c. albicans

Fluconazole (UK-49858) belongs to the triazole class of antifungal agents and is a CYP51 inhibitor (IC99 = 0.20–0.39 μg/mL against Candida albicans), possessing broad-spectrum antifungal activity, good oral absorption, and cell permeability. This compound is used for the treatment of various invasive fungal infections.

Filastatin is a durable inhibitor of Candida albicans filamentation and exhibits potent antifungal activity.

Rezafungin (SP-3025, Biafungin) is a natural product echinocandin and a 1,3-β-D-glucan synthase inhibitor with broad-spectrum antifungal activity, high tissue penetration, and a long half-life, used for the treatment of candidemia and invasive candidiasis.

Isavuconazole (RO-0094815)(BAL-4815; RO-0094815) is the active component of the new azole antifungal agent BAL8557 with MIC(50)s/MIC(90)s ranged from 0.002/0.004 mg/liter for C. albicans to 0.25/0.5 mg/liter for C. glabrata.

Citric acid (Citro) is a weak organic tricarboxylic acid found in citrus fruits. Citric acid is a food additive and a natural preservative.

Oxiconazole is a broad-spectrum imidazole antifungal agent with fungicidal activity against T. rubrum, T. mentagrophytes, T. tonsurans, T. violaceum, E. floccosum, M. canis, M. audouini, M. gypseum, C. albicans, and M. furfur. have fungicidal activity, inhibiting ergosterol biosynthesis and disrupting fungal cell membrane integrity by disrupting cytochrome P450 enzymes (lanosterol 14- α demethylase). It also inhibits DNA synthesis and suppresses intracellular ATP concentration.

NSC 55655 (5-[(2-Nitrophenyl)methylene]-2,4-thiazolidinedione) possesses antimicrobial and antioxidant activities and inhibits the proliferation of B. subtilis, S. aureus, K. pneumonia, E. coli, S. typhi , A. niger and C. albicans. A. niger and C. albicans, and can be used in diabetes mellitus.

Amphotericin X1 is a derivative of Amphotericin B with good antifungal activity. Amphotericin X1 inhibits Candida albicans 33/079, Cryptococcus neoformans 451, C.parapsilosis 937A, Aspergillus niger 57A and A.fumigatus (MICs: 1 μg/mL, 1 μg/mL, 8 μg/mL, 2

Luteolin-7-rutinoside is a natural product that alleviates LPS-induced acute liver injury by inhibiting the PI3K/AKT/AMPK/NF-κB signaling pathways and suppressing TNF-α, IL-6, and IL-1β.

Yck2-IN-1 (Compound 2a) is an inhibitor of the fungus Candida albicans Yck2. It has an IC50 of approximately 80 nM for Yck2 and an MIC80 of 12.5 µM for C. albicans, demonstrating good metabolic stability [66% remaining in mouse liver microsomes]. In a mouse model with drug-resistant Candida, Yck2-IN-1 significantly reduced fungal load in the kidneys. Yck2-IN-1 shows potential for research in antifungal infection treatments.

Antifungalagent 128 (Compound 3ja) is an antifungal agent that, in combination with Fluconazole, has a MIC range of 0.5-4 μg/mL against C. albicans strains. It is applicable in the study of anti-infective therapies.

GW461484A is a small molecule inhibitor targeting Candida albicans Yck2, exhibiting an IC50 of 0.11 µM. It has a MIC80 of 12.5 µM against C. albicans. GW461484A shows potential for research into fungal diseases, including drug-resistant Candida infections.

Reveromycin C is a polyketide compound originally isolated from Streptomyces, exhibiting antifungal activity against Candida albicans with a MIC of 2.0 μg/mL at pH 3 and >500 μg/mL at pH 7.4. It inhibits EGF-induced mitogenic activity in Balb/MK mouse epidermal cell lines. Additionally, it reverses the morphology of sarcoma virus-transformed NRK rat kidney cells (EC50 = 1.58 μg/mL) and inhibits the proliferation of KB cells and K562 human chronic myelogenous leukemia cells (IC50 = 2.0 μg/mL for both).

Antifungalagent 96 (Compound WZ-2) is an antifungal agent with excellent blood-brain barrier permeability and brain penetration. It inhibits the growth of C. neoformans H99 and C. albicans 0304103, with MIC values of 0.016 and 32 μg/mL, respectively.

Antibacterialagent 203 (Compound 5h) possesses both antibacterial and antifungal properties. It demonstrates effective antifungal activity against Candida albicans (C. albicans) with a MIC of 3.90 μg/mL. Additionally, Antibacterialagent 203 exhibits antibacterial activity against normal mouse fibroblasts (L929), with an IC50 of 75.96 μM.

Antibacterialagent 218 (compound d28) is an orally active inhibitor of sterol 24-C-methyltransferase with an IC50 value of 0.273 μM. It also displays antifungal activity against Candida albicans SC5314, with an IC50 of 0.25 μg/mL.

