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Role of Plant-Based Anti-HIV Agents in HIV-Associated Neurocognitive Disorders (Hand)
Published in Megh R. Goyal, Preeti Birwal, Santosh K. Mishra, Phytochemicals and Medicinal Plants in Food Design, 2022
Vishal K. Singh, Himani Chaurasia, Richa Mishra, Ritika Srivastava, Vivek K. Chaturvedi, Ramendra K. Singh
Celasdin B is extracted from Celastru shindsii and it has shown its bioactivity against HIV replication inside H9 cells [44]. Protostanes A and C (types of garcisa terpenes) can be extracted with ethyl acetate from stems and bark of Garcinia speciose and these can bottle up HIV-1 RTase activity [11]. Lanostane-type triterpene is a suberosol that can be obtained from leaves and stems of Polyalthia suberosa; and it has exhibited inhibitory activity on HIV replication in H9 cells. Triterpene lactone (lanci lactone C extracted from roots and stems of Kadsuralancilimba) may restrain HIV replication in veteran cells [50]. TPA (12-O-tetra-decanoylphorbol-13-acetate) is a phorboldi ester and is obtained with methanolic extract from Croton tiglium; and it shows inhibitory activity on cytopathogenic effects of HIV-1. Prostratin (phorbol ester, which is obtained from Homalanthus nutans) also exhibits anti-HIV properties.
Antidiabetic Potential of Medicinal Mushrooms
Published in Hafiz Ansar Rasul Suleria, Megh R. Goyal, Masood Sadiq Butt, Phytochemicals from Medicinal Plants, 2019
Vivek K. Chaturvedi, Sushil K. Dubey, M.P. Singh
β-Glucosidase enzyme secreted by the epithelium of small intestine converts disaccharides and oligosaccharides into glucose. A triterpenoid lanostane, called as ganoderol B [(3β, 24E)-lanosta-7, 9(11), 24-trien-3, 26-diol] isolated from G. lucidum, is a potent inhibitor of β-glucosidase enzyme.23 Since lanostane inhibits the activity of β glucosidase, it hinders the carbohydrate digestion and prevents absorption of glucose. The in-vitro study revealed that ganoderol B has high β-glucosidase inhibition rate with an IC50 of 48.5 μg/mL (119.8 μM).
Therapeutic Medicinal Mushroom (Ganoderma Lucidum): A Review of Bioactive Compounds and their Applications
Published in Megh R. Goyal, Durgesh Nandini Chauhan, Plant- and Marine-Based Phytochemicals for Human Health, 2018
Triterpenes are considered as one of the major group of compounds that contribute to the various bioactivities of G. lucidum.9, 64, 66, 159 These constitute a subclass of naturally occurring terpenes and usually have complex lanostane-based chemical structures that are highly oxidized.9, 64, 159 The triterpenes of G. lucidum include ganoderic acids (GAs) (A, AM1, B, C1, C2, D, DM, F, G, H, K, Me, Mk, S, T, TR, Y), ganoderenic acids (A, B, D), ganoderols (A, B), ganoderiol F, ganodermanontriol, ganoderal A, Me ganoderates (D, G), and lucideric acids.23, 58, 133, 159, 195 Among these, GAs are the most abundantly occurring triterpenes.9 These bitter tasting triterpenes consists of four cyclic and two linear isoprenes.64 GA-A and GA-B were the first triterpenes isolated from G. lucidum by Kubota et al. in 1982.159 Since then, the occurrence of more than 200 triterpenes has been reported from the spores, fruiting body, and mycelia of G. lucidum.9, 64, 66, 159, 162, 174, 183 Studies have shown that the spores have considerably higher GA contents than other parts.103, 166 Also, it has been found that with geographic distribution, the triterpene composition of G. lucidum fruiting body varies considerably.166
Semi-Purified Saponins of Holothuria poli Associated Antiproliferation in Tumor Cell Lines
Published in Nutrition and Cancer, 2022
Nazli Mert-Ozupek, Yasemin Basbinar, Tugba Uysal-Kilic, Omer Koz, Hulya Ellidokuz, Levent Cavas
