Bioassay-Guided Isolation of an Anti-Ulcer Compound, Tagitinin C, from Tithonia diversifolia: Role of Nitric Oxide, Prostaglandins and Sulfhydryls

Abstract

Tithonia diversifolia is a medicinal plant from the Municipality of Suchiapa, Chiapas, Mexico, that according to local folk medicine is considered useful in the treatment of gastric ulcers. The aim of the present study was to investigate the gastroprotective activity of T. diversifolia by using an ethanol-induced gastric ulcer experimental model in male Wistar rats. The results showed that T. diversifolia had gastroprotective activity, and that the dichloromethane extract had the highest protective activity (close to 90% when using doses between 10 to 100 mg/kg), and that further the compound tagitinin C isolated from this extract was the main active gastroprotective agent. Rats treated with tagitinin C suspended in Tween 80 at 1, 3, 10 and 30 mg/kg showed 37.7, 70.1, 100, and 100% gastroprotection, respectively. The effect elicited by tagitinin C (30 mg/kg) was not attenuated by pretreatment with either NG-nitro-L-arginine methyl ester (70 mg/kg, i.p.), a nitric oxide (NO) synthase inhibitor, N-ethylmaleimide (10 mg/kg, s.c.), a blocker of sulfhydryl groups, or indomethacin (10 mg/kg, s.c.), a blocker of prostaglandin synthesis, which suggests that the gastroprotective mechanism of action of this sesquiterpene lactone does not involve NO, sulfhydryl groups or prostaglandins.

The methanolic extract of Boesenbergia rotunda (L.) Mansf. and its major compound pinostrobin induces anti-ulcerogenic property in vivo: Possible involvement of indirect antioxidant action

“…In the digestive system, peptic ulcers denote one of the most critical diseases and a social as well as medical problem of global economic importance (Sánchez-Mendoza et al, 2011). The immediate cause of peptic ulcer is considered as the disturbance in the protection of stomach mucosa against gastric acid (Bucciarelli et al, 2010).…”

Anti-inflammatory sesquiterpene lactones from Tithonia diversifolia trigger different effects on human neutrophils

“…The tested STL from T. diversifolia usually exhibit expected biological activity because, in a general way, they are known for their key medicinal potential (Chagas-Paula et al, 2012; Ghantous et al, 2010). Among all compounds from T. diversifolia already tested for any biological activity, the STL Tag C (1) has been the most frequently studied (Liao et al, , 2013Chagas-Paula et al, 2012;Lin, 2012;Lee et al, 2011;Sánchez-Mendoza et al, 2011;Ghantous et al, 2010;Goffin et al, 2002). In the presence of LPS, all Tags were able to decrease the rate of neutrophil apoptosis.…”

“…Several biological activities have been described for most of these compounds (Liao et al, , 2013Chagas-Paula et al, 2011, 2012Lin, 2012;Zhao et al, 2012;Sánchez-Mendoza et al, 2011;Gu et al, 2002). The tested STL from T. diversifolia usually exhibit expected biological activity because, in a general way, they are known for their key medicinal potential (Chagas-Paula et al, 2012; Ghantous et al, 2010).…”

“…Although STL are plant-derived compounds with remarkable antiinflammatory and antitumor activity, they are usually known for their toxic properties (Chagas-Paula et al, 2011, 2012Merfort, 2011;Ghantous et al, 2010;Schmidt, 1999). Among all compounds from T. diversifolia already tested for biological activity, the tagitinins (Tags), STL, have shown relevant activity in diverse pathologic situations (Chagas-Paula et al, 2012;Gu et al, 2002;Liao et al, 2011;Sánchez-Mendoza et al, 2011;Zhao et al, 2012). At the molecular level, at least partially, the anti-inflammatory effect of STL can be explained by the inhibition of the activation of the nuclear factor-kappa B (NF-B) (Merfort, 2011;Siedle et al, 2004).…”

Effects of aqueous plant extracts and inorganic fertilizer on the germination, growth and development of maize (Zea mays L.)

“…In spite of its phytotoxic attributes, T. diversifolia presents several other uses including medicinal (Goffin et al, 2002;Bouberte et al, 2006;Sánchez-Mendoza et al, 2011) as well as agricultural ones. In effect, the green manure of T. diversifolia has been confirmed to be a good source of essential plant nutrients (Jama et al, 2000;Olabode et al, 2007;Partey, 2010).…”