• 한국분말재료학회지
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• 제27권6호
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• pp.458-463
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• 2020

Hispidin is a secondary metabolite found in numerous medicinal mushrooms that has attracted significant attention, owing to its distinct biological effects, including antioxidant, anti-inflammatory, antitumor, and cytoprotective properties. Experiments are being carried out to study the interaction of detonation nanodiamonds (DNDs) with synthetic and natural hispidin sourced from extracts of Pholiota sp. fungus. The bioluminescence method is used to determine the adsorption/desorption properties of DNDs toward hispidin. It is found that hispidin forms strong conjugates with DNDs, and the use of various eluents does not result in a significant release of the adsorbed hispidin molecules. DND-bovine serum albumin (BSA) complex, where DNDs serve as a carrier for the protein and the latter acts as a hispidin sorbent, has been developed and applied in hispidin adsorption/desorption tests. The results support the use of the DNDs as a carrier for hispidin in medical applications. They also advocate the application of the DND-BSA complex for isolating the substance from fungal extracts.

• Journal of Microbiology and Biotechnology
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• 제18권1호
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• pp.107-109
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• 2008

Medicinal fungi, Phellinus linteus and Inonotus xeranticus, produce a cluster of yellow pigment in their fermentation broth that acts as an important element of biological activity. The pigment is composed of diverse polyphenols with a styrylpyrone moiety, mainly hispidin and its dimers, 3,14'-bihispidinyl, hypholomine B, and 1,1-distyrylpyrylethan. Although dimeric hispidins were proposed to be biosynthesized from two molecules of monomer via oxidative coupling by ligninolytic enzymes, laccase and peroxidase, the details of this process remain unknown. In this preliminary study, we attempted to achieve enzymatic synthesis of the hispidin dimer from hispidin by using commercially available horseradish peroxidase (HRP). Consequently, a hispidin dimer, 3,14'-bihispidinyl, was synthesized, whereas the other dimers, hypholomine B and 1,1-distyrylpyrylethan, were not produced. This result suggested that the oxidative coupling at the C-3 and C-14' positions of hispidins was dominant in the process of dimerization by HRP, and indicated that additional catalysts or substrates would be needed to synthesize other hispidin dimers present in the fungal metabolite.

• Mycobiology
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• 제51권5호
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• pp.360-371
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• 2023

Hispidin is an important styrylpyrone produced by Sanghuangporus sanghuang. To analyze hispidin biosynthesis in S. sanghuang, the transcriptomes of hispidin-producing and non-producing S. sanghuang were determined by Illumina sequencing. Five PKSs were identified using genome annotation. Comparative analysis with the reference transcriptome showed that two PKSs (ShPKS3 and ShPKS4) had low expression levels in four types of media. The gene expression pattern of only ShPKS1 was consistent with the yield variation of hispidin. The combined analyses of gene expression with qPCR and hispidin detection by liquid chromatography-mass spectrometry coupled with ion-trap and time-of-flight technologies (LCMS-IT-TOF) showed that ShPKS1 was involved in hispidin biosynthesis in S. sanghuang. ShPKS1 is a partially reducing PKS gene with extra AMP and ACP domains before the KS domain. The domain architecture of ShPKS1 was AMP-ACP-KS-AT-DH-KR-ACP-ACP. Phylogenetic analysis shows that ShPKS1 and other PKS genes from Hymenochaetaceae form a unique monophyletic clade closely related to the clade containing Agaricales hispidin synthase. Taken together, our data indicate that ShPKS1 is a novel PKS of S. sanghuang involved in hispidin biosynthesis.

• Archives of Pharmacal Research
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• 제27권6호
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• pp.615-618
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• 2004

In the course of screening for reactive oxygen species scavengers from natural products, an antioxidant was isolated from the mycelial culture broth of Phellinus linteus and identified as hispidin. The hispidin content was reached its maximum level at 12 days after onset of inoculation. About 2.5 mg／mL of hispidin was produced by P linteus in a yeast-malt medium (pH 5.8, $25^{\circ}C$). Hispidin inhibited 22.6 and 56.8% of the super oxide anion radical, 79.4 and 95.3% of the hydroxyl radical, and 28.1 and 85.5% of the DPPH radical at 0.1 and 1.0 mM, respectively. The positive control ${\alpha}-tocopherol$ scavenged 25.6 and 60.3%, 74.6 and 96.3%, and 32.7 and 77.5% of each radical, respectively, at the same concentrations. However, hispidin showed no significant activity on the hydrogen peroxide radical.

