Pentacyclic triterpenes of the lupane, oleanane and ursane group as tools in cancer therapy.
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.read more
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Design, Synthesis and Biological Evaluation of Pentacyclic Triterpene Derivatives: Optimization of Anti-ABL Kinase Activity.
Halil I. Ciftci,Mohamed O. Radwan,Safiye Emirdağ Öztürk,N. Gokce Ulusoy,Ece Sozer,Doha El-Sayed Ellakwa,Doha El-Sayed Ellakwa,Zeynep Ocak,Mustafa Can,Mustafa Can,Taha F.S. Ali,Taha F.S. Ali,Howaida I. Abd-Alla,Nurettin Yayli,Hiroshi Tateishi,Masami Otsuka,Mikako Fujita +16 more
TL;DR: The design and derivatizations resulted in enhancing the activity against ABL1 kinase and CML cells, and three promising compounds PT5, GP2 and GP5 were shown to inhibit extracellular signal-regulated kinase downstream signaling, and induce apoptosis in K562 cells.
Journal ArticleDOI
Topical treatment of necrotising herpes zoster with betulin from birch bark.
TL;DR: The successful treatment with betulin emulsion of a severe necrotising herpes zoster in an immunosuppressed patient who had not responded to a conventional topical treatment is reported.
Journal ArticleDOI
Olean-12-eno[2,3-c] [1,2,5]oxadiazol-28-oic acid (OEOA) induces G1 cell cycle arrest and differentiation in human leukemia cell lines.
TL;DR: OEOA significantly reduces cell proliferation without inducing cell death in three types of leukemia cell lines, including K562, HEL and Jurket, and is identified as a novel chemical entity for further development as therapeutics against leukemia.
Journal ArticleDOI
Synthesis and biological evaluation of pentacyclic triterpenoid derivatives as potential novel antibacterial agents.
Panpan Wu,Tu Borong,Liang Jinfeng,Shengzhu Guo,Nana Cao,Chen Silin,Zhujun Luo,Li Jiahao,Wende Zheng,Xiaowen Tang,Dongli Li,Xue-Tao Xu,Wenfeng Liu,Xi Zheng,Zhaojun Sheng,Adam P. Roberts,Kun Zhang,Kun Zhang,Weiqian David Hong,Weiqian David Hong +19 more
TL;DR: A series of ursolic acid (UA), oleanolic acid and 18β-glycyrrhetinic acid (GA) derivatives were synthesized by introducing a range of substituted aromatic side-chains at the C-2 position after the hydroxyl group at C-3 position was oxidized as mentioned in this paper.
Journal ArticleDOI
Xanthones, biflavanones and triterpenes from Pentadesma grandifolia (Clusiaceae): structural determination and bioactivity.
Grace Leontine Nwabouloun Djoufack,Karin M. Valant-Vetschera,Johann Schinnerl,Lothar Brecker,Eberhard Lorbeer,Wolfgang Robien +5 more
TL;DR: Structures were determined by NMR and mass spectrometry, as well as by 13C-NMR CSEARCH and SPECINFO database systems and the triterpenes lupeol, ß-amyrin and betulin were also encountered.
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