Isolation and acetylcholinesterase inhibitory activity of asterric acid derivatives produced by Talaromyces aurantiacus FL15, an endophytic fungus from Huperzia serrata

Yang, Xiao; Liang, Weizhong; Liu, De Li; Zhang, Zhibin; Chang, Jun; Zhu, Du

doi:10.1007/s13205-022-03125-2

Cited by 8 publications

(9 citation statements)

References 74 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Researchers supposed that the variety and size of the esterification substituent at C-2 might be critical for the AChE inhibitory activities, considering the result that the IC 50 values of 1 , 3 , and 36 were 66.7, 23.3, and 20.1 μM, respectively. Meanwhile, molecular docking analysis further unveiled that these compounds interacted with the active catalytic site and peripheral anionic site of AChE …”

Section: Bioactivities Of Asterric Acid Analogsmentioning

confidence: 99%

See 1 more Smart Citation

Naturally Occurring Asterric Acid Analogs: Chemistry and Biology

Tan,

Chen,

Ding

2024

J. Agric. Food Chem.

View full text Add to dashboard Cite

Asterric acid and its analogs belong to diphenyl ethers (DPEs) with multiple substitutions on A/B aromatic rings. This member of DPEs originates from the polyketide pathway and displays a wide range of biological effects. Though the structures of asterric acid analogs are not complex, there were only more than 50 asterric acid analogs found in nature from 1960 to 2023. In this review, the structures, bioactivities, and biosynthesis of asterric acid analogs are summarized. More importantly, the empirical rule about the shielding effect of B-ring on H-6 is suggested, and this provides a convenient and useful way to analyze the NMR spectral data of asterric acid analogs, based on which the chemical shift values of the A-ring in some asterric acid analogs are revised.

show abstract

Section: Bioactivities Of Asterric Acid Analogsmentioning

confidence: 99%

“…Meanwhile, molecular docking analysis further unveiled that these compounds interacted with the active catalytic site and peripheral anionic site of AChE. 85 4.4. Antibacterial, Antifungal, Antiviral, Antinematodal, and Antiplasmodial Activities.…”

Section: Cytotoxic Activitiesmentioning

confidence: 99%

Naturally Occurring Asterric Acid Analogs: Chemistry and Biology

Tan,

Chen,

Ding

2024

J. Agric. Food Chem.

View full text Add to dashboard Cite

show abstract

“…The inhibition potential of the extracted compounds was compared with commercially available withanolide A and limonin. (6) Enzyme inhibition was calculated by employing eq 6, where E o is the enzyme activity in the presence of substrate alone, while E s is the enzyme activity in the presence of substrate, as well as the plant compound. Enzyme activity was measured in terms of absorbance.…”

Section: Extraction Of Bioactive Compounds From Theirmentioning

confidence: 99%

“…Thus, inhibition of AChE reduces the breakdown of ACh in the brain and gives symptomatic relief to the patients. AChE is a carboxylic hydrolase of 121.21 kDa containing 2 side chains, with each chain comprising 534 amino acid residues . The catalytic site is marked by the presence of glutamic acid, serine, and histidine in a 20 Å gorge .…”

Section: Introductionmentioning

confidence: 99%

“…AChE is a carboxylic hydrolase of 121.21 kDa containing 2 side chains, with each chain comprising 534 amino acid residues. 6 The catalytic site is marked by the presence of glutamic acid, serine, and histidine in a 20 Å gorge. 7 Direct interaction of any compound with this site causes competitive inhibition of the enzyme, while the compounds interacting with sites other than the catalytic site also inhibit the enzyme by modifying the catalytic site and inducing steric blockade.…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Screening of Multitarget-Directed Natural Compounds as Drug Candidates for Alzheimer’s Disease Using In Silico Techniques: Their Extraction and In Vitro Validation

Srivastava,

Sharma,

Deep

et al. 2023

ACS Omega

View full text Add to dashboard Cite

Alzheimer's disease (AD) is a neurodegenerative disorder that impairs neurocognitive function. Acetylcholinesterase (AChE) and β-site APP cleaving enzyme 1 (BACE1) are the two main proteins implicated in AD. Indeed, the major available commercial drugs (donepezil, rivastigmine, and galantamine) against Alzheimer's are AChE inhibitors. However, none of these drugs are known to reverse or reduce the pathophysiological condition of the disease since there are multiple contributing factors to AD. Therefore, there is a need to develop a multitarget-directed ligand approach for its treatment. In the present study, plant bioactive compounds were screened for their AChE and BACE1 inhibition potential by conducting molecular docking studies. Considering their docking score and pharmacokinetic properties, limonin, peimisine, serratanine B, and withanolide A were selected as the lead compounds. Molecular dynamics simulations of these protein−ligand complexes confirmed the conformational and energetically stabilized enzyme−inhibitor complexes. The inhibition potential of the lead compounds was validated by in vitro enzyme assay. Withanolide A inhibited AChE (IC 50 value of 107 μM) and showed mixedtype inhibition. At this concentration, it inhibited BACE1 activity by 57.10% and was stated as most effective. Both the compounds, as well as their crude extracts, were found to have no cytotoxic effect on the SH-SY5Y cell line.

show abstract

Discovery of Enzyme Inhibitors from Mangrove Sediment Derived Fungus Trichoderma harzianum SCSIO 41051

Huang,

Chen,

Cai

et al. 2024

Chemistry & Biodiversity

View full text Add to dashboard Cite

One new fatty acid derivative, (2E,4E)‐6,7‐dihydroxy‐2‐methylocta‐2,4‐dienoic acid (1), and 16 known compounds (2−17) were isolated from the mangrove sediment derived fungus Trichoderma harzianum SCSIO 41051. Their structures were established by spectroscopic methods, computational ECD, and Mo2(OAc)4‐induced ECD experiment. All the compounds were evaluated for their acetylcholinesterase (AChE) and pancreatic lipase (PL) inhibition. Compounds 9 and 14 exhibited moderate AChE inhibitory activities with IC50 values of 2.49 and 2.92 μM, respectively, which compounds 8 and 9 displayed moderate inhibition on PL with IC50 value of 2.30 and 2.34 μM, respectively.

show abstract

Isolation and acetylcholinesterase inhibitory activity of asterric acid derivatives produced by Talaromyces aurantiacus FL15, an endophytic fungus from Huperzia serrata

Cited by 8 publications

References 74 publications

Naturally Occurring Asterric Acid Analogs: Chemistry and Biology

Naturally Occurring Asterric Acid Analogs: Chemistry and Biology

Screening of Multitarget-Directed Natural Compounds as Drug Candidates for Alzheimer’s Disease Using In Silico Techniques: Their Extraction and In Vitro Validation

Discovery of Enzyme Inhibitors from Mangrove Sediment Derived Fungus Trichoderma harzianum SCSIO 41051

Contact Info

Product

Resources

About