• 대한화학회지
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• 제58권6호
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• pp.553-559
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• 2014

Alzheimer's disease (AD) is a devastating neurodegenerative disease that represents the most common form of dementia among the elderly population. The deposition of aggregated ${\beta}$-amyloid ($A{\beta}$) senile plaques in the human brain is a classic observation in the neuropathology of AD, yet an understanding of the mechanism of their formation remains elusive. $A{\beta}$ is formed through endoproteolysis of the amyloid precursor protein (APP) by ${\beta}$-secretase (BACE1, ${\beta}$-site APP-cleaving enzyme) and ${\gamma}$-secretase. In this study, BACE1 protein was successfully over-expressed, purified, and refolded and utilized in a binding study with hispidin. We developed a simpler refolding method using a urea gradient and size-exclusion gel filtration to purify an active BACE1 protein variant, in larger quantities than that reported previously, and measured the binding affinity of hispidin to the BACE1 protein variant through isothermal titration calorimetry.

• Mycobiology
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• 제40권2호
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• pp.142-144
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• 2012

During the search for neuraminidase inhibitors from medicinal fungi, we found that the culture broth of Phellinus linteus exhibited potent inhibitory activity. Solvent partition, Sephadex LH-20 column chromatography, and high-performance liquid chromatography (HPLC) were performed for purification of two active substances from the culture broth. According to $^1H$ NMR measurements and comparison of HPLC retention times with those of authentic compounds, their chemical structures were identified as hispidin and hypholomine B. Compounds (hispidin) 1 and 2 (hypholomine B) inhibited neuraminidase, with $IC_{50}$ values of 13.1 and 0.03 ${\mu}M$, respectively.

• Mycobiology
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• 제36권1호
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• pp.55-59
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• 2008

Gymnopilus spectabilis, a hallucinogenic mushroom belonging to the family Cortinariaceae, is found growing in dense clusters on stumps and logs of hardwoods and conifers. It contains the hallucinogenic alkaloid psilocybin and its strongly bitter taste makes it undesirable as an edible. In an effort to identify chemical constituents of Korean native wild mushrooms, 4,6-decadiyne-1,3,8-triol (1), ergosta-4,6,8(14), 22-tetraen-3-one (2), bisnoryangonin (3), and hispidin (4) were isolated from the methanolic extract of the fruiting bodies of G. spectabilis. Their structures were assigned on the basis of various spectroscopic studies. Compounds 3 and 4 displayed significant scavenging activity against the ABTS radical cation, DPPH radical, and superoxide radical anion, while 1 and 2 exhibited no antioxidant activity.

• 한국버섯학회지
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• 제18권1호
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• pp.29-36
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• 2020

P. linteus(품종명: 고려상황, PLKS)와 P. baumii (장수상황, PBJS)를 동일한 조건하에서 인공재배하여 얻어진 자실체를 70% 메탄올, 60% 에탄올, 열수추출하여 폴리페놀과 플라보노이드 측정 시 함량은 60%에탄올 추출물에서 가장 높게 나타났다. 60%에탄올을 용매로 PLKS와 PBJS의 자실체를 추출하여 농도별로 DPPH (2,2-diphenyl-1-picrylhydrazyl), ABTS (2,2'-azino-bis (3-ethylbisthiazoline-6-sulfonic acid) 라디칼 소거능을 측정한 결과 PLKS와 PBJS는 거의 유사한 항산화 활성을 보였으며 자실체가 균사체보다 2-3배 이상 높은 항산화 활성이 측정되었으나 FRAP (ferric reducing antioxidant power)분석에서는 자실체와 균사체 간에 큰 차이가 없는 것을 확인하였다. PLKS와 PBJS의 자실체 ethyl acetate 분획물을 HPLC 분석한 결과 styrylpyrone 계 폴리페놀 성분인 davallialactone, hispidin, hypholomine B, inoscavin A를 검출할 수 있었으나 균사체에서는 검출되지 않아 자실체 특이적인 화합물인 것을 확인하였다.

• 한국버섯학회지
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• 제16권4호
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• pp.311-317
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• 2018

참나무 단목원목으로 재배한 P. linteus KACC93057P(PLHS)2년산 자실체 60%에탄올 추출물의 총 페놀함량은 $19.05{\pm}0.32mg\;GAE/g$로 다른 비교구 버섯 종에 비하여 4배에서 10배이상의 높게 나타났다. $125{\mu}g/mL$농도에서 DPPH와 ABTS 라디칼 소거능은 62%와 100%를 나타냈으며 FRAP 환원력은 $0.7{\mu}MFeSO_4/g$으로 비교 구 버섯종 보다 2에서 10배이상의 유효활성이 검출 되었다. PLHS 자실체 ethyl acetate분배 추출물의 HPLC분석에서 styrylpyrone 계열의 화합물 davallialactone, hispidin, hypholomine B와 phenylpropanoid 계열의 화합물인 caffeic acid가 동정 되었다.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.271.2-271.2
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• 2003

The ${\gamma}$- and ${\beta}$-secretase are one of the most important proteases, which cleave amyloid precursor protein (APP) into neurotoxic A${\beta}$ peptide in Azheimer's type dementia. In the course of screening for anti-dementia agents from natural products, the mycelial culture of mushroom Phellinus linteus showed potent inhibition againt ${\beta}$-secretase (BACE1). (omitted)