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Russelioside B: a Pregnane Glycoside with Pharmacological Potential.

ABSTRACT: Pregnanes and pregnane glycosides or their esters are well-studied secondary metabolites, many of them exhibit immunomodulator, anticancer, antidiabetic, antarthritic, antiulcer, anti-nociceptive, hypolipidemic, anti-inflammatory, and antibacterial properties. Pregnane glycosides are widely distributed in the families Apocyanaceae and Asclepiadaceae. Plant members of the genus Caralluma R.Br., Apocynaceae, are among the most studied species because of uses in traditional medicine or as food. They are a rich source of pregnane glycosides, as russelioside B. However, the bioactivity profile of this pregnane glycoside has not been reviewed until now. The present review aims to summarize the most important pharmacological and therapeutic applications of russelioside B with specific emphasis on the mechanism of actions associated with its administration in preclinical models. Russelioside B has many pharmacological effects including antidiabetic, anti-obesity, anti-nociceptive, antiulcer, anti-inflammatory, anti-arthritis effects, and antibiofilm, and wound healing activities. Despite its outstanding pharmacotherapeutic potential, russelioside B has never been tested in clinical trials. This review indicates that russelioside B is a potentially promising bioactive candidate, but further deeper mechanistic studies and clinical trials are needed in the future to elucidate its interaction with receptors of specific genes.

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Supplementary information

The online version contains supplementary material available at 10.1007/s43450-022-00245-x.

SUBMITTER: Abdel-Sattar E

PROVIDER: S-EPMC8941831 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature

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Russelioside B: a Pregnane Glycoside with Pharmacological Potential.

Abdel-Sattar Essam E Ali Dalia E DE

Revista brasileira de farmacognosia : orgao oficial da Sociedade Brasileira de Farmacognosia 20220323 2

Pregnanes and pregnane glycosides or their esters are well-studied secondary metabolites, many of them exhibit immunomodulator, anticancer, antidiabetic, antarthritic, antiulcer, anti-nociceptive, hypolipidemic, anti-inflammatory, and antibacterial properties. Pregnane glycosides are widely distributed in the families Apocyanaceae and Asclepiadaceae. Plant members of the genus <i>Caralluma</i> R.Br., Apocynaceae, are among the most studied species because of uses in traditional medicine or as fo ...[more]

PMID: 35345418

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Project description:Background and purpose: Russelioside B (RB) is a pregnane glycoside obtained from Caralluma quadrangula; a herb with antidiabetic, anti-inflammatory, and antihyperlipidemic activities. The present experiment tested the possible role of RB in controlling weight gain in rats fed on high fat (HF) diet. Methods: RB was separated from the n-butanol fraction of the crude methanolic extract by chromatographic separation on a Si gel column according to the procedures described previously. The experiment of the biological assessment of RB used 32 male Wistar rats (4 groups, n = 8). Group 1 rats were fed with a palatable normal diet. Group 2, 3, and 4 were fed on HF diet for 16 weeks. Group 2 served as the HF diet control group while Group 3 and 4 received daily oral doses of RB (25 and 50 mg/kg) during the last four weeks. Animals' parameters like weight gain, fasting level of blood sugar, serum lipids, and serum liver enzyme activities were measured. Liver or adipose tissue weight was divided by the rat's body weight and multiplied by 100 to obtain the liver or adipose tissue index, respectively. Adipose tissues were processed for histopathological examination, measurement of mRNA expression of visfatin, leptin, adiponectin, uncoupling protein-1 (UCP-1), and carnitine palmitoyl transferase-1 (CPT-1). Furthermore, serum levels of insulin, interleukin-6 (IL-6), IL-1β, tumor necrosis factor-α (TNF-α), leptin, resistin, and adiponectin were assessed using ELISA kits. Results: Rats fed with the HF diet exhibited significant body weight gain, abnormal liver function, disturbed lipid profile, and greater serum level of pro-inflammatory cytokines in addition to greater insulin resistance, adipose tissue and liver indices. Further, rats fed with the HF diet displayed upregulations in the expression of visfatin and leptin with downregulations in the expression of adiponectin, UCP-1, and CPT-1 compared to normal rats. Interestingly, RB (25 or 50 mg/kg) favorably modulated the measured parameters. Conclusion: Data from this study documented the beneficial role of RB in diminishing weight gain, improving the inflammatory perturbations and energy expenditure in HF diet fed rats. Therefore, RB might be a promising candidate for obesity.

Project description:Visceral leishmaniasis (VL) and post kala-azar dermal leishmaniasis (PKDL) affect most of the poor populations worldwide. The current treatment modalities include liposomal formulation or deoxycholate salt of amphotericin B, which has been associated with various complications and severe side effects. Encouraged from the recent marked antimalarial effects from plant-derived glycosides, in this study, we have exploited a green chemistry-based approach to chemically synthesize a library of diverse glycoside derivatives (Gly1-12) and evaluated their inhibitory efficacy against the AG83 strain of Leishmania donovani. Among the synthesized glycosides, the in vitro inhibitory activity of Glycoside-2 (Gly2) (1.13 µM IC50 value) on L. donovani promastigote demonstrated maximum cytotoxicity with ~94% promastigote death as compared to amphotericin B that was taken as a positive control. The antiproliferative effect of Gly2 on promastigote encouraged us to analyze the structure-activity relationship of Gly2 with Gp63, a zinc metalloprotease that majorly localizes at the surface of the promastigote and has a role in its development and multiplication. The result demonstrated the exceptional binding affinity of Gly2 toward the catalytic domain of Gp63. These data were thereafter validated through cellular thermal shift assay in a physiologically relevant cellular environment. Mechanistically, reduced multiplication of promastigotes on treatment with Gly2 induces the destabilization of redox homeostasis in promastigotes by enhancing reactive oxygen species (ROS), coupled with depolarization of the mitochondrial membrane. Additionally, Gly2 displayed strong lethal effects on infectivity and multiplication of amastigote inside the macrophage in the amastigote-macrophage infection model in vitro as compared to amphotericin B treatment. Gp63 is also known to bestow protection against complement-mediated lysis of parasites. Interestingly, Gly2 treatment enhances the complement-mediated lysis of L. donovani promastigotes in serum physiological conditions. In addition, Gly2 was found to be equally effective against the clinical promastigote forms of PKDL strain (IC50 value of 1.97 µM); hence, it could target both VL and PKDL simultaneously. Taken together, this study reports the serendipitous discovery of Gly2 with potent antileishmanial activity and proves to be a novel chemotherapeutic prototype against VL and PKDL.

Dataset Information

Russelioside B: a Pregnane Glycoside with Pharmacological Potential.

Graphical abstract

Supplementary information

Publications

Russelioside B: a Pregnane Glycoside with Pharmacological Potential.

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