< em > Capsicum annuum < /em > Oleoresin Nanoemulgel - Design Characterization and < em > In vitro < /em > Investigation of Anticancer and Antimicrobial Activities
CONCLUSION: C. annuum oleoresin and its nanoemulgel can be considered valuable sources for the discovery of new antibacterial, antifungal, and anticancer compounds in the pharmaceutical industry, especially due to their potent activity against various cancer cell lines as well as bacterial and fungal strains.PMID:38532324 | DOI:10.2174/0113816128283684231220062019 (Source: Current Pharmaceutical Design)
Source: Current Pharmaceutical Design - March 27, 2024 Category: Drugs & Pharmacology Authors: Ahmad M Eid Hiba Natsheh Linda Issa Majdulin Zoabi Monia Amer Effat Mahamid Ahmed Mousa Source Type: research

Pore-forming peptide C14R exhibits potent antifungal activity against clinical isolates of Candida albicans and Candida auris
DiscussionC14R has a potent antifungal activity against a large set of clinical isolates of both C. albicans and C. auris, showing its capacity to disrupt Candida membranes. This antifungal activity remains consistent across isolates regardless of their clinical source. Furthermore, the absence of correlation between MICs to C14R and resistance to fluconazole indicates the peptide’s potential effectiveness against fluconazole-resistant strains. Our results suggest the potential of C14R, a pore-forming peptide, as a treatment option for fungal infections, such as invasive candidiasis, including fluconazole and amphoterici...
Source: Frontiers in cellular and infection microbiology - March 27, 2024 Category: Microbiology Source Type: research

Antifungal activity of ruthenium (II) complex combined with fluconazole against drug-resistant Candida albicans in vitro and its anti-invasive infection in vivo
J Inorg Biochem. 2024 Mar 12;255:112522. doi: 10.1016/j.jinorgbio.2024.112522. Online ahead of print.ABSTRACTWith the abuse of antibiotics and azoles, drug-resistant Candida albicans infections have increased sharply and are spreading rapidly, thereby significantly reducing the antifungal efficacy of existing therapeutics. Several patients die of fungal infections every year. Therefore, there is an urgent requirement to develop new drugs. Accordingly, we synthesized a series of polypyridyl ruthenium (II) complexes having the formula [Ru (NN)2 (bpm)] (PF6)2 (N-N = 2,2'-bipyridine) (bpy, in Ru1), 1,10-phenanthroline (phen, i...
Source: Journal of Inorganic Biochemistry - March 24, 2024 Category: Biochemistry Authors: Zhi-Chang Xu Xiu-Rong Ma Li-Juan Zhang Hui-Ting Chen Ding-Mei Qing Rong-Tao Li Rui-Rong Ye Rui-Rui Wang Source Type: research

Antifungal activity of ruthenium (II) complex combined with fluconazole against drug-resistant Candida albicans in vitro and its anti-invasive infection in vivo
J Inorg Biochem. 2024 Mar 12;255:112522. doi: 10.1016/j.jinorgbio.2024.112522. Online ahead of print.ABSTRACTWith the abuse of antibiotics and azoles, drug-resistant Candida albicans infections have increased sharply and are spreading rapidly, thereby significantly reducing the antifungal efficacy of existing therapeutics. Several patients die of fungal infections every year. Therefore, there is an urgent requirement to develop new drugs. Accordingly, we synthesized a series of polypyridyl ruthenium (II) complexes having the formula [Ru (NN)2 (bpm)] (PF6)2 (N-N = 2,2'-bipyridine) (bpy, in Ru1), 1,10-phenanthroline (phen, i...
Source: Journal of Inorganic Biochemistry - March 24, 2024 Category: Biochemistry Authors: Zhi-Chang Xu Xiu-Rong Ma Li-Juan Zhang Hui-Ting Chen Ding-Mei Qing Rong-Tao Li Rui-Rong Ye Rui-Rui Wang Source Type: research

Pharmacology and pharmacokinetics of tazemetostat
AbstractTazemetostat, a novel oral selective inhibitor of enhancer of zeste homolog 2 (EZH2), was approved by the Food and Drug Administration (FDA) in 2020 for use in patients with advanced epithelioid sarcoma or relapsed/refractory (R/R) EZH2-mutated follicular lymphoma. These indications were approved by the FDA trough accelerated approval based on objective response rate and duration of response that resulted from phase 2 clinical trials. Tazemetostat competes with S-adenosylmethionine (SAM) cofactor to inhibit EZH2, reducing the levels of trimethylated lysine 27 of histone 3 (H3K27me3), considered as pharmacodynamic m...
Source: Cancer Chemotherapy and Pharmacology - March 23, 2024 Category: Cancer & Oncology Source Type: research

