X-ray crystal structures, density functional theory and docking on deacetylase enzyme for antiproliferative activity of hispolon derivatives on HCT116 colon cancer

Rossi, Miriam; Caruso, Francesco; Costanzini, Ilaria; Kloer, Carmen; Sulovari, Aron; Monti, Elena; Gariboldi, Marzia Bruna; Marras, Emanuela; Balaji, Neduri V.; Ramani, Modukuri V.; Subbaraju, Gottumukkala V.

doi:10.1016/j.bmc.2019.07.008

Cited by 11 publications

(6 citation statements)

References 34 publications

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“…Lu et al 9 Rossia et al 28 studied the structure activity relationship (SAR) of hispolon for anti-proliferative action against HCT116 tumor, indicating the significance of the hydrogenation of hispolon bridge. Yun et al 29 analyzed the susceptibility of human renal carcinoma cells to hispolon, which was mediated by inducing apoptosis through TNF-related apoptosisinducing ligand (TRAIL).…”

Section: Phellinus Linteus -Black Hoof Mushroommentioning

confidence: 99%

Biological Activities of Hispolon

Kolla¹,

Bollikolla²

2022

CJST

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Natural products are a great source for the discovery of new chemotherapeutic agents. Phenolic compounds are significant natural products, mostly from the source of microorganisms and plants. Among fungi, mushrooms are not only the source of nutrients but also many bioactive components. In this paper, the authors made a comprehensive review of the biological activities of hispolon. The biological activities like anticancer, antioxidant, anti-inflammatory, and antimicrobial are possessed by hispolon. Along with anti-tuberculosis properties, hispolon exhibited effectiveness in the treatment of metabolic disorders and functional as immunomodulators.

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Section: Phellinus Linteus -Black Hoof Mushroommentioning

confidence: 99%

Biological Activities of Hispolon

Kolla¹,

Bollikolla²

2022

CJST

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“…Recently, several hispolon derivatives have been submitted to in silico predictions to preliminarily evaluate their anticancer activity. Theoretical analysis confirmed that aromatic ring substitution with methoxy and hydroxy groups delivers new hispolon analogues with good antiproliferative activity, sometimes even higher than that of hispolon itself [ 236 , 237 ]. In fact, the hispolon derivatives dehydroxyhispolon methyl ether and hispolon methyl ether exhibited higher in vitro cytotoxicity than hispolon against colorectal cancer [ 238 , 239 ].…”

Section: Diphenolsmentioning

confidence: 99%

Tailored Functionalization of Natural Phenols to Improve Biological Activity

et al. 2021

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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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“…2 , Fig. 3 ( Rossia et al, 2019 ; Weia et al, 2020 ). These groups have different influences on activity as calculated by DFT.…”

Section: Introductionmentioning

confidence: 98%

“…Substitution of different groups in basic skeleton of hispolon especially in aromatic phenyl ring played an excellent role in enhancing the biological activity. For example placement of methoxy group ( -OCH 3 ) in phenyl ring increase the cytotoxicity but in comparison, the presence of hydroxyl ( -OH ) group decrease the cytotoxicity and this has been supposed to be due to greater lipocity of methoxy (- OCH 3 ) as compared to hydroxyl ( OH ) ( Bisogno et al, 2007 ; Gaoa et al, 2018 ; Rossia et al, 2019 ). Moreover, it has been observed that the position of substitution on hispolon skeleton also played a crucial role in enhancing its activity as shown in Fig.…”

Section: Introductionmentioning

confidence: 99%

Hispolon: A natural polyphenol and emerging cancer killer by multiple cellular signaling pathways

Sarfraz

Rasul

Sarfraz

et al. 2020

Environmental Research

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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.

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X-ray crystal structures, density functional theory and docking on deacetylase enzyme for antiproliferative activity of hispolon derivatives on HCT116 colon cancer

Cited by 11 publications

References 34 publications

Biological Activities of Hispolon

Biological Activities of Hispolon

Tailored Functionalization of Natural Phenols to Improve Biological Activity

Hispolon: A natural polyphenol and emerging cancer killer by multiple cellular signaling pathways

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