Protective effect of ursolic acid on ethanol-mediated experimental liver damage in rats

Saravanan, R.; Viswanathan, P. N.; Pugalendi, Kodukkur Viswanathan

doi:10.1016/j.lfs.2005.05.060

Cited by 165 publications

(102 citation statements)

References 29 publications

(23 reference statements)

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“…The present study showed a significant increase in the bilirubin levels of CCl 4 -injected rats, which is in accordance with the findings of previous studies (19,34,35). This hyper-bilirubinemia may be caused by the inhibition of the conjugation reaction and also the release of unconjugated bilirubin from injured and dead hepatocytes (33).…”

Section: Discussionsupporting

confidence: 93%

“…Bilirubin is a product of the chemical breakdown of hemoglobin that increases water solubility in hepatocytes in conjugation with glucuronic acid (33). The present study showed a significant increase in the bilirubin levels of CCl 4 -injected rats, which is in accordance with the findings of previous studies (19,34,35).…”

Section: Discussionsupporting

confidence: 93%

“…Studies have shown that liver toxicity decreases serum albumin levels (37). The results of the present study are in agreement with this finding and demonstrate the decreased functional ability of CCl 4 -injected rat livers (33). Decreased serum TP and albumin levels have been reported in CCl 4 -administered rats (38).…”

Section: Discussionsupporting

confidence: 91%

See 2 more Smart Citations

Hepatoprotective Effects of Arbutin against Liver Damage Induced by Carbon Tetrachloride in Rats

Mirshahvalad

Feizi

Barkhordar

et al. 2016

Jundishapur J Nat Pharm Prod

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Section: Discussionsupporting

confidence: 93%

Section: Discussionsupporting

confidence: 93%

See 1 more Smart Citation

Hepatoprotective Effects of Arbutin against Liver Damage Induced by Carbon Tetrachloride in Rats

Mirshahvalad

Feizi

Barkhordar

et al. 2016

Jundishapur J Nat Pharm Prod

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“…Ursolic acid and its isomer, oleanolic acid, are triterpenoid compounds found across the vegetal kingdom that have anti-inflammatory, anti-arthritic, cytostatic, antiproliferative, and hepato-protective effects in mice, as well as membrane stabilizing properties [161][162][163].…”

Section: Plant-derived Agents With Anti-glycation Activity 239mentioning

confidence: 99%

Plant-Derived Agents with Anti-Glycation Activity

Odjakova¹,

Popova²,

Sharif³

et al. 2012

Glycosylation

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“…Ursolic acid (38-hydroxy-urs-12-en-28-oic acid), shown in Figure 1, is a naturally occurring pentacyclic triterpenoid compound that possesses important pharmacological properties including hepatoprotective (Saravanan, Viswanathan, Pugalendi, 2006), antioxidant (Ramachandran, Prasad, 2008), immunomodulatory (Raphael, Kuttan, 2003), antiglycative (Wang et al, 2010), vasorelaxant (Aguirre-Crespo et al, 2006 and antimutagenic (Resende et al, 2006) functions. Furthermore, ursolic acid is a potential candidate for the treatment of Chagas disease due to its activity against Trypanosoma cruzi (Cunha et al, 2006;Ferreira et al, 2010).…”

Section: Introductionmentioning

confidence: 99%

Preparation, characterization and evaluation of the in vivo trypanocidal activity of ursolic acid-loaded solid dispersion with poloxamer 407 and sodium caprate

Eloy

Saraiva

Albuquerque

et al. 2015

Braz. J. Pharm. Sci.

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Ursolic acid is a promising candidate for treatment of Chagas disease; however it has low aqueous solubility and intestinal absorption, which are both limiting factors for bioavailability. Among the strategies to enhance the solubility and dissolution of lipophilic drugs, solid dispersions are growing in popularity. In this study, we employed a mixture of the surfactants poloxamer 407 with sodium caprate to produce a solid dispersion containing ursolic acid aimed at enhancing both drug dissolution and in vivo trypanocidal activity. Compared to the physical mixture, the solid dispersion presented higher bulk density and smaller particle size. Fourier Transform Infrared Spectroscopy results showed hydrogen bonding intermolecular interactions between drug and poloxamer 407. X-ray diffractometry experiments revealed the conversion of the drug from its crystalline form to a more soluble amorphous structure. Consequently, the solubility of ursolic acid in the solid dispersion was increased and the drug dissolved in a fast and complete manner. Taken together with the oral absorption-enhancing property of sodium caprate, these results explained the increase of the in vivo trypanocidal activity of ursolic acid in solid dispersion, which also proved to be safe by cytotoxicity evaluation using the LLC-MK2 cell line. O ácido ursólico é um candidato promissor para o tratamento da doença de Chagas, contudo este fármaco possui baixa solubilidade aquosa e limitada absorção intestinal, ambos os fatores limitantes da biodisponibilidade. Entre as estratégias para potencializar a solubilidade e a dissolução de fármacos lipofílicos, as dispersões sólidas estão crescendo em popularidade. Neste estudo, empregamos mistura dos tensoativos, poloxamer 407 e caprato de sódio, para produzir dispersão sólida contendo ácido ursólico, com o objetivo de aumentar tanto a dissolução do fármaco quanto a atividade tripanocida in vivo. Comparada à mistura física, a dispersão sólida apresentou maior densidade e menor tamanho de partícula. Os resultados da análise de espectroscopia no infravermelho com transformada de Fourier mostraram interações intermoleculares do tipo ligações de hidrogênio entre o fármaco e o poloxamer 407. Os experimentos de difratometria de raio-X revelaram a conversão do fármaco de sua forma cristalina para a forma amorfa, mais solúvel. Consequentemente, a solubilidade do ácido ursólico em dispersão sólida foi aumentada e o fármaco dissolveu-se de maneira mais rápida e completa. Em conjunto com as propriedades promotoras de absorção oral do caprato de sódio, estes resultados explicaram o aumento da atividade tripanocida in vivo do ácido ursólico em dispersão sólida, que também se provou segura após avaliação de citotoxicidade empregando a linhagem celular LLC-MK2.Unitermos: Ácido ursólico/atividade tripanocida. Doença de Chagas/tratamento. Tensoativos. Dispersões sólidas/dissolução. Poloxamer 407. Caproato de sódio.

show abstract

Protective effect of ursolic acid on ethanol-mediated experimental liver damage in rats

Cited by 165 publications

References 29 publications

Hepatoprotective Effects of Arbutin against Liver Damage Induced by Carbon Tetrachloride in Rats

Hepatoprotective Effects of Arbutin against Liver Damage Induced by Carbon Tetrachloride in Rats

Plant-Derived Agents with Anti-Glycation Activity

Preparation, characterization and evaluation of the in vivo trypanocidal activity of ursolic acid-loaded solid dispersion with poloxamer 407 and sodium caprate

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