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Ursolic Acid: A Pentacyclic Triterpene from Plants in Nanomedicine
Published in Mahfoozur Rahman, Sarwar Beg, Mazin A. Zamzami, Hani Choudhry, Aftab Ahmad, Khalid S. Alharbi, Biomarkers as Targeted Herbal Drug Discovery, 2022
Monalisha Sen Gupta, Md. Adil Shaharyar, Mahfoozur Rahman, Kumar Anand, Imran Kazmi, Muhammad Afzal, Sanmoy Karmakar
Ursolic acid (UA) is a naturally derived pentacyclic triterpenoid, an important bioactive phytochemical. Ursolic acid is the most promising member of the triternenoid groups. Depending upon the quantities of different structural isoprene units, families of triterpenoids are classified. By squalene cyclization, these triterpenoids are synthesized which generally found in natural sources like many plants and fruits (Jager et al., 2009). Roots of Catharanthus trichophyllus, leaves of Plumeria obtuse, Eriobotrya japonica, and Rosmarinus officinalis, etc., are some source of UA (Shanmugam et al., 2013). Pentacyclic triterpenes, exhibit numerous biological functions due to the presence of different functional groups. It also possesses activity like cytotoxicity on different cancer cell lines. Having many potential benefits, some physical limitations restrict the oral and systemic delivery of UA (Jeong et al., 2007; Jager et al., 2008; Yin et al., 2012). To increase the solubility and to improve the bioactivity of UA, formulations like liposomes, nanoemulsions, nanoparticles (polymeric, solid, and metallic, among others) and cyclodextrin drug complexes, among other systems try to develop successfully (Jager et al., 2015; Xie et al., 2016; Li et al., 2015). The main focus of this chapter will be different evaluation techniques (in-vitro and in-vivo) regarding the antitumor effects of pentacyclic triternene, i.e., UA. Not only that, but the contribution of nanotechnology to facilitate the effective delivery of UA will be also concerned.
Chemopreventive Agents
Published in David E. Thurston, Ilona Pysz, 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.
An Alternative Approach for Anti-Alzheimer’s Compounds from Plant Extracts
Published in Atanu Bhattacharjee, Akula Ramakrishna, Magisetty Obulesu, Phytomedicine and Alzheimer’s Disease, 2020
G. K. Pratap, Manjula Shantaram
Triterpenoids are the most important group of terpenoids as they exhibit a wide diversity of biological activities and they are the major constituents in many medicinal plant decoctions and extracts. Some new plant bioactive compounds have been identified from traditional medicines, leading to the isolation of numerous triterpenoids with important pharmacological properties and activities (Jainendra et al., 2018). Triterpenoids are widespread in nature and can be found in vegetables, fruits, cereals, ferns, fungi, monocotyledonous and dicotyledonous plants, animals, and marine organisms. The higher plants are the major source of biologically active triterpenoids, with numerous reports showing that the Rhamnaceae, Cucurbitaceae and Apocynaceae plant families and the fungal Ganodermataceae family produce a wide variety of tetracyclic triterpenoids (Bishayee et al., 2011).The acidic function and -OH (hydroxyl) groups of the triterpenoids cannot interact with the stationary phase, as the two groups are located on the opposite sides of the compound (Parmar et al., 2013). The triterpenoid compounds found in the oleane family are erythrodiol, oleanolic acid, and β-amyrinandin, whereas those in the ursane family include uvaol and ursolic acid, with the lupane family including lupeol, betulinic acid, and botulin (Dzubak et al., 2005; Han and Bakovic, 2015; Battineni et al., 2018).
Lucialdehyde B suppresses proliferation and induces mitochondria-dependent apoptosis in nasopharyngeal carcinoma CNE2 cells
Published in Pharmaceutical Biology, 2023
Lingxue Liu, Zhangning Yu, Jing Chen, Benchen Liu, Changhui Wu, Ye Li, Jianhua Xu, Peng Li
Triterpenoids, a class of terpenoids, play an important role in the bioactivity of G. lucidum. To date, more than 150 triterpenoids have been identified from the fruiting bodies, spores, and mycelia of G. lucidum (Zhao et al. 2016). The antiproliferative effects of G. lucidum triterpenoids have been demonstrated in various human tumor cells such as leukemia, bladder cancer, breast cancer, cervical cancer, colorectal cancer, gastric cancer, and hepatoblastoma cells (Liang et al. 2019). G. lucidum triterpenoids also showed inhibitory effects on nasopharyngeal carcinoma. CNE1 and CNE2 are two nasopharyngeal carcinoma cell lines with distinct degrees of differentiation, which are often used in the research of nasopharyngeal carcinoma. CNE1 is a highly differentiated human nasopharyngeal carcinoma cell line, and CNE2 is a poorly differentiated human nasopharyngeal carcinoma cell line (Chen et al. 2019). In the present study, LB, a triterpenoid from G. lucidum, inhibited the nasopharyngeal carcinoma CNE2 cells in a dose- and time-dependent manner as detected using the MTT assay. Subsequently, the CFSE and colony formation assays further confirmed that LB had an antiproliferation effect on nasopharyngeal carcinoma CNE2 cells. In contrast, LB showed weak inhibitory activity against CNE1 cells.
Evaluation of immunological adjuvant activities of saponin rich fraction from the fruits of Asparagus adscendens Roxb. with less adverse reactions
Published in Drug and Chemical Toxicology, 2023
Rahul Singh, Rinku Sharma, Rajat Varshney, Gorakh Mal, Mayukh Ghosh, Birbal Singh
Asparagus adscendens Roxb. (AA) (family: Asparagaceae) commonly known as ‘Shatavari’ is frequently found in India and Pakistan (Mannan et al. 2015). It consists of triterpenoids, saponins, steroids, aliphatic, nitrogenous, and phenolic compounds. Asparagus genus has been attributed to have various pharmacological properties including anti-inflammatory, antitussive, antimicrobial, immunomodulatory, hepatoprotective, antistress, and antiulcer activities (Singh and Geetanjali 2016). However, so far there is no published information available about the safe use of SRF extracted from the fruits of Asparagus adscendens Roxb. (AA-SRF) as a potential adjuvant. Therefore, in vitro hemolytic and cytotoxicity, in vivo toxicity and adjuvant potential of the AA-SRF in Swiss albino mice have been evaluated for the first time in the present study.
An updated patent review of Nrf2 activators (2020-present)
Published in Expert Opinion on Therapeutic Patents, 2023
Ziquan Zhao, Ruitian Dong, Keni Cui, Qidong You, Zhengyu Jiang
In order to alleviate adverse side effects and improve pharmacological action in clinical application, a number of researchers have performed several structural modifications on triterpenoid derivatives during the past 3 years. Based on CDDO-Me, Zhou et al. [99] designed a series of Cathepsin B (CTSB)-sensitive prodrugs by connecting CTSB linkers to the α-cyano-α,β-unsaturated ketone moiety with the installation of polyethylene glycol (PEG) groups. These novel prodrugs could be circulated stably and converted to the active compound CDDO-Me in lysosomes by CTSB. Among all prodrugs, prodrug 7 (Figure 4) exhibited the best activity to suppress the release of nitric oxide (NO) in RAW264.7 cells, activate the Nrf2-ARE pathway, and inhibit the NF-κB pathway in HEK293T cells, which were comparable to that of CDDO-Me. Most significantly, prodrug 7 was much safer than CDDO-Me as manifested in relatively low cytotoxicity and human ether-a-go-go-related gene (hERG) inhibitory activity [99].