Chemopreventive Agents
David E. Thurston, Ilona Pysz in Chemistry and Pharmacology of Anticancer Drugs, 2021
Triterpenoids are a group of secondary plant metabolites comprised of 30 carbons (i.e., six isoprene units) which are widely abundant in the plant kingdom. Well-known examples of triterpenoids include oleanolic acid (Figure 12.30), ursolic acid, betulinic acid, and glycyrrhetinic acid, all of which have been reported to cause a diverse range of pharmacological effects, including NF-κB activation, mitochondrial dysfunction, the promotion of apoptosis, and the reduction of proliferation and angiogenesis. Structure of the triterpenoid oleanolic acid.
Development and Commercialization of Asiaticoside in Madagascar
Charles Wambebe in African Indigenous Medical Knowledge and Human Health, 2018
Meanwhile, Boiteau was able to contact Professor Albert Rakoto Ratsimamanga. This first physical meeting opened a new and promising avenue to Ratsimamanga for the investigation of medicinal plants and traditional medicine of Madagascar, and it is in this area that he gained his reputation. He did a successful and fruitful work on the pharmacology of C. asiatica, and published several papers with Boiteau about the progress of the work. Two review papers summarized the overall pharmacological work (Boiteau and Ratsimamanga, 1956; Ratsimamanga and Boiteau, 1964). One paper gave an overview on the physiological role of triterpenoids (Ratsimamanga and Boiteau, 1964). Boiteau then left the Muséum National d'Histoire Naturelle to work fully in Ratsimamanga's laboratory. Boiteau et al. (1964) wrote an excellent book on triterpenoids and their role in animal and plant physiology.
Medicinal Mushrooms
Anil K. Sharma, Raj K. Keservani, Surya Prakash Gautam in Herbal Product Development, 2020
The primary activities of triterpenoids include antioxidant, liver protection, improved atherogenic index, anti-inflammatory and inhibition of hista-mine release. Triterpenoids also play a complementary role with β-glucans in immunomodulatory activities (Wachtel-Galor et al., 2011). The mechanism of anticancer action by mushroom triterpenoids may include: inhibition of tumor cell growthinhibiting metastasisinhibiting angiogenesis (Petrovi´c et al., 2014; Xiao et al., 2009).
Boswellic acids: privileged structures to develop lead compounds for anticancer drug discovery
Published in Expert Opinion on Drug Discovery, 2021
Hidayat Hussain, Iftikhar Ali, Daijie Wang, Faruck L. Hakkim, Bernhard Westermann, Luay Rashan, Ishtiaq Ahmed, Ivan R. Green
Triterpenes having six isoprene units are quite widespread and are found in many natural sources dating from ancient times. It was later determined that these compounds are synthesized via a cascade cyclization of squalene in many plants. Furthermore, over 20,000 triterpenes have been reported from various natural sources and interestingly, most of them are found in their free form while others occur as triterpene glycosides (saponins) [1–4]. Additionally, triterpenes are widespread in various medicinal plants and in particular, in their resin, fruits, leaves, seeds, and bark of the specific herbs. Furthermore, on the basis of the number of isoprene units, triterpenoids can be classified as acyclic, mono-, bi-, tri-, tetra- and pentacyclic. On the other hand, among the triterpenoids, tetracyclic triterpenes (viz., dammaranes, protostanes, euphanes, and cycloartanes) and pentacyclic triterpenes (viz., ursanes, oleananes, gammaceranes, hopanes, and lupanes) are the most studied of the triterpenes [1–4].
Therapeutic targets and early stage clinical trials for pulmonary fibrosis
Published in Expert Opinion on Investigational Drugs, 2019
Seidai Sato, Toyoshi Yanagihara, Martin R. J. Kolb
Bardoxolone methyl (Reata Pharmaceuticals) is an orally bioavailable semi-synthetic triterpenoid, based on the scaffold of the natural product oleanolic acid. Bardoxolone methyl acts as an activator of the Nrf2 pathway and an inhibitor of the NF-κB pathway [71]. In a preclinical model, bardoxolone methyl reduced the histopathological score and the number of inflammatory cells and concentrations of total protein in BALF, suppressed secretion and expression of proinflammatory cytokines, including TGF-β and IL-6, elevated expression of the anti-inflammatory cytokine IL-10. It also downregulated the mRNA level of profibrotic genes, including fibronectin, α-smooth muscle actin, and collagen-I in the bleomycin- [72] and a radiation-induced lung injury mouse model [73]. In an ongoing Phase II study, the safety and efficacy of bardoxolone were evaluated in about 165 patients whose pulmonary hypertension is associated with several lung diseases including IPF and idiopathic interstitial pneumonia. The latest results covered eight patients with IPF who were treated with bardoxolone or a placebo. After 16 weeks of bardoxolone, the IPF patients were able to walk 38 m further than before treatment in an exercise-capacity assessment known as the 6-min walking distance test. In contrast, placebo-treated patients were able to walk 13 fewer meters [NCT02036970].
Lactoferrin-tethered betulinic acid nanoparticles promote rapid delivery and cell death in triple negative breast and laryngeal cancer cells
Published in Artificial Cells, Nanomedicine, and Biotechnology, 2020
Asim Halder, Megha Jethwa, Pritha Mukherjee, Subarna Ghosh, Suvadra Das, A. B. M. Helal Uddin, Arup Mukherjee, Urmi Chatterji, Partha Roy
Various naturally occurring triterpenoids are gaining importance for applications in complex medical conditions such as in cancer, HIV aids and auto-immune diseases [32]. BA is one such compound promoted by NIH for rapid access to cancer chemotherapy. BA depolarises mitochondrial membrane potential and induces caspase-independent apoptotic cell death. The drug exhibits a broader therapeutic window since its cytotoxicity does not affect the normal cells [14]. BA is a ROS scavenger in normal cells but facilitate excessive ROS generation in cancerous cells [33]. Also, BA is enormously useful in drug-resistant cancer cells since it triggers mitochondrial pathways of apoptosis. Entry of BA in cells is however very restricted. BA is classified as BCS class IV type compound due to poor water solubility and very low permeability. Delivery of this chemotherapeutic bioactive through surface engineered nanoparticle system is a very effective strategy. We have developed lactoferrin functionalized biopolymer nanoparticles loaded with BA for targeted delivery in cancer cell types.