Anti-fungal effects of novel N-(tert-butyl)-2-(pyridin-2-yl)imidazo[1,2-a]pyridin-3-amine derivative and it's in-vitro, in-silico, and mode of action against Candida spp
In this study, two newly synthesized imidazo[1,2-a]pyridine derivative (Probe I and Probe II) molecules were investigated for its antimicrobial potency against of a panel of bacterial (Gram-positive and Gram-negative bacteria) and fungal pathogens. Among the different types of pathogens, we found that Probe II showed excellent antifungal activity against fungal pathogens, based on the preliminary screening the potent molecule further investigated against multidrug-resistance Candida sp. (n = 10) and compared with commercial molecules. In addition, in-silico molecular docking, its dynamics, absorption, distribution, metabol...
Source: Archives of Microbiology - March 21, 2024 Category: Microbiology Authors: Manivannan Nandhagopal Ramanjaneyulu Mala Kanagasabai Somarathinam Divya Dhakshinamurthy Mathivanan Narayanasamy Priyadharshni Vijayan Manimuthu Mani Shankar Source Type: research

Anti-fungal effects of novel N-(tert-butyl)-2-(pyridin-2-yl)imidazo[1,2-a]pyridin-3-amine derivative and it's in-vitro, in-silico, and mode of action against Candida spp
In this study, two newly synthesized imidazo[1,2-a]pyridine derivative (Probe I and Probe II) molecules were investigated for its antimicrobial potency against of a panel of bacterial (Gram-positive and Gram-negative bacteria) and fungal pathogens. Among the different types of pathogens, we found that Probe II showed excellent antifungal activity against fungal pathogens, based on the preliminary screening the potent molecule further investigated against multidrug-resistance Candida sp. (n = 10) and compared with commercial molecules. In addition, in-silico molecular docking, its dynamics, absorption, distribution, metabol...
Source: Archives of Microbiology - March 21, 2024 Category: Microbiology Authors: Manivannan Nandhagopal Ramanjaneyulu Mala Kanagasabai Somarathinam Divya Dhakshinamurthy Mathivanan Narayanasamy Priyadharshni Vijayan Manimuthu Mani Shankar Source Type: research

Synthesis, structure-activity relationship and biological evaluation of indole derivatives as anti-Candida albicans agents
Bioorg Chem. 2024 Mar 16;146:107293. doi: 10.1016/j.bioorg.2024.107293. Online ahead of print.ABSTRACTIn this work, we synthesized a series of indole derivatives to cope with the current increasing fungal infections caused by drug-resistant Candida albicans. All compounds were evaluated for antifungal activities against Candida albicans in vitro, and the structure-activity relationships (SARs) were analyzed. The results indicated that indole derivatives used either alone or in combination with fluconazole showed good activities against fluconazole-resistant Candida albicans. Further mechanisms studies demonstrated that com...
Source: Bioorganic Chemistry - March 20, 2024 Category: Chemistry Authors: Yandan Wu Aimei Sun Fei Chen Yin Zhao Xianhu Zhu Tianbao Zhang Guanghui Ni Ruirui Wang Source Type: research

Synthesis, structure-activity relationship and biological evaluation of indole derivatives as anti-Candida albicans agents
Bioorg Chem. 2024 Mar 16;146:107293. doi: 10.1016/j.bioorg.2024.107293. Online ahead of print.ABSTRACTIn this work, we synthesized a series of indole derivatives to cope with the current increasing fungal infections caused by drug-resistant Candida albicans. All compounds were evaluated for antifungal activities against Candida albicans in vitro, and the structure-activity relationships (SARs) were analyzed. The results indicated that indole derivatives used either alone or in combination with fluconazole showed good activities against fluconazole-resistant Candida albicans. Further mechanisms studies demonstrated that com...
Source: Bioorganic Chemistry - March 20, 2024 Category: Chemistry Authors: Yandan Wu Aimei Sun Fei Chen Yin Zhao Xianhu Zhu Tianbao Zhang Guanghui Ni Ruirui Wang Source Type: research

