Potent vasorelaxant analogs from chemical modification and biotransformation of isosteviol

Bioactivity Profile of the Diterpene Isosteviol and its Derivatives

“…These bio-transformations are performed to obtain metabolites that are more bioactive than the parent compound. Cunninghamella echinulata NRRL 1386 is the fungus used to obtain the isosteviol metabolite (Figure 2B) that has a 17-fold increase in vaso-relaxant activity as compared to the parent isosteviol [50]. Pancreatin catalyst demonstrated the best hydrolytic efficiency, producing isosteviol at a yield of 93.9% at low pH of 4.0 [51].…”

Diterpenoids of terrestrial origin

“…120 Some derivatives of isosteviol with vasorelaxant properties have been prepared. 121 The cytotoxic and apoptosis-inducing activities of various steviol and isosteviol derivatives have been examined, including a number in which a heterocyclic ring has been added to ring D. [122][123][124] Seasonal variations in the formation of grandioric acid derivatives by Mikania (Asteraceae) species have been noted. 125 A number of kaurenes have been associated with the cytotoxic activity of medicinal plants.…”

Synthesis and characterization of new pyrazole–tetrazole derivatives as new vasorelaxant agents

“…In fact, hypertension is considered as risk factor of the most known cardiovascular disease that can be responsible of coronary disease, stroke, and sudden death (Lawes et al, 2008). It is also the main causes of cardiac failure and renal insufficiency (Wonganan et al, 2013). The literature reports a wide array of antihypertensive drugs are available for hypertensive patients, among which the vasodilators (Chidsey III & Gottlieb, 1974).…”