Effects of Abietane diterpenes from Rosmarinus officinalis on guinea pig hearts

A plant in the Lamiaceae family, rosemary ( Rosmarinus officinalis ) is a perennial shrub native to the Mediterranean region. The current study used right atrial specimens from guinea pigs to assess the biological activity of 3 catechol diterpenes with an abietane skeleton―carnosic acid (CA ― 1), demethylsalvicanol (DS ― 1), and carnosol (CN ― 1)―contained in rosemary. Administration of CA ― 1 had a positive inotropic effect (PIE) while administration of CN ― 1 conversely had a negative inotropic effect (NIE). Administration of DS ― 1 resulted in no changes in myocardial contractility. Administration of CA ― 1 or DS ― 1 did not result in significant changes in heart rate. However, administration of CN ― 1 had a negative chronotropic effect (NCE), and administration of CN ― 1 at a final concentration of 10 － 4 M caused cardiac arrest. In addition, the PIE of CA ― 1 was inhibited by prior administration of the phosphodiesterase (PDE) inhibitor IBMX (5 μM)

Effects of ent -Kaurene diterpenes from Rabdosia excisa on the cardiac function of guinea pigs

The medicinal plant Rabdosia excisa in the Lamiaceae family is found in Northeastern China and is used to treat a fever due to a cold, mastitis, arthralgia, and bruises[1]. A previous study reported that an aqueous extract from that plant yielded ent -kaurene diterpenes with antitumor action. In addition, diterpenes have been used to synthesize analogs in relatively large quantities, and their structureactivity relationship in terms of cytotoxic activity[2] and inhibition of the activation of the intracellular transcription factor NF-κB[3] has been examined. Various studies have also examined ent -kaurene diterpenes[4] ― [7]. Three diterpenes―kamebakaurin (1), kamebanin (2), and excisanin A (3)―can be obtained in relatively large quantities from R. excisa . The current study examined the effects of those diterpenes on cardiac function in guinea pigs. Some of those findings are reported here

Synthesis and cytotoxicity evaluation of fluorinated brusatol, bruceosin, and dehydrobrusatol

Three fluorinated quassinoid analogues—4α-fluorobruceosin, 1α-fluorobrusatol, and 1-fluorodehydrobrusatol—were synthesized from brusatol, bruceosin, and dehydrobrusatol, respectively, by treatment with Selectfluor. These analogues were less cytotoxic to HL-60 cells than their non-fluorinated counterparts