series of novel oxime ethers derived from a natural isochroman-4-one were synthesized.@*METHOD@#Compounds 3 and 6, derived from the natural antihypertensive compound 7, 8-dihydroxy-3-methyl-isochroman-4-one (XJP), were designed and synthesized. Subsequently, a series of novel isochroman-4-one oxime ether hybrids were prepared by hybridizing various N-substituted isopropanolamine functionalities to isochroman-4-one oxime. Furthermore, β1-adrenergic blocking activities of the synthesized compounds were assayed using the isolated rat left atria.@*RESULTS@#Twenty target compounds were obtained, and the preliminary structure-activity relationships were deduced. The most promising compound Ic exhibited β1-adrenoceptor blocking activity (inhibition: 52.2%) at 10(-7) mol·L(-1), which was superior to that of propranolol (inhibition: 49.7%).@*CONCLUSION@#The results suggested that natural product XJP/isopropanolamine moiety hybrids may provide a promising approach for the discovery of novel cardiovascular drug candidates.