MOLECULES
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2019
·Vol. 24
·期 16
·2980
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IF 3.06
Wei Li,Qian Liu,Shimian Cheng,Shanren Li,Yongbiao Zheng
Termitomyces albuminosusis the symbiotic edible mushroom of termites and cannot be artificially cultivated at present. In the project of exploring its pharmaceutical metabolites by microbial fermentation, four new selinane type sesquiterpenoids—teucdiol C (1), D (2), E (3), and F (4), together with two known sesquiterpenoids teucdiol B (5) and epi-guaidiol A (6)—were obtained from its fermented broth ofT. albuminosus. Their structures were elucidated by the analysis of NMR data, HR Q-TOF MS spectral data, CD, IR, UV, and single crystal X-ray diffraction.Epi-guaidiol A showed obvious anti-acetylcholinesterase activity in a dose-dependent manner. The experimental results displayed thatT. albuminosuspossess the pharmaceutical potential for Alzheimer’s disease, and it was an effective way to dig new pharmaceutical agent ofT. albuminosuswith the microbial fermentation technique.Keywords:Termitomyces albuminosus;selinane;sesquiterpenoids;anti-acetylcholinesterase;microbial fermentation
研究领域:
药理学
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真菌学
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天然产物化学
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DOI
PubMed
高影响因子
MICROPOROUS AND MESOPOROUS MATERIALS
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2024
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IF 4.8
Huanhuan Zheng,Hengchang He,Min Lu,Yuhui Pei,Huapei Peng,Wanli Zhou,Cheng Guo,Jianqiang Wang
Novel composite material (g-C 3 N 4 @Ser-PMO) based on the combination of serine mesoporous organosilicon (Ser-PMO) and graphitic carbon nitride (g-C 3 N 4 ) was designed to purify water containing antibiotic under light illumination. Serine mesoporous organosilicon was first formed by using self-created organosilicon precursor with serine as organic silicon resource in the presence of g-C 3 N 4 under template via co-condensation method. The structural, morphological and optical properties of composite material were confirmed by series of characterizations including XRD, FTIR, N 2 adsorption-desorption, UV–vis DRS spectra, TEM and XPS spectra. These results displayed that ordered mesoporous channels were formed on the surface of graphitic carbon nitride to enhance optical properties. Meanwhile, Serine was first induced in mesoporous framework to provide active sites. During photo-degradation experiment of ofloxacin in water, composite material exhibited excellent degradation efficiency. 99 % of ofloxacin was nearly degraded under the light irradiation in 90 min, compared with pristine g-C 3 N 4 . Moreover, composite material showed good stability and recyclability after multiple cycle experiments, which provided an ideal way to alleviate the pollution problem from antibiotics in water.
研究领域:
环境科学
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材料科学
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DOI
高影响因子
BIOMEDICINE & PHARMACOTHERAPY
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2023
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IF 7.5
Yiqian Zhang,Qianrui Huang,Qisi Xu,Chengsen Jia,Yong Xia
Triple negative breast cancer (TNBC) poses a significant clinical challenge due to its lack of targeted therapy options and the frequent development of chemotherapy resistance. Metastasis remains a primary cause of mortality in late-stage TNBC patients, underscoring the urgent need for alternative treatments. Repurposing existing drugs offers a promising strategy for the discovery of novel therapies. In this study, we investigated the potential of pimavanserin tartrate (PVT) as a treatment for TNBC. While previous studies have highlighted PVT's anticancer effects in various cancer types, its activity in TNBC remains unclear. Our investigation aimed to elucidate the anticancer effects and underlying mechanisms of PVT in TNBC. We evaluated the impact of PVT and combination treatments involving PVT on TNBC cell viability, apoptosis, autophagy, and associated signaling pathways. Our findings revealed that PVT may induce mitochondria-dependent intrinsic apoptosis and caused cytoprotective autophagy via the PI3K/Akt/mTOR pathway in TNBC cells in vitro . Notably, our study demonstrated strong synergistic anti-TNBC effects when combining PVT with doxorubicin. We also found PVT showed some efficacies to inhibit TNBC tumor growth in vivo . These results provided valuable insights into the potential of PVT as an anti-TNBC therapeutic and a possible option for enhancing the sensitivity of TNBC cells to conventional chemotherapy drugs. Further studies are needed to determine the activity and mechanism of PVT in inhibiting TNBC.
