c. glabrata

iKIX1 是一种 Pdr1 依赖性基因激活。 它在体外和在播散性和泌尿道光滑念珠菌感染的动物模型中使耐药的光滑念珠菌对唑类抗真菌剂重新敏感。它可研究多药耐药性和光滑念珠菌感染。

Isavuconazole (RO-0094815) 是一种三唑类前药，对酵母、霉菌和二型真菌具有抗真菌活性。它抑制麦角固醇生物合成，导致真菌膜结构和功能的破坏。它是 CYP3A4抑制剂。

Rezafungin (SP-3025) 是一种长效的广谱棘皮菌素，对念珠菌、曲霉和肺孢子菌具有强效抗真菌活性。

Antiangiogenic agent 8 (Compound 3m) 是一种抑菌剂，并具有抗血管生成活性。其对E. coli、P. aeruginosa、B. subtilis、S. aureus、C. glabrata的MIC分别为16、8、4、16、8 μg mL，MBC范围为32-64 μg mL。Antiangiogenic agent 8 可能在抗感染和心血管疾病研究中具有应用潜力。

Milbemycin A4 oxime is a derivative of milbemycin A4 and a component of milbemycin oxime , compounds that both have insecticidal and nematocidal activity. Milbemycin A4 oxime (0.05 mg kg) reduces the number of microfilariae of the heartworm D. immitis in naturally infested dogs. It inhibits the growth of clinical isolates of C. glabrata with MIC80 values ranging from 16 to greater than 32 μg ml. Milbemycin A4 oxime (2.5 μg ml) blocks efflux of fluconazole from a clinical isolate of C. glabrata, but not from a strain lacking the efflux pumps CgCDR1 and PDH1, and reduces the MICs of fluconazole and 4-nitroquinoline 1-oxide in wild-type C. glabrata. It enhances adriamycin-induced inhibition of cell growth, as well as increases the intracellular accumulation of adriamycin and the P-glycoprotein substrate rhodamine 123 , in adriamycin-resistant, but not -sensitive, MCF-7 breast cancer cells in a concentration-dependent manner.

Diallyl tetrasulfide is an organosulfur compound that has been found in A. sativum and has diverse biological activities, including antimicrobial, antioxidant, and anticancer properties.[1],[2],[3],[4] It is active against the bacteria S. aureus and methicillin-resistant S. aureus (MRSA; MICs = 0.5 and 2 mg L, respectively), as well as the fungi C. albicans, C. krusei, C. glabrata, A. niger, A. flavus, and A. fumigatus (MICs = 0.5, 4, 2, 1, 2, and 4 mg L, respectively).[1] It reduces cadmium-induced increases in hepatic levels of thiobarbituric acid reactive substances (TBARS) and increases cadmium-induced decreases in the hepatic activity of superoxide dismutase (SOD1), catalase, GST, and glucose-6-phosphate dehydrogenase (G6PDH) in rats when administered at a dose of 40 mg kg.[2] Diallyl tetrasulfide is cytotoxic to MCF-7 breast cancer cells (IC50 = 92 μM) and reduces tumor growth in a BGC-823 mouse xenograft model when administered at doses of 20, 30, and 40 mg kg for 32 days.[3],[4]

Sordarin is an inhibitor of fungal protein synthesis originally isolated from S. araneosa.[1] It binds to elongation factor 2 (EF-2) in the presence of ribosomes and inhibits the uncoupled GTPase activity of equimolar mixtures of EF-2 and ribosomes from C. albicans (IC50 = 0.1 μM). Sordarin inhibits protein synthesis in cell-free lysates of C. albicans, C. glabrata, and C. neoformans (IC50s = 0.01, 0.2, and 0.06 μg/ml, respectively) but not in rabbit reticulocytes (IC50 = >100 μg/ml).[1] [2] It inhibits the growth of C. albicans (MIC = 8 μg/ml) but not C. glabrata or C. neoformans (MICs = >125 μg/ml).

Sphinganine is a synthetic bioactive sphingolipid that inhibits the growth of C. glabrata and C. albicans with a minimum fungicidal concentration (MFC) value of 0.5 μg/ml for both. More commonly, sphinganine is used as an internal standard in the analysis of sphingoid compounds by chromatographic or spectrometric methods.

Anticandidal agent-1 (化合物 c2) 是有效的广谱抗念珠菌剂，可通过阻断菌丝伸长和丝化来抑制生物膜。Anticandidal agent-1 对光滑念珠菌和白念珠菌具有抗念珠菌活性，MIC50值分别为 13.51 和 8.65 μg mL。

Antifungalagent 72（Compound B8）是一款高效抗真菌药物。该化合物通过抑制Pdr1-KIX相互作用（Ki：11.7μM）来干扰外排泵功能，并降低与耐药性相关的基因表达。Antifungalagent 72对抗氟康唑（Fluconazole）耐药的C. glabrata 0161菌株显示出显著的抗菌活性，其MIC值为63 ng mL，并与氟康唑合用时表现出协同效果。此化合物可应用于C. glabrata感染的相关研究。