预约演示

更新于：2025-05-07

SQLE x CYP51A1

更新于：2025-05-07

基本信息

关联

项与 SQLE x CYP51A1 相关的药物

Ketoconazole/Terbinafine

酮康唑/特比萘芬

靶点

CYP51A1 x SQLE

作用机制

CYP51A1抑制剂 [+1]

在研机构-

原研机构

台湾生研股份有限公司

在研适应症-

非在研适应症

甲癣

最高研发阶段无进展

首次获批国家/地区-

首次获批日期1800-01-20

100 项与 SQLE x CYP51A1 相关的临床结果

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100 项与 SQLE x CYP51A1 相关的转化医学

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0 项与 SQLE x CYP51A1 相关的专利（医药）

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项与 SQLE x CYP51A1 相关的文献（医药）

2025-01-01·Diagnostic Microbiology and Infectious Disease

In vitro and silico activity of piperlongumine against azole-susceptible/resistant Aspergillus fumigatus and terbinafine-susceptible/resistant Trichophyton species

Article

作者: Teymoori, Ali ; Hedayati, Mohammad Taghi ; Otaševi´c, Suzana ; Ebrahimi-Barough, Robab ; Haghani, Iman ; Sillanpää, Mika ; Hoseinnejad, Akbar ; Nosratabadi, Mohsen ; Azadeh, Hossein ; Abastabar, Mahdi ; Aghili, Seyed Reza ; Yahyazadeh, Zahra ; Badali, Hamid ; Shokohi, Tahereh ; Rashidi, Mohsen ; Otasevic, Suzana ; Hashemi, Seyedeh Mahdieh

In recent years, the widespread emergence of drug resistance in yeasts and filamentous fungi to existing antifungal armamentariums has become a severe threat to global health. There is also concern regarding increased rates of azole resistance in Aspergillus fumigatus and Terbinafine resistance in Trichophyton species. To overcome this concern of resistance to regular therapies, new antifungal drugs with novel and effective mechanisms are crucially needed. Herbal remedies may be promising strategies for the treatment of resistant infections. We aimed to investigate the in vitro and silico activity of piperlongumine against clinical azole susceptible/resistant A. fumigatus and terbinafine-susceptible/resistant Trichophyton species. In the current study, piperlongumine demonstrated potent antifungal activity, with minimum inhibitory concentrations (MICs) ranging from 0.016-4 μg/mL against Trichophyton isolates and 0.25-2 μg/mL for A. fumigatus isolates. Additionally, molecular docking studies indicated that piperlongumine has a strong binding affinity to the active sites of squalene epoxidase and sterol 14-alpha demethylase. However, further studies are warranted to correlate these findings with clinical outcomes and provide the basis for further investigations to pave the way for developing novel antifungal agents.

2021-04-01·Graefe's Archive for Clinical and Experimental Ophthalmology

Linoleic acid inhibits in vitro function of human and murine dendritic cells, CD4+T cells and retinal pigment epithelial cells

Article

作者: Ye, Zi ; Wang, Qingfeng ; Su, Guannan ; Hu, Jianping ; Huang, Xinyue ; Yi, Shenglan ; Kijlstra, Aize ; Yang, Peizeng ; Du, Ziyu

PURPOSEIncreased linoleic acid (LA) was observed in acute anterior uveitis (AAU) patient feces in our previous study. To investigate the immunoregulatory effect of LA, we studied the effect of LA on human and murine dendritic cells (DCs), CD4⁺T cells, and retinal pigment epithelial (RPE) cells in vitro.METHODSThe level of LA in feces from AAU patients and healthy individuals was measured by gas chromatography coupled with a mass spectrometer (GC-MS). The immunoregulatory effect of LA on human and murine DCs, CD4⁺ T cells, and RPE cells was evaluated by enzyme linked immunosorbent assay (ELISA) and flow cytometry (FCM). The effect of LA on DCs was evaluated by Tandem mass tag (TMT)-based proteomics analysis.RESULTSIncreased LA was observed in feces from AAU patients (1018.35 ± 900.01 mg/kg) as compared with healthy individuals (472.55 ± 365.49 mg/kg, p = 0.0136). LA attenuated the antigen-presenting function of human and murine DCs by decreasing the expression of CD40, the secretion of IL-6 and IL-12p70, and the ability to shift naïve T cells towards T helper type 1 (Th1) and Th17 cells. LA also inhibited the secretion of MCP-1 and IL-8 from RPE cells. Proteomics analysis showed differential expression of 28 proteins, including squalene epoxidase (SQLE), farnesyl-diphosphate farnesyltransferase 1 (FDFT1), and cytochrome P450 family 51 subfamily A member 1 (CYP51A1), in LA-treated DCs compared with controls. LA also accelerated the apoptosis of DCs from healthy individuals.CONCLUSIONLA inhibited the function of human and murine DCs, CD4⁺T cells, and RPE cells, regulated the expression of proteins, and promoted the apoptosis of human DCs. These results collectively suggest that LA might decrease the function of immune cells in vitro, and further studies are needed to investigate its role in the pathogenesis of AAU.

2021-03-01·The Journal of Antibiotics4区 · 医学

Antifungal activity and potential mechanism of magnoflorine against Trichophyton rubrum

4区 · 医学

Article

作者: Luo, Nanxuan ; Zhang, Baoshun ; Li, Xuegang ; Yang, Changqing ; Jin, Liang ; Ye, Xiaoli ; Zhu, Yurong

Coptis alkaloids show potent antifungal activity against Trichophyton rubrum (T. rubrum), which was a Tinea pedis fungus, but little of the literature was reported to investigate the antifungal activity of magnoflorine against it. Meanwhile, the potential mechanism of magnoflorine against T. rubrum is unknown. In the present study, we found that Coptis alkaloids, especially magnoflorine had significant antifungal activities against T. rubrum and Trichophyton mentagrophyte (T. mentagrophyte). The MIC values of magnoflorine against T. rubrum and T. mentagrophyte were both 62.5 μg ml^-1, but magnoflorine exerted a better fungicidal efficiency against T. rubrum than T. mentagrophyte. Magnoflorine inhibited the conidia germination and hyphal growth, and changed the mycelial morphology such as deformation growth, surface peeling, and cytoplasmic contraction in T. rubrum. Magnoflorine had no significant effect on cell wall integrity. However, magnoflorine destroyed the fungal cell membrane of T. rubrum through increasing the nucleic acid leakage, reducing the activities of squalene epoxidase and CYP51 enzyme, and decreasing the content of ergosterol in hyphae. Our study supported the potential use of magnoflorine as an antifungal agent against T. rubrum and made contributions to the clinical application of magnoflorine against fungi.

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