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Herbal Drug Discovery Against Inflammation: From Traditional Wisdom to Modern Therapeutics
Published in Amit Baran Sharangi, K. V. Peter, Medicinal Plants, 2023
Shalini Dixit, Karuna Shanker, Madhumita Srivastava, Priyanka Maurya, Nupur Srivastava, Jyotshna, Dnyaneshwar U. Bawankule
Wide literature available throughout the world has now proven the uses of cloves in a toothache, headache, and respiratory disorders and in many more ailments. Oleanolic acid, one of the constituents of the cloves of Syzygium aromaticum is a triterpenoid known for its anti-inflammatory and anti-cancer properties (Lee et al., 2013).3-acetoxyoleanolic acid 3-acetoxy-28-methylester oleanolic acid was synthesized by oleanolic acid isolated from S. aromaticum was evaluated for their anti-inflammatory properties using the serotonin and fresh egg albumin-induced inflammatory test models in male Wistar rats weighing from 250 to 300 g (Figure 3.7). Significant results were obtained for semisynthetic analogs 3-acetoxyoleanolic acid and 3-acetoxy, 28-methylester. Oleanolic acid was found to exhibit anti-inflammatory properties in the albumin and serotonin-induced inflammatory test (Nkeh et al., 2015). In traditional Mexican medicine, Verbesina persicifolia, a medicinal plant commonly known as ‘huichin,’ has been used to treat a variety of diseases. One more compound, i.e., 4β-cinnamoyloxy, 1β, 3α-dihydroxyeudesm-7, 8-ene (1) and its derivates namely diacetate (2), hydrogenate (3) and diacetate hydrogenate (4) were synthesized in lab (Figure 3.8). Further, the anti-inflammatory effect was assayed by TPA-induced ear edema test. All derivatives exerts an anti-inflammatory effect significantly lower than that exerted by (1) (Via et al., 2015).
Anti-Proliferative Properties of Various South African Buddleja Species
Published in Namrita Lall, Medicinal Plants for Cosmetics, Health and Diseases, 2022
Oleanolic acid induces apoptosis in melanoma (A375) cells through upregulating the expression of pro-apoptotic proteins (p53, Bax and cytochrome c) and downregulating the anti-apoptotic protein Bcl-2 in a dose-dependent manner. It exhibited an IC50 of 40.7 µg/mL against A375 cells (Ghosh et al., 2014). Ursolic acid exhibited anti-proliferative activity in human melanoma cells (SK-MEL-2, IC50: 58.4 µg/mL) and induced apoptosis in A2058 melanoma cells. It has been reported that ursolic acid downregulates angiogenesis-promoting proteins such as vascular endothelial growth factor (VEGF). Anti-proliferative effects were also observed in A375 cells (IC50: 68.2 µg/mL) (Liu, 1995; Kashyap et al., 2016; Oprean et al., 2016; Caunii et al., 2017; Oprean et al., 2018).
Chemopreventive Agents
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
Oleanolic acid is a naturally occurring pentacyclic triterpenoid, widely distributed in plants where it is found as a free acid or an aglycone of triterpenoid saponins. Oleanolic acid is produced by wide range of medicinal herbs and other plants, for example, Calendula officinalis, Olea europaea, and Viscum album L, and is also found in olive oil. Similarly to other triterpenoids, oleanolic acid has been reported to exert several chemopreventive effects, although the mechanisms involved are not clear.
Synthesis and bioactivities evaluation of oleanolic acid oxime ester derivatives as α-glucosidase and α-amylase inhibitors
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Xu-Yang Deng, Jun-Jie Ke, Ying-Ying Zheng, Dong-Li Li, Kun Zhang, Xi Zheng, Jing-Ying Wu, Zhuang Xiong, Pan-Pan Wu, Xue-Tao Xu
Oleanolic acid (OA), one of the naturally occurring pentacyclic triterpenoid compounds, was widely found in plant-derived food and medicinal herbs10–14. OA and its derivatives possess different biological activities such as anti-inflammatory, anti-hyperglycaemic, anti-hyperlipidaemic, anti-oxidant and hepatoprotective1. The research found that the introduction of oxime-ester moiety into OA can improve its anti-tumour activity15, anti-inflammatory effect16, the inhibition of HIV-1 protease dimerisation and the inhibitory activity of glycogen phosphorylase compared with the parent compound17,18 and other activities, which was presumably associated with the enhancement of the hydrophilic performance19. Furthermore, our group has been dedicated to the structural modification and derivation of OA skeleton at the C2, C3, C12, C13, or C28 position, simultaneously the inhibition of α-glucosidase and its mechanism have been explored in depth20,21.
Oleanolic Acid Suppressed DMBA-Induced Liver Carcinogenesis through Induction of Mitochondrial-Mediated Apoptosis and Autophagy
Published in Nutrition and Cancer, 2021
Samar Hosny, Heba Sahyon, Magdy Youssef, Amr Negm
The limited conventional therapy of liver cancer are connected with high morbidity and mortality rate, suggesting imperative requests for introduction of novel efficient therapeutic drugs (7,8). Nutritional supplements of plant sources are currently being investigated for their use in the prevention and reversion of cancer progression (8). OA is a pentacyclic triterpenes with a wide spread occurrence throughout the plant kingdom. Oleanolic acid exists in olives (Olea europaea L.) and their products, as olive oil. It is estimated that the average daily intake of oleanolic acid in the Mediterranean diet, which includes olives and olive oils, is around 25 mg. Other foods such as various legumes that contain oleanolic acid are in the range of 0.251–2.591 µg/g fresh weight (9,10). High amounts of oleanolic acid are also present in edible parts of jujube (Ziziphus jujube Mill.) (11).
Influence of verapamil on the pharmacokinetics of rotundic acid in rats and its potential mechanism
Published in Pharmaceutical Biology, 2021
Haihua Shang, Ze Wang, Hong Ma, Yinghui Sun, Xiaoyan Ci, Yuan Gu, Changxiao Liu, Duanyun Si
Pentacyclic triterpene acids (PTAs) are generally considered to have low bioavailability due to the poor solubility and dissolution rate, low intestinal absorption, potential efflux transport, first-pass metabolism, etc. It has previously been reported (Lee et al. 2011; Zhang et al. 2018; Liu et al. 2019) that efflux pump P-glycoprotein (P-gp) and cytochrome P450 (CYP450) enzymes CYP3A located in the intestine and liver have the potential to affect the disposition of TCM and drug–drug interaction (DDI) in vivo. Therefore, in addition to their own physicochemical properties and pharmaceutical dosage form, CYP450 enzymes and efflux transporters play a major role in the assessment of bioavailability. For example, the bioavailability of glycyrrhizin in rats is 4.0% due to the poor mucosal permeability and first-pass elimination (Wang et al. 1994). With poor absorption, extensive metabolic clearance, and involvement of P-gp efflux transport, the absolute oral bioavailability of oleanolic acid in rats was 0.7% (Jeong et al. 2007; Yang et al. 2017). It was reported in a previous study that the oral bioavailability of RA was only 4.52% after oral administration in rats (Nan et al. 2016). However, to date, there is no information available regarding the metabolic stability and intestinal absorption characteristics of RA, and the reason for its poor bioavailability. We hypothesized the low oral bioavailability of RA is due to P-gp mediated drug efflux and/or CYP3A mediated metabolism of RA as the same as PTAs.