c. albicans

Fluconazole (UK-49858) is a triazole antifungal agent used to treat oropharyngeal candidiasis and cryptococcal meningitis in AIDS.

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.

1. Citric acid (Citro) (1-2 g kg) can decrease brain lipid peroxidation and inflammation, liver damage, and DNA fragmentation. 2. Citric acid denture cleansers can reduce C. albicans biofilm accumulation and cell viability. However, this CT did not prevent biofilm recolonization.

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

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.

Rezafungin (SP-3025) is a broad-spectrum and long-lasting echinocandin with potent antifungal activity against Candida, Aspergillus and Pneumocystis.

(+)-Magnoflorine (Thalictrin) has sedative and anxiolytic effects, probably mediated by Magnoflorine through a GABAergic mechanism of action. Magnoflorine and Sinomenine have protective effects, are mediated by some mechanism other than prevention of micelle formation or protection of the erythrocyte membrane against osmotic imbalance.

AN2718 inhibits protein synthesis through the OBORT mechanism and displays broad antifungal effectiveness.

Pachybasin is an anthraquinone fungal metabolite. Pachybasin shows antimicrobial activities against E. coli, B. subtilis, M. luteus, S. cerevisiae, C. albicans, A. niger, and A. flavus, with MIC values of 64.0 μg mL, and against S. aureus and F. oxysporum with MIC values of 32.0 and 16.0 μg mL respectively.

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 exhibits both antifungal and anti-arthritic activities, potentially serving as a combination therapy for fungal arthritis caused by C. albicans infection.

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.

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.

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 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts. It inhibits the growth of the periodontopathogenic and cariogenic bacteria F. nucleatum, S. mutans, S. sobrinus, S. salivarius, and L. casei (MICs = 12.5-100 mg/l). It also inhibits the growth of S. aureus, S. pyogenes, P. aeruginosa, E. coli, and C. albicans. β-Defensin-3 stimulates gene expression and production of IL-6, IL-10, CXCL10, CCL2, MIP-3α, and RANTES by keratinocytes when used at a concentration of 30 μg/ml. It also stimulates calcium mobilization, migration, and proliferation of keratinocytes when used at concentrations of 30, 5, and 20 μg/ml, respectively. β-Defensin-3 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.

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].

Emestrin, a mycotoxin originally isolated from *E. striata*, exhibits antimicrobial, immunomodulatory, and cytotoxic activities. It is effective against fungi *C. albicans* and *C. neoformans*, and bacteria *E. coli*, *S. aureus*, and methicillin-resistant *S. aureus* (MRSA; IC50s = 3.94, 0.6, 2.21, 4.55, and 2.21 μg ml, respectively). Emestrin acts as a chemokine (C-C motif) receptor 2 (CCR2) antagonist (IC50 = 5.4 μM in a radioligand binding assay using isolated human monocytes). At 0.1 μg ml, it induces apoptosis in HL-60 cells and causes necrosis in heart, thymus, and liver tissues in mice at doses of 18-30 mg kg.

Linearmycin A is a polyene antibiotic found in [Streptomyces]. It exhibits activity against bacteria [S. aureus] and [E. coli] (MICs = 3.1 and 1.6 μg disc, respectively), fungi [S. cerevisiae] and [C. albicans] (MICs = 0.1 and 1.6 μg disc, respectively), and the plant pathogenic fungus [A. niger] (MIC = 0.2 μg disc) in disc assays. Linearmycin A also induces lysis and degradation of [B. subtilis] as a component of [Streptomyces Mg1] extract.

D13 is an acylhydrazone antifungal.1 It is active against C. neoformans in vitro (MIC80 = 0.06 μg/ml). D13 (20 mg/kg per day, p.o.) increases survival in mouse models of C. neoformans, C. albicans, or A. fumigatus infection. |1. Lazzarini, C., Haranahalli, K., Rieger, R., et al. Acylhydrazones as antifungal agents targeting the synthesis of fungal sphingolipids. Antimicrob. Agents Chemother. 62(5), e00156-00118 (2018).

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]

Terpendole I is a fungal metabolite that has been found in A. yamanashiensis.1 It is a weak inhibitor of acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 145 μM) and is active against the bacteria B. cereus and B. subtilis (MICs = 100 μg/ml for both) but not S. aureus, P. aeruginosa, or K. pneumoniae (MICs = >200 μg/ml for all) or the fungus C. albicans (MIC = 200 μg/ml).1,2 It is cytotoxic to HeLa cells with an IC50 value of 52.6 μM.3 |1. Tomoda, H., Tabata, N., Yang, D.-J., et al. Terpendoles, novel ACAT inhibitors produced by Albophoma yamanashiensis. III. Production, isolation and structure elucidation of new components. J. Antibiot. (Tokyo) 48(8), 793-804 (1995).|2. Zhao, J.-C., Wang, Y.-L., Zhang, T.-Y., et al. Indole diterpenoids from the endophytic fungus Drechmeria sp. as natural antimicrobial agents. Phytochemistry 148, 21-28 (2018).|3. Nagumo, Y., Motoyama, T., Hayashi, T., et al. Structure-activity relationships of terpendole E and its natural derivatives. ChemistrySelect 2(4), 1533-1536 (2017).