研究领域:
肿瘤学
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药理学
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癌症生物学
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PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
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2023
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IF 6.1
Yu Wang,Yao Yu,Yi-Ping Hou,Xue-Wei Mao,Zong-Liang Liu,Jian Cui,Bi Wang,Shu Xu,Yi-Yun Qian,Yan-Qin Jiang,Min Wei,Ping-Ping Song
Botrytis cinerea causes gray mold in many fruit and vegetable crops. We previously found that Seselin (SL) displayed antifungal activity against B. cinerea (EC50 = 6.1 μg·mL–1), and this study investigated the effects of Ca2+ and the Ca2+/CN signaling pathway on its antifungal activity against B. cinerea. The results indicated that exogenous Ca2+, Cyclosporine A, and Verapamil reduced the sensitivity of SL against B. cinerea; SL significantly reduced the intracellular Ca2+ concentration in the hyphae; the sensitivity of strains ΔbcCCH1 and ΔbcMID1 to SL were significantly increased; and the expressions of CCH1, MID1, CNA, PMC1, and PMR1 genes of the Ca2+/CN signaling pathway were significantly downregulated by SL treatment. Hence, SL is a potential compound for developing fungicides against B. cinerea. SL dramatically reduces intracellular Ca2+ concentration and disturbs Ca2+ homeostasis, leading to cell death. The Ca2+/CN signaling pathway plays an important role in the antifungal activity of SL against B. cinerea.
研究领域:
植物病理学
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分子生物学
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DOI
PubMed
高影响因子
ACTA PHARMACOLOGICA SINICA
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2021
·Vol. 42
·期 11
·1860-1874
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IF 6.15
Liu Zhen-zhen,Liu Xiao-ning,Fan Rui-cheng,Jia Yu-ping,Zhang Qing-ke,Gao Xin-qing,Wang Yu-qing,Yang Meng-qing,Ji Li-zhen,Zhou Yong-qing,Li Hong-li,Li Ping,Tang Bo
Glioblastoma multiforme (GBM) is the most common and malignant type of primary brain tumor, and 95% of patients die within 2 years after diagnosis. In this study, aiming to overcome chemoresistance to the first-line drug temozolomide (TMZ), we carried out research to discover a novel alternative drug targeting the oncogenic NFAT signaling pathway for GBM therapy. To accelerate the drug’s clinical application, we took advantage of a drug repurposing strategy to identify novel NFAT signaling pathway inhibitors. After screening a set of 93 FDA-approved drugs with simple structures, we identified pimavanserin tartrate (PIM), an effective 5-HT 2A receptor inverse agonist used for the treatment of Parkinson’s disease-associated psychiatric symptoms, as having the most potent inhibitory activity against the NFAT signaling pathway. Further study revealed that PIM suppressed STIM1 puncta formation to inhibit store-operated calcium entry (SOCE) and subsequent NFAT activity. In cellula, PIM significantly suppressed the proliferation, migration, division, and motility of U87 glioblastoma cells, induced G1/S phase arrest and promoted apoptosis. In vivo, the growth of subcutaneous and orthotopic glioblastoma xenografts was markedly suppressed by PIM. Unbiased omics studies revealed the novel molecular mechanism of PIM’s antitumor activity, which included suppression of the ATR/CDK2/E2F axis, MYC, and AuroraA/B signaling. Interestingly, the genes upregulated by PIM were largely associated with cholesterol homeostasis, which may contribute to PIM’s side effects and should be given more attention. Our study identified store-operated calcium channels as novel targets of PIM and was the first to systematically highlight the therapeutic potential of pimavanserin tartrate for glioblastoma.
研究领域:
肿瘤学
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药理学
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细胞生物学
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分子生物学
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DOI
PubMed
高影响因子
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