Astragalin: A Bioactive Phytochemical with Potential Therapeutic Activities

Abstract

Natural products, an infinite treasure of bioactive chemical entities, persist as an inexhaustible resource for discovery of drugs. This review article intends to emphasize on one of the naturally occurring flavonoids, astragalin (kaempferol 3-glucoside), which is a bioactive constituent of various traditional medicinal plants such as Cuscuta chinensis. This multifaceted compound is well known for its diversified pharmacological applications such as anti-inflammatory, antioxidant, neuroprotective, cardioprotective, antiobesity, antiosteoporotic, anticancer, antiulcer, and antidiabetic properties. It carries out the aforementioned activities by the regulation and modulation of various molecular targets such as transcription factors (NF-κB, TNF-α, and TGF-β1), enzymes (iNOS, COX-2, PGE2, MMP-1, MMP-3, MIP-1α, COX-2, PGE-2, HK2, AChe, SOD, DRP-1, DDH, PLCγ1, and GPX), kinases (JNK, MAPK, Akt, ERK, SAPK, IκBα, PI3K, and PKCβ2), cell adhesion proteins (E-cadherin, vimentin PAR-2, and NCam), apoptotic and antiapoptotic proteins (Beclin-1, Bcl-2, Bax, Bcl-xL, cytochrome c, LC3A/B, caspase-3, caspase-9, procaspase-3, procaspase-8, and IgE), and inflammatory cytokines (SOCS-3, SOCS-5, IL-1β, IL-4, IL-6, IL-8, IL-13, MCP-1, CXCL-1, CXCL-2, and IFN-γ). Although researchers have reported multiple pharmacological applications of astragalin in various diseased conditions, further experimental investigations are still mandatory to fully understand its mechanism of action. It is contemplated that astragalin could be subjected to structural optimization to ameliorate its chemical accessibility, to optimize its absorption profiles, and to synthesize its more effective analogues which will ultimately lead towards potent drug candidates.

Polyphenol analysis using high‐resolution mass spectrometry allows differentiation of drought tolerant peanut genotypes

“…Isorhamnetin Many flavonols found in the present study have already been identified in peanuts. 10,30,31 Also, to the best of our knowledge, rhamnazin, a dimethoxylated derivative of quercetin reported to have potent antiangiogenic activity and antitumor efficacy, which can be found in Rhamus petiolaris, 32 and astragalin, a constituent of various traditional medicinal plants such as Cuscuta chinesis, described as displaying anti-inflammatory, antioxidant, anticancer, antidiabetic, anti-ulcer, anti-obesity, cardioprotective activities, neuroprotective effect and cosmetic use, 33 have been here identified for the first time in peanuts (Fig. 1G,H).…”

Optimization of Extraction Conditions of Phytochemical Compounds and Anti-Gout Activity of Euphorbia hirta L. (Ara Tanah) Using Response Surface Methodology and Liquid Chromatography-Mass Spectrometry (LC-MS) Analysis

“…Previous study also reported the presence of astragalin in other Euphorbia species [59]. As reviewed by Riaz et al [60], astragalin showed potent anti-inflammatory activity by inhibiting the production of inflammatory mediators such as interleukin-1 beta (IL-1β), interleukin-6 (IL-6), and tumor necrosis factor-alpha (TNF-α) in macrophages [61,62]. Moreover, Jia et al [63] demonstrated for the first time that astragalin effectively inhibited the worsening of synovial inflammation and joint destruction in the animal model.…”

LC/MS-QToF Profiling, Anti-Diabetic and Anti-Adipogenic potential of Divya MadhuKalp: A Novel Herbo-mineral Formulation

“…DMK contains Astragalin which is multifaceted compound regulating various molecular targets such as transcription factors, enzymes, kinases etc. with diversified pharmacological applications including anti-obesity and anti–diabetic properties 31 . The flavonoid rutin has anti– hyperglycemic property including decrease of carbohydrates absorption in small intestine, increase of tissue glucose uptake, stimulation of insulin secretion from beta cells, protecting Langerhans islet against degeneration and inhibition of tissue gluconeogenesis 32 .…”