Abstract:Hispolon (HS), a
bioactive polyphenol, and its derivatives such
as hispolon monomethyl ether (HME), hispolon pyrazole (HP), and hispolon
monomethyl ether pyrazole (HMEP) were evaluated for comparative toxicity
and antigenotoxic effects. The stability of HS derivatives in biological
matrices followed the order HS < HP ≈ HME < HMEP. The
cytotoxicity analysis of HS derivatives indicated that HP and HMEP
were less toxic than HS and HME, respectively, in both normal and
tumor cell types. The mechanisms of toxicity … Show more
“…These reported data suggest the potential of hispolon as a potent multi-target anticancer drug. Chethna et al [ 51 ] reported that hispolon showed higher toxicity in three types of cancer cells (MCF7, A549, and CHO) than splenic lymphocytes at the same dose. From the results depicted in Figure 1 , the doses of hispolon used in our experiment (≤10 μM) exhibited anti-inflammatory effects but not a significant cytotoxic effect on macrophages.…”
Hispolon is a potent anticancer, anti-inflammatory, antioxidant, and antidiabetic agent isolated from Phellinus linteus, an oriental medicinal mushroom. However, the immunomodulatory mechanisms by which hispolon affects macrophages and lymphocytes remain poorly characterized. We investigated the immunomodulatory effects of hispolon on oxidative stress, inflammatory responses, and lymphocyte proliferation using lipopolysaccharide (LPS)-treated RAW264.7 macrophages or mitogen/alloantigen-treated mouse splenocytes. Hispolon inhibited LPS-induced reactive oxygen and nitrogen species (ROS/RNS) generation and decreased total sulfhydryl (SH) levels in a cell-free system and RAW264.7 cells. Hispolon exerted significant anti-inflammatory effects by inhibiting production of the proinflammatory cytokines interleukin 6 (IL-6) and tumor necrosis factor alpha (TNF-α) and activation of nuclear factor kappa B (NF-κB) and signal transducer and activator of transcription 3 (STAT3) in LPS-treated RAW264.7 cells. Hispolon also modulated NF-κB and STAT3 activation by suppressing the NF-κB p65 interaction with phospho-IκBα and the STAT3 interaction with JAK1, as determined via coimmunoprecipitation analysis. Additionally, hispolon significantly decreased lymphocyte proliferation, T cell responses and T helper type 1 (Th1)/type 2 (Th2) cytokines production in mitogen/alloantigen-treated splenocytes. We conclude that hispolon exerts immunomodulatory effects on LPS-treated macrophages or mitogen/alloantigen-treated splenocytes through antioxidant, anti-inflammatory, and antiproliferative activities. Thus, hispolon may be a therapeutic agent for treating immune-mediated inflammatory diseases.
“…These reported data suggest the potential of hispolon as a potent multi-target anticancer drug. Chethna et al [ 51 ] reported that hispolon showed higher toxicity in three types of cancer cells (MCF7, A549, and CHO) than splenic lymphocytes at the same dose. From the results depicted in Figure 1 , the doses of hispolon used in our experiment (≤10 μM) exhibited anti-inflammatory effects but not a significant cytotoxic effect on macrophages.…”
Hispolon is a potent anticancer, anti-inflammatory, antioxidant, and antidiabetic agent isolated from Phellinus linteus, an oriental medicinal mushroom. However, the immunomodulatory mechanisms by which hispolon affects macrophages and lymphocytes remain poorly characterized. We investigated the immunomodulatory effects of hispolon on oxidative stress, inflammatory responses, and lymphocyte proliferation using lipopolysaccharide (LPS)-treated RAW264.7 macrophages or mitogen/alloantigen-treated mouse splenocytes. Hispolon inhibited LPS-induced reactive oxygen and nitrogen species (ROS/RNS) generation and decreased total sulfhydryl (SH) levels in a cell-free system and RAW264.7 cells. Hispolon exerted significant anti-inflammatory effects by inhibiting production of the proinflammatory cytokines interleukin 6 (IL-6) and tumor necrosis factor alpha (TNF-α) and activation of nuclear factor kappa B (NF-κB) and signal transducer and activator of transcription 3 (STAT3) in LPS-treated RAW264.7 cells. Hispolon also modulated NF-κB and STAT3 activation by suppressing the NF-κB p65 interaction with phospho-IκBα and the STAT3 interaction with JAK1, as determined via coimmunoprecipitation analysis. Additionally, hispolon significantly decreased lymphocyte proliferation, T cell responses and T helper type 1 (Th1)/type 2 (Th2) cytokines production in mitogen/alloantigen-treated splenocytes. We conclude that hispolon exerts immunomodulatory effects on LPS-treated macrophages or mitogen/alloantigen-treated splenocytes through antioxidant, anti-inflammatory, and antiproliferative activities. Thus, hispolon may be a therapeutic agent for treating immune-mediated inflammatory diseases.
