Ursolic Acid is really a good compound. We still think the big issues with it are the solubility. And getting it complexed will improve it greatly. Just so you guys dont think I'm full of it....here is the research:
World J Gastroenterol. 2006 Feb 14;12(6):874-9.
Anti-hepatoma activity and mechanism of ursolic acid and its derivatives isolated from Aralia decaisneana.
Tian Z,
Lin G,
Zheng RX,
Huang F,
Yang MS,
Xiao PG.
Source
Department of Pharmacology, Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100094, China.
[email protected]
Abstract
AIM:
To investigate the anti-tumor activity of ursolic acid (UA) and its derivatives isolated from Aralia decaisneana on hepatocellular carcinoma both in vitro and in vivo.
METHODS:
In vivo cytotoxicity was first screened by 3-[4,5-dimethylthiazol-2-yl]-2, 5-diphenyltetrazolium bromide (MTT) assay. Morphological observation, DNA ladder, flow cytometry analysis, Western blot and real time PCR were employed to elucidate the cytotoxic mechanism of UA. Implanted mouse hepatoma H22 was used to evaluate the growth inhibitory effect of UA in vivo.
RESULTS:
UA could significantly inhibit the proliferation of HepG2 and its drug-resistance strain, R-HepG2 cells, but had no inhibitory effect on primarily cultured normal mouse hepatocytes whereas all the six derivatives of UA could not inhibit the growth of all tested cell lines. Further study on mechanism demonstrated that apoptosis and G0/G1 arrest were involved in the cytotoxicity and cleavage of poly-(ADP-ribose)-polymerase (PARP). Downregulation of cyclooxygenase-2 (COX-2) protein and upregulation of heat shock protein (HSP) 105 mRNA correlated to the apoptosis of HepG2 cells treated with UA. In addition, UA also could inhibit the growth of H22 hepatoma in vivo.
CONCLUSION:
UA is a promising anti-tumor agent, but further work needs to be done to improve its solubility.
PMID: 16521214 [PubMed - indexed for MEDLINE]
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AAPS PharmSciTech. 2009;10(4):1137-44. Epub 2009 Oct 16.
The influence of cosolvent on the complexation of HP-beta-cyclodextrins with oleanolic acid and ursolic acid.
Li R,
Quan P,
Liu DF,
Wei FD,
Zhang Q,
Xu QW.
Source
Department of Pharmaceutics, School of Pharmacy, Nanjing Medical University, 140 Hanzhong Road, 210029, Nanjing, People's Republic of China.
Abstract
The present work was aimed at the influence of ethanol on the complex formation of hydroxypropyl-beta-cyclodextrin (HP-beta-CD) with oleanolic acid (OA) and ursolic acid (UA), two insoluble isomeric triterpenic acids. Phase solubility studies were carried out to evaluate the solubilizing power of HP-beta-CD, in association with ethanol, toward OA and UA. A mathematical model was applied to explain and predict the solubility of OA and UA influenced by HP-beta-CD and ethanol. The solid complexes were prepared by evaporating the filtrate of samples which was prepared in different complexing media. The solubility of OA is much higher than that of UA in all the tested aqueous solutions. The solubility of OA
and UA can be increased over 900 and
200 times, respectively, by forming complex with HP-beta-CD. Ethanol (0.5%, v/v) can help the formation of OA-HP-beta-CD complex, but is harmful to the formation of UA-HP-beta-CD complex. Increasing solubility in water can be achieved by adding ethanol into the complexing media, but the concentration of ethanol should be optimized. The ring E of the chemical compounds has a great influence on the complexing process.
PMID: 19834815 [PubMed - indexed for MEDLINE] PMCID: PMC2799583
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