10-Butyl EtherMinocycline is a derivative of Minocycline and acts as an inhibitor of MMP-8 and MMP-9, with IC50 values of 69.4 µM and 47.0 µM, respectively. It exhibits negligible antibacterial activity against E. coli, S. typhi, and C. albicans. Additionally, 10-Butyl EtherMinocycline inhibits LPS-induced microglial activation and VEGF-induced endothelial cell migration, as well as L-Glutamine-induced ROS levels. This compound significantly reduces alcohol consumption in a chronic intermittent ethanol (CIE) mouse model and is utilized in studies related to neuroinflammation and alcohol use disorder (AUD).

Fluconazole (hydrate) is a triazole antifungal agent used for oral treatment and prevention of both superficial and systemic fungal infections, including but not limited to balanitis, various Candida infections, Cryptococcus infections, dermatomycosis, and fungal infections of the respiratory and urinary tracts. As the hydrate salt form of fluconazole, it exhibits antifungal activity by inhibiting the growth and development of pathogenic fungi, such as Candida species, at minimal inhibitory concentrations often exceeding 100 mg/l. Notably, it disrupts the branching and hyphal formation in C. albicans at concentrations as low as 0.3 mg/l, indicating its potency compared to other antifungals like miconazole and ketoconazole which are effective at 100-fold lower concentrations. Clinical studies have not shown a significant increase in the risk of most birth defects with oral fluconazole, although there may be an associated risk of tetralogy of Fallot. Its efficacy against Cryptococcus gattii in koalas suggests it may be ineffective as a sole therapeutic agent at a dosage of 10 mg/kg orally every 12 h. Toxicity symptoms from overdose can include hallucinations and paranoid behavior.

7-oxo Staurosporine is an antibiotic originally isolated from S. platensis with diverse biological activites. It inhibits PKC, PKA, phosphorylase kinase, EGFR, and c-Src in vitro (IC50s = 9, 26, 5, 200, and 800 nM, respectively). 7-oxo Staurosporine induces cell cycle arrest in the G2/M phase in human leukemia K562 cells with a minimal effective dose (MED) of 30 ng/ml. It is cytotoxic to P388 mouse leukemia cells that are resistant and susceptible to doxorubicin . 7-oxo Staurosporine inhibits growth of the mycelial, but not yeast form of C. albicans, C. krusei, C. tropicalis, and C. lusitaniae (MICs = 3.1-25 μg/ml). It increases sphingomyelin synthesis in CHO-K1 cells when used at a concentration of 50 nM.

β-Defensin-3 (human) trifluoroacetate salt (hBD-3) is a key antimicrobial peptide in the human innate immune system, exhibiting broad-spectrum bactericidal, immunomodulatory, and tissue-repairing activities. β-Defensin-3 (human) trifluoroacetate salt can be used in the treatment of skin diseases and cancer, as well as in research on drug-resistant bacterial infections.

β-Defensin-4 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts. It induces migration of monocytes in vitro when used at a concentration of 10 nM but does not affect migration of neutrophils and eosinophils. β-Defensin-4 (30 μg/ml) stimulates gene expression and production of IL-6, IL-10, CXCL10, CCL2, MIP-3α, and RANTES by keratinocytes. It also stimulates calcium mobilization, migration, and proliferation of keratinocytes when used at concentrations of 30, 10, and 40 μg/ml, respectively. β-Defensin-4 induces IL-31 production by human peripheral blood-derived mast cells in vitro when used at a concentration of 10 μg/ml and by rat mast cells in vivo following a 500 ng intradermal dose. It also inhibits growth of E. coli, P. aeruginosa, and S. aureus with lethal concentration (LC) values of 5, 12, and 15 μM, respectively, of S. carnosus (MIC = 4.5 μg/ml), and of C. albicans with a minimum fungicidal concentration (MFC) value of 7.5 μM.

2-Acetylthiophene thiosemicarbazone is an antimicrobial agent that exhibits antimicrobial activity against a wide range of gram-negative (E. coli, P. aeruginosa, and S. marcescens ) and gram-positive (S. aureus, M. luteus, and B. cereus) bacteria. In addition, it has antimicrobial activity against a wide range of fungi (C. albicans, G. candidum, T. rubrum, F. oxysporum, A. flavus, and S. brevicaulis).

FR901379 is an echinocandin-like antifungal lipopeptide.1 It is active against C. albicans, C. krusei, C. tropicalis, C. utilis, A. fumigatus, and A. niger fungi (IC50s = <0.003-1.9 μg/ml). FR901379 is protective against C. albicans infection in mice (ED50 = 1.1 mg/kg). It also reduces the number of pulmonary cysts and trophozoites in a mouse model of P. carinii infection. |1. Fujie, A., Iwamoto, T., Sato, B., et al. FR131535, a novel water-soluble echinocandin-like lipopeptide: Synthesis and biological properties. Bioorg. Med. Chem. Lett. 11(3), 399-402 (2001).

IKD-8344 is a macrocyclic dilactone originally isolated from an actinomycete species with diverse biological activities, including anticancer, antimicrobial, and anthelmintic properties [1,2,3]. It is cytotoxic to L5178Y murine leukemia cells (IC50 = 0.54 ng/ml) [1], inhibits growth of the mycelial form of C. albicans (MIC = 6.25 μg/ml), and potentiates the activity of polymyxin B against the multidrug-resistant pathogenic bacterium B. cenocepacia [2,3]. Additionally, it is active against T. spiralis in vitro and in vivo [1].