Chromene and chromone derivatives as liver X receptors modulators from a marine-derived Pestalotiopsis neglecta fungus

Liang, Zhi; Gu, Tanwei; Wang, Jianjiao; She, Jianglian; Ye, Yuxiu; Cao, Wenzhi; Luo, Xiaowei; Xiao, Jiangjian; Liu, Yonghong; Tang, Lan; Zhou, Xuefeng

doi:10.1016/j.bioorg.2021.104927

Cited by 11 publications

(6 citation statements)

References 20 publications

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“…Further study discovered pestalotiochromones A (103) as a potential LXRs agonist, remarkably upregulated LXRβ and downstream gene ABCA1. Moreover, 103 combined well with LXRα in a dose-dependent manner, the kinetic curves of which resembled those of the potent LXRs agonist GW3965 for binding with LXRα, with K D of 6.2 μM ( Liang et al, 2021 ).…”

Section: Natural Products Targeting Liver X Receptorsmentioning

confidence: 95%

Natural Products Targeting Liver X Receptors or Farnesoid X Receptor

She

Pang

et al. 2022

Front. Pharmacol.

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Nuclear receptors (NRs) are a superfamily of transcription factors induced by ligands and also function as integrators of hormonal and nutritional signals. Among NRs, the liver X receptors (LXRs) and farnesoid X receptor (FXR) have been of significance as targets for the treatment of metabolic syndrome-related diseases. In recent years, natural products targeting LXRs and FXR have received remarkable interests as a valuable source of novel ligands encompassing diverse chemical structures and bioactive properties. This review aims to survey natural products, originating from terrestrial plants and microorganisms, marine organisms, and marine-derived microorganisms, which could influence LXRs and FXR. In the recent two decades (2000–2020), 261 natural products were discovered from natural resources such as LXRs/FXR modulators, 109 agonists and 38 antagonists targeting LXRs, and 72 agonists and 55 antagonists targeting FXR. The docking evaluation of desired natural products targeted LXRs/FXR is finally discussed. This comprehensive overview will provide a reference for future study of novel LXRs and FXR agonists and antagonists to target human diseases, and attract an increasing number of professional scholars majoring in pharmacy and biology with more in-depth discussion.

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Section: Natural Products Targeting Liver X Receptorsmentioning

confidence: 95%

Natural Products Targeting Liver X Receptors or Farnesoid X Receptor

She

Pang

et al. 2022

Front. Pharmacol.

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“…The second most common synthetic LXR-α and LXR-β agonist is GW3965 ( Figure 2 ). 255 , 272 , 317 , 319 , 321 , 334 , 348 - 352 GW3965 increased mRNA 317 , 319 , 321 , 348 , 349 , 351 , 352 and protein levels 255 , 272 , 351 in different ABCA1-expressing cells. Functionally, increased Abca1 mRNA and ABCA1 protein levels correlated with enhanced cholesterol efflux.…”

Section: Part I: Status Quomentioning

confidence: 93%

“…Several other natural compounds induced ABCA1 / Abca1 targeting LXR-α and LXR-β activation 256 , 272 , 256 , 349 , 367 and/or LXRA / Lxra and LXRB / Lxrb induction. 331 , 348 , 350 , 368 , 369 , 370 , 371 , 372 , 373 , 374 The garlic ingredient allicin, 350 the alkaloid berberine, 256 the coumarin bergapten A, 368 certain Pestalotiopsis neglecta -derived chromene derivatives, 348 the Rheum palmatum -derived anthraquinone danthron, 369 the lacton 1,6- O,O -diacetylbritannilactone, 371 epigallocatechin gallate (EGCG), 370 the glycoside geniposide, 375 the vegetable ingredient phenethyl isothiocyanate, 373 the carotenoid lycopene, 372 the Pestalotiopsis neglecta -derived hydroquinone pestalotioquinoside C, 349 the alkaloid rutaecarpine, 367 selenium, 374 the macrolactone soraphene A, 272 and vitamin D 3 331 led to increased ABCA1 / Abca1 mRNA 256 , 272 , 331 , 348 , 369 , 256 , 367 , 370 , 372 , 373 and ABCA1 protein 256 , 272 , 331 , 349 , 350 , 368 , 369 , ...…”

Section: Part I: Status Quomentioning

confidence: 99%

Strategies to gain novel Alzheimer’s disease diagnostics and therapeutics using modulators of ABCA transporters

Pahnke

Bascuñana

Brackhan

et al. 2021

Free Neuropathology

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Adenosine-triphosphate-(ATP)-binding cassette (ABC) transport proteins are ubiquitously present membrane-bound efflux pumps that distribute endo- and xenobiotics across intra- and intercellular barriers. Discovered over 40 years ago, ABC transporters have been identified as key players in various human diseases, such as multidrug-resistant cancer and atherosclerosis, but also neurodegenerative diseases, such as Alzheimer’s disease (AD). Most prominent and well-studied are ABCB1, ABCC1, and ABCG2, not only due to their contribution to the multidrug resistance (MDR) phenotype in cancer, but also due to their contribution to AD. However, our understanding of other ABC transporters is limited, and most of the 49 human ABC transporters have been largely neglected as potential targets for novel small-molecule drugs. This is especially true for the ABCA subfamily, which contains several members known to play a role in AD initiation and progression. This review provides up-to-date information on the proposed functional background and pathological role of ABCA transporters in AD. We also provide an overview of small-molecules shown to interact with ABCA transporters as well as potential in silico , in vitro , and in vivo methodologies to gain novel templates for the development of innovative ABC transporter-targeting diagnostics and therapeutics.

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“…OSMAC manipulation of Pestalotiopsis heterocornis led to production of polyketides 643–650 and ceramide 651 , 230 a P. neglecta culture yielded chromenes 652–655 and chromones 656 and 657 , 231 (−)-tricinonoic acid 658 and polyketide 659 were isolated from Phaeosphaeria spartinae , 232 and deep-sea sediment-derived Phomopsis strains yielded tenellone–macrolides 660–662 , 233 and chlorinated azaphilones 663–667 . 234 Pleosporales strains were the source of phenalenone derivatives 668–670 , 235 and polyketides 671 and 672 .…”

Section: Marine Microorganisms and Phytoplanktonmentioning

confidence: 99%