“…Hispolon isolated from Inonotus hispidius shows a strong antioxidant activity ( Venkateswarlu et al, 2010 ). Recently, hispolon and its derivatives have also been reported to exhibit ROS scavenging activities in cell-free systems ( Chethna et al, 2018a ), affirming its potential as antioxidant agent.…”
Section: Biological Activities Of Hispolonmentioning
confidence: 95%
“…Similarly, phenyl substitution enhances the activity while cyclohexyl decreases the activity. Similarly, by comparison of benzyl group and simple alkyl group, it has been observed that the benzyl group increases the activity more than a simple alkyl group ( Chethna et al, 2018b ; Weia et al, 2020 ). Fig.…”
Section: Introductionmentioning
confidence: 95%
“…Highly diverse and amply decorated mushroom-derived polyphenolic styrylpyrone scaffolds hold great promise for utilization in drug discovery ( Lee and Yun, 2011 ). One such bioactive styrylpyrone polyphenolic entity present in several mushrooms is hispolon ( Chethna et al, 2018a ). Hispolon, a bioactive constituent of traditionally used medicinal mushrooms, exhibits a broad range of medicinal properties.…”
Nature as an infinite treasure of chemotypes and pharmacophores will continue to play an imperative role in the drug discovery. Natural products (NPs) such as plant and fungal metabolites have emerged as leads in drug discovery during recent years due to their efficacy, safety and selectivity. The current review summarizes natural sources as well as pharmacological potential of hispolon which is a major constituent of traditional medicinal mushroom
Phellinus linteus
. The study aims to update the scientific community about recent developments of hispolon in the arena of natural drugs by providing insights into its present status in therapeutic pursuits. Hispolon, a polyphenol has been reported to possess anticancer, antidiabetic, antioxidant, antiviral and anti-inflammatory activities. It fights against cancer
via
induction of apoptosis, halting cell cycle and inhibition of metastasis by targeting various cellular signaling pathways including PI3K/Akt, MAPK and NF-κB. The current review proposes that hispolon provides a novel opportunity for pharmacological applications and its styrylpyrone carbon skeleton might serve as an attractive scaffold for drug development. However, future researches are recommended to assess bioavailability, toxicological limits, pharmacokinetic and pharmacodynamic profiles of hispolon, in order to establish its potential as a potent multi-targeted drug in the near future.
“…Dehydrohispolon is a promising antitubercular agent showing lower MIC against M. tuberculosis with respect to hispolon [ 240 ]. Hispolon and hispolon methyl ether pyrazole derivatives ( Scheme 20 ) showed improved stability with respect to their precursors as well as antigenotoxic effects against radiation exposure [ 241 ].…”
Phenols are widespread in nature, being the major components of several plants and essential oils. Natural phenols’ anti-microbial, anti-bacterial, anti-oxidant, pharmacological and nutritional properties are, nowadays, well established. Hence, given their peculiar biological role, numerous studies are currently ongoing to overcome their limitations, as well as to enhance their activity. In this review, the functionalization of selected natural phenols is critically examined, mainly highlighting their improved bioactivity after the proper chemical transformations. In particular, functionalization of the most abundant naturally occurring monophenols, diphenols, lipidic phenols, phenolic acids, polyphenols and curcumin derivatives is explored.
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