Chemistry and Pharmacology of Guggulsterone: An Active Principle of Guggul Plant

Bhat, Musadiq Hussain; Fayaz, Mufida; Kumar, Amit; Jain, Ashok Kumar

doi:10.1007/978-3-030-04408-4_14

Cited by 5 publications

(5 citation statements)

References 72 publications

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“…Saxagliptin is a known substrate for CYP3A4 and the phytochemicals of GE might compete with this drug when given concomitantly. The primary active constituent of GE is guggulsterone E & Z (G E&Z) and the antidiabetic potential of these phytochemicals has already been reported in previous studies 37,38 . Hence, this phytochemical was predominantly chosen over others to dock with CYP3A4 alone and in combination with SAXA.…”

Section: Discussionmentioning

confidence: 76%

Indigenous Indian Guggul extract augments saxagliptin effect against diabetes-induced complications

Jain,

Sharma,

Chatterjee

et al. 2023

Preprint

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Type 2 Diabetes Mellitus is an endocrine metabolic disorder leading to impaired glucose utilization. This disease is managed by both commercial drugs and herbal products eliciting various interactions. The evaluation of one such interaction between saxagliptin (SAXA, substrate of CYP3A4), and guggul extract (GE) from Commiphora wightii is done in this present study. The concomitant administration of the SAXA with GE had restored otherwise increased blood glucose and biochemical parameters’ levels more effectively as compared to the solely consumed SAXA or GE. These results were corroborated by histopathological evaluation where the combination treatment showed better mitigation of hepatic, renal and pancreatic tissue damage that occurred due to induced diabetes. Furthermore, CYP3A11 mRNA (murine homolog to human CYP3A4) expression levels were observed to be reduced to non-diabetic levels in combination therapy which was otherwise unachievable. The molecular docking studies predicted improved interaction between CYP3A4 and bioactive content of GE, i.e., guggulsterone E-Z (G E&Z), possessing binding energy = -9.96 kcal/mol along with SAXA, confirming the co-existence of both the ligands at different binding sites of the metabolizing enzyme. The synergistic interactions of GE and SAXA helped in better restoration of tissue damage and CYP3A11 mRNA expression levels caused by induced diabetes.

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Section: Discussionmentioning

confidence: 76%

Indigenous Indian Guggul extract augments saxagliptin effect against diabetes-induced complications

Jain,

Sharma,

Chatterjee

et al. 2023

Preprint

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“…Lipid guggul extract (LGE) is reported for anti-in ammatory activity by ameliorating the levels of pro-in ammatory mediators such as IL-6, TNFα, IL-1β, NO, IL-12 and IFN-γ. E and Z-guggulsterones decrease the levels of pro-in ammatory cytokines like IL-1β, IL-2, TNF-α and suppresses cyclooxygenase-2 (COX-2) mRNA levels, thereby demonstrates antiin ammation and anti-arthritic activity [14,15]. Both the drugs are lipophilic in nature, hence delivering in the form of nanoemulsion can increase their e cacy and suppress side effects in the management of RA.…”

Section: Introductionmentioning

confidence: 99%

Development and preclinical assessment of nanoemulgel loaded with phytoconstituents for the management of rheumatoid arthritis

Chando,

Basudkar,

Gharat

et al. 2023

Drug Deliv. and Transl. Res.

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In recent years, natural ingredients have gained importance for therapeutic treatment due to their minimal toxicity. However, the delivery of these phytoconstituents poses a challenge to provide better e cacy. Current research reports the development of nanoemulgel (NEG) loaded with ginger oleoresin (GOR) and lipid guggul extract (LGE) for the management of rheumatoid arthritis (RA). The nanoemulsion (NE) was developed using the spontaneous emulsi cation technique by the pseudo-ternary method. The optimized nanoemulsion exhibited globule size of 16.08±2.55, PDI of 0.187±0.06 and Zeta Potential of-22.4±0.31.The cumulative release from in-vitro diffusion studies at pH 7.4 was about 99.72±3.47%, 57.98±2.11% and 86.42±5.13% of 6-gingerol, E-guggulsterone and Z-guggulsterone respectively at the end of 24 hours.The ex vivo studies on porcine ear skin showed sustained release with 92.8±3.21% for 6-gingerol, 55.61±0.91% for E-guggulsterone, and 84.2±4.22% for Z-guggulsterone released at the end of 24 hours. The cell culture studies on RAW 264.7 cells indicated a robust inhibition of LPS-induced IL-6 and TNF-α production indicating its e cacy in the management of RA. The Preclinical studies on male Wistar rats suggests that the developed NEG exhibited a comparable decrease in paw edema in ammation as compared to the marketed diclofenac sodium gel. These encouraging results demonstrates the potential of the developed nanoemulgel containing combination of GOR and LGE for the management of RA.

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“…GS (C 21 H 28 O 2 ) is a phytosteroid family of natural products, chemically classed as pregna-4,17-diene-3-16-dione. 66 It is a tetracyclic ring-fused molecule consisting of three numbers of six-membered cyclohexane rings (A, B, and C) and one five-membered cyclopentane ring (D); the basic structure is represented in Table 1. These rings (A–D) are constructed in a highly specific tetracyclic 17-carbon core that has a perhydrocyclopentano[ α ]phenanthrene orientation.…”

Section: Structure Of Guggulsteronementioning

confidence: 99%

Guggulsterone – a potent bioactive phytosteroid: synthesis, structural modification, and its improved bioactivities

Adarsh Krishna,

Ajeesh Krishna,

Edachery

et al. 2024

RSC Med. Chem.

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Chemistry and Pharmacology of Guggulsterone: An Active Principle of Guggul Plant

Cited by 5 publications

References 72 publications

Indigenous Indian Guggul extract augments saxagliptin effect against diabetes-induced complications

Indigenous Indian Guggul extract augments saxagliptin effect against diabetes-induced complications

Development and preclinical assessment of nanoemulgel loaded with phytoconstituents for the management of rheumatoid arthritis

Guggulsterone – a potent bioactive phytosteroid: synthesis, structural modification, and its improved bioactivities

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