Effect of ursolic acid, a triterpenoid antioxidant, on ultraviolet-B radiation-induced cytotoxicity, lipid peroxidation and DNA damage in human lymphocytes

Samivel, Ramachandran; Prasad, Nagarajan Rajendra

doi:10.1016/j.cbi.2008.08.010

Cited by 119 publications

(70 citation statements)

References 65 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Pre-treatment with ursolic acid increases the activities of antioxidant enzymes such as superoxide dismutase, catalase and glutathione peroxidase in UVB-irradiated lymphocytes (Ramachandran & Rajendra, 2008). Similar result, was also reported in HaCaT cells, and correlated with an increase in glutathione levels (Hitoshi et al, 2008).…”

Section: Discussionsupporting

confidence: 65%

Apoptosis-Induced Cell Death due to Oleanolic Acid in HaCaT Keratinocyte Cells -a Proof-of-Principle Approach for Chemopreventive Drug Development

George¹,

Ragupathi²,

Suresh³

et al. 2012

Asian Pacific Journal of Cancer Prevention

View full text Add to dashboard Cite

Oleanolic acid (OA) is a naturally occurring triterpenoid in food materials and is a component of the leaves and roots of Olea europaea, Viscum album L., Aralia chinensis L. and more than 120 other plant species. There are several reports validating its antitumor activity against different cancer cells apart from its hepatoprotective activity. However, antitumor activity against skin cancer has not beed studied well thus far. Hence the present study of effects of OA against HaCaT (immortalized keratinocyte) cells -a cell-based epithelial model system for toxicity/ethnopharmacology-based studies -was conducted. Radical scavenging activity (DPPH•) and FRAP were determined spectrophotometrically. Proliferation was assessed by XTT assay at 24, 48 and 72 hrs with exposure to various concentrations (12.5-200 µM) of OA. Apoptotic induction potential of OA was demonstrated using a cellular DNA fragmentation ELISA method. Morphological studies were also carried out to elucidate its antitumor potential. The results revealed that OA induces apoptosis by altering cellular morphology as well as DNA integrity in HaCaT cells in a dose-dependent manner, with comparatively low cytotoxicity. The moderate toxicity observed in HaCaT cells, with induction of apoptosis, possibly suggests greater involvement of programmed-cell death-mediated mechanisms. We conclude that OA has relatively low toxicity and has the potential to induce apoptosis in HaCaT cells and hence provides a substantial and sound scientific basis for further validation studies.

show abstract

Section: Discussionsupporting

confidence: 65%

Apoptosis-Induced Cell Death due to Oleanolic Acid in HaCaT Keratinocyte Cells -a Proof-of-Principle Approach for Chemopreventive Drug Development

George¹,

Ragupathi²,

Suresh³

et al. 2012

Asian Pacific Journal of Cancer Prevention

View full text Add to dashboard Cite

show abstract

“…Ma et al (22) suggested that ursolic acid protects against CCl 4 -induced oxidative stress and inflammation of the liver in mice. Ramachandran et al (23) concluded that ursolic acid protects against exposure to ultraviolet B-induced reactive oxygen species through modulation of antioxidants (23). The present results indicated that the protective effect of ursolic acid on I/R-IAKI is correlated with the modulation of oxidative stress.…”

Section: Discussionsupporting

confidence: 52%

Renoprotective effects of ursolic acid on ischemia/reperfusion-induced acute kidney injury through oxidative stress, inflammation and the inhibition of STAT3 and NF-κB activities

Peng

Ren

Lan

et al. 2016

Molecular Medicine Reports

View full text Add to dashboard Cite

Abstract. Ursolic acid, a pentacyclic triterpene compound with low toxicity and easy availability, has a variety of biological activities, including antitumor, antioxidant, antihepatitis, anti-inflammatory and antibacterial effects. The present study aimed to investigate the renoprotective effects of ursolic acid on ischemia/reperfusion-induced acute kidney injury (I/R-IAKI) in rats associated with its antioxidant and anti-inflammatory effects, as well as interference with the signal transducer and activator of transcription (STAT)3/nuclear factor (NF)-κB signaling pathway. The present study demonstrated that pre-treatment with ursolic acid significantly increased renal functioning and attenuated increases of serum angiotensin II levels in rats subjected to I/R-IAKI. In addition, I/R-IAKI-induced inflammation and oxidative stress were significantly reduced by pre-treatment with ursolic acid. Furthermore, ursolic acid significantly suppressed the upregulation of STAT3, NF-κB and caspase-3 activities in rats following I/R-IAKI. These results indicated that ursolic acid may be a potential drug for reducing I/R-IAKI through suppression of inflammation and oxidative stress damage, as well as modulation of STAT3 and NF-κB activities.

show abstract

“…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.

View full text Add to dashboard Cite

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

Effect of ursolic acid, a triterpenoid antioxidant, on ultraviolet-B radiation-induced cytotoxicity, lipid peroxidation and DNA damage in human lymphocytes

Cited by 119 publications

References 65 publications

Apoptosis-Induced Cell Death due to Oleanolic Acid in HaCaT Keratinocyte Cells -a Proof-of-Principle Approach for Chemopreventive Drug Development

Apoptosis-Induced Cell Death due to Oleanolic Acid in HaCaT Keratinocyte Cells -a Proof-of-Principle Approach for Chemopreventive Drug Development

Renoprotective effects of ursolic acid on ischemia/reperfusion-induced acute kidney injury through oxidative stress, inflammation and the inhibition of STAT3 and NF-κB activities

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

Contact Info

Product

Resources

About