TTGs, the secondary metabolites from sea cucumbers, have lots of bioactivity because of their unique chemical structural futures. Kalinin reported that since sea cucumber triterpene glycosides consist of two different units (glycone and aglycone), each part of these molecules show many bioactivities (9). Lanostane part of the molecule plays role on formation of complex with sterols and the membrane by creating hydrophilic structures. (9). Also, both 12α-hydroxyl and 17α-hydroxyl groups in TTGs cause hydrophilicity (9). 18(20)-lactone is of great importance on formation of membrane sterol complex (9). Actually, sea cucumber TTGs show this effect against cell membranes that contain Δ5 and Δ5,7 sterols. Also, they can tolerate their own toxins because of the presence of sulfated and glycosylated sterols, also their membrane lipids contain free Δ7 sterols with low levels (instead of Δ5 sterols) (19). The glycone parts of TTGs have formation and conservation property of the pores and channels (9). Xylose is the first monosaccharide that is linked to C-3 hydroxy group of the holostanol skeleton (26) and shows formation of channel, pores and lysis. Xylose-linked 4-O-sulfate group has little membranotropic activity (9). According to mass analysis, both H. tubulosa and H. poli have holothurin A and it has both 12α- and 17α-hydroxyl groups. This feature may increase the membranolytic activity and this could probably determine the biological activities, including antiproliferative activity.
Steroid sulfatase inhibitors: the current landscape
Published in Expert Opinion on Therapeutic Patents, 2021
Hanan S. Anbar, Zahraa Isa, Jana J. Elounais, Mariam A. Jameel, Joudi H. Zib, Aya M. Samer, Aya F. Jawad, Mohammed I. El-Gamal
Piptolinic acid D (21), pinicolic acid B (22), and ganoderol A (23) are natural lanostane triterpene compounds isolated from natural sources and reported as STS inhibitors. Compounds 21 and 22 are isolated from Fomitopsis pinicola Karst. (strain 442, voucher number: FompinE00442) [115] while compound 23 is isolated from Ganoderma lucidum Karst. (voucher number: 680,898). They were tested against STS enzyme and showed modest activity. The three compounds were tested at 20 µM concentration and exerted inhibition percentage values of 74%, 72%, and 62%, respectively. Their IC50 values in cell-free STS assay are 10.5, 12.4, and 15.7 µM, respectively. Reduction of the ketone group attached to ring A of compound 23 to secondary alcohol or oxidation of the terminal alcoholic group into aldehyde led to weaker inhibitory effect against STS (39% and 31% inhibition at 20 µM, respectively). Reduction of the ketone group attached to ring A in general in all the compounds led to weaker activity, so this carbonyl group seems essential for activity[116]. Further lead optimization and development of more potent semi-synthetic analogs of these three compounds maybe required to optimize the potency against STS.
Recent progress in the development of steroid sulphatase inhibitors – examples of the novel and most promising compounds from the last decade
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Mateusz Daśko, Sebastian Demkowicz, Karol Biernacki, Olga Ciupak, Witold Kozak, Maciej Masłyk, Janusz Rachon
Recently, Grienke et al.42 applied interesting in silico method to identify STS inhibitors from natural sources. According to the pharmacophore-based virtual screening of the Traditional Chinese Medicine (TCM) database, triterpenes based on the lanostane structure were taken into account as potential STS ligands. Evaluated compounds were isolated from traditionally used polypores, which are rich in lanostane derivatives. (i.e. Ganoderma lucidum Karst., Gleophyllum odoratum Imazeki, and Fomitopsis pinicola Karst). After sophisticated purification protocols, 3 out of 18 isolated lanostane analogues exhibited STS inhibitory activities (when evaluated in an assay with JEG-3 cells). Piptolinic acid D 10, Pinicolic acid B 11, and Ganadrol A 12 (Table 1) inhibited STS with IC50 values of 10.5, 12.4, and 15.7 µM, respectively. Despite the moderate STS inhibitory potency, authors indicated that reported compounds are the first STS inhibitors isolated from natural sources. Further application of in silico methods might be useful in the identification of more potent natural compounds demonstrating STS inhibitory properties.