Evaluating cardiac disorders associated with triazole antifungal agents based on the US Food and Drug Administration Adverse Event reporting system database
Conclusion:Isavuconazole might be the safest of the five TAAs for cardiac AEs. TAA-associated cardiac disorders may result in serious adverse outcomes. Therefore, in addition to AEs on the drug label, we should pay attention to new AEs unrecorded on the drug label during the clinical use of TAAs. (Source: Frontiers in Pharmacology)
Source: Frontiers in Pharmacology - March 20, 2024 Category: Drugs & Pharmacology Source Type: research

Comparing the efficacy of fluconazole and cryotherapy Versus cryotherapy alone on treating cutaneous leishmaniasis: a triple-blind randomized clinical trial
This study aimed t... (Source: BMC Infectious Diseases)
Source: BMC Infectious Diseases - March 20, 2024 Category: Infectious Diseases Authors: Ahmad Reza Parhizkar, Mehdi Sharafi, Susan Mansuri, Maryam Hadibarhaghtalab, Sima Afrashteh, Hossein Fatemian and Mahsa Rostami Chijan Tags: Research Source Type: research

Evaluation of the Vitek 2 system for antifungal susceptibility testing of Candida auris using a representative international panel of clinical isolates: overestimation of amphotericin B resistance and underestimation of fluconazole resistance
Journal of Clinical Microbiology, Ahead of Print. (Source: Journal of Clinical Microbiology)
Source: Journal of Clinical Microbiology - March 19, 2024 Category: Microbiology Authors: Maria SiopiIoannis PachoulisSevasti LeventakiBram SpruijtenburgJacques F. MeisSpyros PournarasGeorgia VrioniAthanasios TsakrisJoseph Meletiadis1Clinical Microbiology Laboratory, “Attikon” University General Hospital, Medical School, National and Kapod Source Type: research

Antifungal therapy for the treatment of CNS infections
AbstractPurpose of reviewA review of existing and emerging therapies for the treatment of fungal infections of the CNS is presented, highlighting more recent studies. Newly authorized and emerging therapies and the data surrounding their use are also introduced.Recent findingsEarly data suggests Ibrexafungerp, a newly released antifungal for the treatment of vulvovaginal candidiasis, does not have a significant role in the treatment of CNS infections. Combination therapy including therapy with terbinafine appears promising for difficult-to-treat fungal infections of the CNS. Antifungal treatment remains pathogen-specific b...
Source: Current Fungal Infection Reports - March 16, 2024 Category: Infectious Diseases Source Type: research

A physiologically ‐based pharmacokinetic/pharmacodynamic modeling approach for drug–drug‐gene interaction evaluation of S‐warfarin with fluconazole
This study provides a whole-body physiologically-based pharmacokinetic/PD (PBPK/PD) model of S-warfarin for predicting the effects of drug–drug−gene interactions on S-warfarin PKs and PDs. The PBPK/PD model of S-warfarin was developed in PK-Sim and MoBi. Drug-depende nt parameters were obtained from the literature or optimized. Of the 34 S-warfarin plasma concentration-time profiles used, 96% predicted plasma concentrations within twofold range compared to observed data. For S-warfarin plasma concentration-time profiles withCYP2C9 genotype, 364 of 386 predicted plasma concentration values (~94%) fell within the twofold...
Source: CPT: Pharmacometrics and Systems Pharmacology - March 15, 2024 Category: Drugs & Pharmacology Authors: Kuo Geng, Chaozhuang Shen, Xiaohu Wang, Xingwen Wang, Wenxin Shao, Wenhui Wang, Tao Chen, Hua Sun, Haitang Xie Tags: ARTICLE Source Type: research

Natural Isatin Derivatives Against Black Fungus: In Silico Studies
Curr Microbiol. 2024 Mar 12;81(5):113. doi: 10.1007/s00284-024-03621-z.ABSTRACTDuring this coronavirus pandemic, when a lot of people are already severely afflicted with SARS-CoV-19, the dispersion of black fungus is making it worse, especially in the Indian subcontinent. Considering this situation, the idea for an in silico study to identify the potential inhibitor against black fungal infection is envisioned and computational analysis has been conducted with isatin derivatives that exhibit considerable antifungal activity. Through this in silico study, several pharmacokinetics properties like absorption, distribution, me...
Source: Current Microbiology - March 13, 2024 Category: Microbiology Authors: Md Saddam Hossain Md Anisur Rahman Prithbey Raj Dey Md Parvez Khandocar Md Yeakub Ali Mahajabin Snigdha Henrique Douglas Melo Coutinho Muhammad Torequl Islam Source Type: research