Antidiabetic natural products

Kar, Amit; Banerjee, Subhadip; Katiyar, Chandra Kant

doi:10.1016/bs.armc.2020.06.002

Cited by 4 publications

(3 citation statements)

References 63 publications

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“…The α -glucosidase inhibition activity was investigated by a spectrophotometric method as previous researches [ 12 , 14 – 16 , 18 ]. Acarbose (Bayer Healthcare Co Ltd, Beijing, China) was utilized as a positive control and was dissolved in phosphate buffer (PB, 0.1 mM, pH = 6.8).…”

Section: Methodsmentioning

confidence: 99%

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Synthesis and biological evaluation of (20S,24R)-epoxy-dammarane-3β,12β,25-triol derivatives as α-glucosidase and PTP1B inhibitors

Yang

Geng

et al. 2022

Med Chem Res

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The dammarane triterpenoid (20 S ,24 R )-epoxy-dammarane-3 β ,12 β ,25-triol obtained from Cyclocarya paliurus in our previous study showed inhibitory activity on α -glucosidase in vitro with an inhibitory ratio of 32.2% at the concentration of 200 μM. In order to reveal the structure-activity relationships (SARs) and get more active compounds, 42 derivatives of (20 S ,24 R )-epoxy-dammarane-3 β ,12 β ,25-triol were synthesized by chemical modification on the hydroxyls (C-3 and C-12), rings A and E, and assayed for their α -glucosidase and PTP1B inhibitory activities. Two compounds ( 8 , 26 ) increased activity against α -glucosidase, and four compounds ( 8 , 15 , 26 , 42 ) significantly inhibited PTP1B. It was noted that compounds 8 and 26 could inhibit both α -glucosidase and PTP1B as dual-target inhibitors with IC 50 values of 489.8, 467.7 μM ( α -glucosidase) and 319.7, 269.1 μM (PTP1B). Compound 26 was revealed to be a mix-type inhibitor on α -glucosidase and a noncompetitive-type inhibitor on PTP1B based on enzyme kinetic study. Furthermore, compound 42 could selectively inhibited PTP1B as a mix-type inhibitor with IC 50 value of 134.9 μM, which was 2.5-fold higher than the positive control, suramin sodium (IC 50 339.0 μM), but not inhibit α -glucosidase.

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Section: Methodsmentioning

confidence: 99%

“…Natural products are rich sources for searching new antidiabetic agents [ 11 , 12 ], and the discovery of natural products and their derivatives as potential antidiabetic lead compounds are continuing goals of our laboratory [ 13 – 21 ]. The leaves of Cyclocarya paliurus were widely used to treat obesity and diabetes in China.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and biological evaluation of (20S,24R)-epoxy-dammarane-3β,12β,25-triol derivatives as α-glucosidase and PTP1B inhibitors

Yang

Geng

et al. 2022

Med Chem Res

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“…Diabetes is the familiar metabolic disorders where the counting of humans enduring from the disorder is escalating across the globe (GBD 2021 Diabetes Collaborators, 2023; Park & Jang, 2017), often associated with obesity, the condition can elevate the risk of diabetic kidney failure, cardiovascular disorder, retinal disease, and artery disease (Lazarus et al, 2023; Mukherjee et al, 2020). β‐sitosterol has also been extensively researched for its role in regulating cholesterol and blood glucose levels, numerous studies have demonstrated that β‐sitosterol effectively lowers LDL cholesterol by inhibiting its absorption in the intestines (Wu et al, 2022); moreover, it has been shown to improve glycemic control in diabetic patients by enhancing insulin sensitivity and reducing blood glucose levels (Prasad et al, 2022) These actions of β‐sitosterol highlight its multi‐faceted health benefits and its potential for use in the management of metabolic disorders.…”

Section: Other Pharmacological Properties Of β‐Sitosterolmentioning

confidence: 99%

Anticancer activity and other biomedical properties of β‐sitosterol: Bridging phytochemistry and current pharmacological evidence for future translational approaches

Nandi,

Nag,

Khatua

et al. 2023

Phytotherapy Research

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Sterols, including β‐sitosterol, are essential components of cellular membranes in both plant and animal cells. Despite being a major phytosterol in various plant materials, comprehensive scientific knowledge regarding the properties of β‐sitosterol and its potential applications is essential for scholarly pursuits and utilization purposes. β‐sitosterol shares similar chemical characteristics with cholesterol and exhibits several pharmacological activities without major toxicity. This study aims to bridge the gap between phytochemistry and current pharmacological evidence of β‐sitosterol, focusing on its anticancer activity and other biomedical properties. The goal is to provide a comprehensive understanding of β‐sitosterol's potential for future translational approaches. A thorough examination of the literature was conducted to gather relevant information on the biological properties of β‐sitosterol, particularly its anticancer therapeutic potential. Various databases were searched, including PubMed/MedLine, Scopus, Google Scholar, and Web of Science using appropriate keywords. Studies investigating the effects of β‐sitosterol on different types of cancer were analyzed, focusing on mechanisms of action, pharmacological screening, and chemosensitizing properties. Modern pharmacological screening studies have revealed the potential anticancer therapeutic properties of β‐sitosterol against various types of cancer, including leukemia, lung, stomach, breast, colon, ovarian, and prostate cancer. β‐sitosterol has demonstrated chemosensitizing effects on cancer cells, interfering with multiple cell signaling pathways involved in proliferation, cell cycle arrest, apoptosis, survival, metastasis invasion, angiogenesis, and inflammation. Structural derivatives of β‐sitosterol have also shown anti‐cancer effects. However, research in the field of drug delivery and the detailed mode of action of β‐sitosterol‐mediated anticancer activities remains limited. β‐sitosterol, as a non‐toxic compound with significant pharmacological potential, exhibits promising anticancer effects against various cancer types. Despite being relatively less potent than conventional cancer chemotherapeutics, β‐sitosterol holds potential as a safe and effective nutraceutical against cancer. Further comprehensive studies are recommended to explore the biological properties of β‐sitosterol, including its mode of action, and develop novel formulations for its potential use in cancer treatment. This review provides a foundation for future investigations and highlights the need for further research on β‐sitosterol as a potent superfood in combating cancer.

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The bioaccessibility, bioavailability, bioactivity, and prebiotic effects of phenolic compounds from raw and solid-fermented mulberry leaves during in vitro digestion and colonic fermentation

Zhao

Wang

et al. 2023

Food Research International

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Antidiabetic natural products

Cited by 4 publications

References 63 publications

Synthesis and biological evaluation of (20S,24R)-epoxy-dammarane-3β,12β,25-triol derivatives as α-glucosidase and PTP1B inhibitors

Synthesis and biological evaluation of (20S,24R)-epoxy-dammarane-3β,12β,25-triol derivatives as α-glucosidase and PTP1B inhibitors

Anticancer activity and other biomedical properties of β‐sitosterol: Bridging phytochemistry and current pharmacological evidence for future translational approaches

The bioaccessibility, bioavailability, bioactivity, and prebiotic effects of phenolic compounds from raw and solid-fermented mulberry leaves during in vitro digestion and colonic fermentation

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