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Open AccessJournal ArticleDOI

Pentacyclic triterpenes of the lupane, oleanane and ursane group as tools in cancer therapy.

Melanie N. Laszczyk
- 01 Dec 2009 - 
- Vol. 75, Iss: 15, pp 1549-1560
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TLDR
This review summarizes the potential of triterpenes belonging to the lupane, oleanane or ursane group, to treat cancer by different modes of action and utilisation of different plants as their sources is of interest.
Abstract
Today cancer treatment is not only a question of eliminating cancer cells by induction of cell death. New therapeutic strategies also include targeting the tumour microenvironment, avoiding angiogenesis, modulating the immune response or the chronic inflammation that is often associated with cancer. Furthermore, the induction of redifferentiation of dedifferentiated cancer cells is an interesting aspect in developing new therapy strategies. Plants provide a broad spectrum of potential drug substances for cancer therapy with multifaceted effects and targets. Pentacyclic triterpenes are one group of promising secondary plant metabolites. This review summarizes the potential of triterpenes belonging to the lupane, oleanane or ursane group, to treat cancer by different modes of action. Since Pisha et al. reported in 1995 that betulinic acid is a highly promising anticancer drug after inducing apoptosis in melanoma cell lines in vitro and in vivo, experimental work focused on the apoptosis inducing mechanisms of betulinic acid and other triterpenes. The antitumour effects were subsequently confirmed in a series of cancer cell lines from other origins, for example breast, colon, lung and neuroblastoma. In addition, in the last decade many studies have shown further effects that justify the expectation that triterpenes are useful to treat cancer by several modes of action. Thus, triterpene acids are known mainly for their antiangiogenic effects as well as their differentiation inducing effects. In particular, lupane-type triterpenes, such as betulin, betulinic acid and lupeol, display anti-inflammatory activities which often accompany immune modulation. Triterpene acids as well as triterpene monoalcohols and diols also show an antioxidative potential. The pharmacological potential of triterpenes of the lupane, oleanane or ursane type for cancer treatment seems high; although up to now no clinical trial has been published using these triterpenes in cancer therapy. They provide a multitarget potential for coping with new cancer strategies. Whether this is an effective approach for cancer treatment has to be proven. Because various triterpenes are an increasingly promising group of plant metabolites, the utilisation of different plants as their sources is of interest. Parts of plants, for example birch bark, rosemary leaves, apple peel and mistletoe shoots are rich in triterpenes and provide different triterpene compositions.

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Terpenoids as potential chemopreventive and therapeutic agents in liver cancer.

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Triterpenoids as potential agents for the chemoprevention and therapy of breast cancer.

TL;DR: In vitro and in vivo effects of these agents and related molecular mechanisms are presented and potential challenges and future directions involved in the advancement of these promising compounds in the prevention and therapy of human breast cancer are identified.
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Ursolic Acid—A Pentacyclic Triterpenoid with a Wide Spectrum of Pharmacological Activities

TL;DR: The current state of knowledge about the health-promoting properties of this widespread, biologically active compound, as well as information about its occurrence and biosynthesis are presented.
References
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Journal ArticleDOI

Betulinic acid: A new cytotoxic agent against malignant brain-tumor cells

TL;DR: Findings suggest that Bet A may be a promising new agent for the treatment of medulloblastomas and glioblastoma cells that clearly warrants further pre‐clinical and clinical evaluation.
Journal ArticleDOI

Betulinic Acid Suppresses Carcinogen-Induced NF-κB Activation Through Inhibition of IκBα Kinase and p65 Phosphorylation: Abrogation of Cyclooxygenase-2 and Matrix Metalloprotease-9

TL;DR: Results indicated that BA inhibits activation of NF-κB and NF-kkB-regulated gene expression induced by carcinogens and inflammatory stimuli, which may provide a molecular basis for the ability of BA to mediate apoptosis, suppress inflammation, and modulate the immune response.
Journal ArticleDOI

Investigations on the steroidal anti-inflammatory activity of triterpenoids from Diospyros leucomelas.

TL;DR: Three triterpenes were isolated from Diospyros leucomelas and identified as betulin, betulinic acid, and ursolic acid and showed anti-inflammatory activity in the carrageenan and serotonin paw edema tests and TPA and EPP ear edema Tests.
Journal ArticleDOI

Thematic review series: skin lipids. Peroxisome proliferator-activated receptors and liver X receptors in epidermal biology.

TL;DR: Because of their broad profile of beneficial effects on skin homeostasis, PPAR and LXR have great potential to serve as drug targets for common skin diseases such as psoriasis, atopic dermatitis, and skin cancer.
Journal ArticleDOI

Effects of Betulinic Acid Alone and in Combination with Irradiation in Human Melanoma Cells

TL;DR: The strictly additive mode of growth inhibition in combination with irradiation suggests that the two treatment modalities may function by inducing different cell death pathways or by affecting different target cell populations.
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