Betulinic Acid Inhibits Growth Factor‐induced in vitro Angiogenesis via the Modulation of Mitochondrial Function in Endothelial Cells

Kwon, Ho Jeong; Shim, Joong Sup; Kim, Jin Hee; Cho, Hyun Young; Yum, Young Na; Kim, Seung Hee; Yu, Jaehoon

doi:10.1111/j.1349-7006.2002.tb01273.x

Cited by 72 publications

(39 citation statements)

References 30 publications

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“…These processes lead to the release of mitochondrial apoptogenic factors, activation of caspases, and DNA fragmentation [5][6][7]. It was observed that betulinic acid inhibited the in vitro activity of aminopeptidase N [8], an endogenous angiogenic factor, but could not inhibit the enzyme in vivo even though it inhibits mitochondrial function in endothelial cells [9]. Betulinic acid, by an antioxidant mechanism tends to protect congenital melanocyte naevi cells from UV-C-induced DNA strand breakage independent of p53 and p21 [10].…”

Section: Introductionmentioning

confidence: 99%

Lupane Triterpenoids—Betulin and Betulinic acid derivatives induce apoptosis in tumor cells

et al. 2009

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In the present investigation the antiproliferative activity of thirteen derivatives of betulinic acid and betulin was tested against five different tumor cell lines. The toxicity against normal human fibroblasts (WWO70327) and the mode of cell death on HT-29 (colon cancer) as well as caspase activity induced by the most active compounds, 9 (3-O-chloroacetylbetulinic acid) and 15 (28-O-chloroacetylbetulin) were determined. Investigated derivatives exerted a dose dependent antiproliferative action at micromolar concentrations toward target tumor cell lines. Treatment of HT-29 cells for 24 h with 9 and 15 induced apoptosis, as observed by dye exclusion test (trypan blue) and confirmed by the appearance of a typical ladder pattern in the DNA fragmentation assay.

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Section: Introductionmentioning

confidence: 99%

Lupane Triterpenoids—Betulin and Betulinic acid derivatives induce apoptosis in tumor cells

et al. 2009

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“…88 Betulinic acid has also been shown to protect congenital melanocyte naevi cells from UV-C-induced DNA strand breakage independent of p53 and p21. 89 It was speculated that betulinic acid may be acting through an antioxidant mechanism.…”

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confidence: 98%

Chemistry, biological activity, and chemotherapeutic potential of betulinic acid for the prevention and treatment of cancer and HIV infection

Cichewicz

Kouzi

2003

Medicinal Research Reviews

479

220

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3beta-Hydroxy-lup-20(29)-en-28-oic acid (betulinic acid) is a pentacyclic lupane-type triterpene that is widely distributed throughout the plant kingdom. A variety of biological activities have been ascribed to betulinic acid including anti-inflammatory and in vitro antimalarial effects. However, betulinic acid is most highly regarded for its anti-HIV-1 activity and specific cytotoxicity against a variety of tumor cell lines. Interest in developing even more potent anti-HIV agents based on betulinic acid has led to the discovery of a host of highly active derivatives exhibiting greater potencies and better therapeutic indices than some current clinical anti-HIV agents. While its mechanism of action has not been fully determined, it has been shown that some betulinic acid analogs disrupt viral fusion to the cell in a post-binding step through interaction with the viral glycoprotein gp41 whereas others disrupt assembly and budding of the HIV-1 virus. With regard to its anticancer properties, betulinic acid was previously reported to exhibit selective cytotoxicity against several melanoma-derived cell lines. However, more recent work has demonstrated that betulinic acid is cytotoxic against other non-melanoma (neuroectodermal and malignant brain tumor) human tumor varieties. Betulinic acid appears to function by means of inducing apoptosis in cells irrespective of their p53 status. Because of its selective cytotoxicity against tumor cells and favorable therapeutic index, even at doses up to 500 mg/kg body weight, betulinic acid is a very promising new chemotherapeutic agent for the treatment of HIV infection and cancer.

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“…Reporter assay experiments were repeated three times and transfections performed in duplicate regimens. Ursolic and betulinic acids not only exhibit cytotoxic effect against endothelial cells, but also inhibits tube-like structure formation of aortic endothelial cells (Kwon et al, 2002;Mukherjee et al, 2004). In the present study treatment of OVCAR 432 cells with UABC increased the Sub-G1 cell population to 72.3%.…”

Section: Discussionmentioning

confidence: 52%

Ursolic acid benzaldehyde chalcone leads to inhibition of cell proliferation and arrests cycle in G1/G0 phase in ovarian cancer

Jia

Chen

et al. 2015

Bangladesh J Pharmacol

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<p>In the present study, the effect of ursolic acid benzaldehyde chalcone (UABC) on ovarian carcinoma cells was studied. The results revealed that ovarian carcinoma cells on UABC treatment increased Sub-G1 cell population, increased rate of cell apoptosis and morphological changes in mitochondrial membrane. In OVCAR 432 cells treatment with UABC increased the Sub-G1 cell population to 72.3% and growth inhibition rate of >72%. Treatment with 20 µM of UABC for 48 hours, led to an induction of apoptosis in 67.2% and induced morphological changes in OVCAR 432 cells. The Western blot results showed high concentration of cytochrome c in the cell cytosol after 48 hours of UABC treatment. Treatment of RMS-13 cells with UABC resulted in inhibition of GLI1, GLI2, PTCH1, and IGF2 genes. In addition, we found a significant reduction in hedgehog activity of RMS-13 cells after UABC treatment by means of a hedgehog-responsive reporter assay. Therefore, UABC can be a promising agent for the treatment of ovarian carcinoma.</p>

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Betulinic Acid Inhibits Growth Factor‐induced in vitro Angiogenesis via the Modulation of Mitochondrial Function in Endothelial Cells

Cited by 72 publications

References 30 publications

Lupane Triterpenoids—Betulin and Betulinic acid derivatives induce apoptosis in tumor cells

Lupane Triterpenoids—Betulin and Betulinic acid derivatives induce apoptosis in tumor cells

Chemistry, biological activity, and chemotherapeutic potential of betulinic acid for the prevention and treatment of cancer and HIV infection

Ursolic acid benzaldehyde chalcone leads to inhibition of cell proliferation and arrests cycle in G1/G0 phase in ovarian cancer

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