Global regulation of preservatives and cosmetic preservatives
Philip A. Geis in Cosmetic Microbiology, 2006
Humectants or hydroxy-containing compounds — Although high concentrations of propylene glycol can act as preservatives, the safety of products that contain them would prevent their marketing. The esthetics of products with glycol levels high enough to reduce water activity to sufficiently low levels to prohibit microbial growth are unacceptable to consumers. Certain products are antimicrobial and fulfill this function when used as humectants in cosmetics. They include: Farnesol, a long-chained unsaturated hydrocarbon with a terminal hydroxyl group; frequently found in fragrances; also shows activity against Gram-positive bacteria.Pentylene glycol, a 5-carbon diol, shows good broad-spectrum activity when used at levels over 2%; functions as an excellent humectant at that level.Caprylyl glycol, an 8-carbon diol exerting major activity against bacteria.1,2 Hexanediol, a 6-carbon diol, has been shown to be synergistic with pentylene glycol to offer broad-spectrum coverage and adequate humectancy.
Nanotechnology and Delivery System for Bioactive Antibiofilm Dental Materials
Mary Anne S. Melo in Designing Bioactive Polymeric Materials for Restorative Dentistry, 2020
Furthermore, NPCs were loaded with farnesol. Farnesol is an antibacterial agent that is highly effective in disrupting acid tolerance and glucan synthesis of planktonic cells of S. mutans, and is more active at acidic pH (Koo et al. 2005). However, topically applied farnesol has demonstrated limited activity against S. mutans biofilms due to the suboptimal retention and poor aqueous solubility. Thus, farnesol is an ideal model agent to demonstrate NPC efficacy, as verified previously (Chen et al. 2009). NPC can load farnesol at ~22% wt, which shows a high loading capacity. Importantly, it increases the aqueous solubility 400 times more than free farnesol. NPC-encapsulated farnesol is completely water-soluble, which is crucial for formulation development. Moreover, the release of farnesol that encapsulated within NPC can be expedited in response to acidic pH. Specifically, the initial release rate, constant and half time was 2.5 times faster at pH 4.5 vs. pH 7.2.
Metabolism of Terpenoids in Animal Models and Humans
K. Hüsnü Can Başer, Gerhard Buchbauer in Handbook of Essential Oils, 2020
Farnesol is present in many essential oils such as Cymbopogon species and neroli. It is used in perfumery and soaps to emphasize the odors of sweet floral perfumes and due to its fixative and antibacterial properties (O'Neil, 2006; Bornscheuer et al., 2014). Interestingly, it is also produced in humans where it acts on numerous nuclear receptors (Joo and Jetten, 2010). In vitro studies using recombinant drug metabolizing enzymes and human liver microsomes have shown that CYP isoenzymes participate in the metabolism of farnesol to 12-hydroxyfarnesol (Figure 10.29). Subsequently, farnesol and its metabolite are glucuronidated (DeBarber et al., 2004; Staines et al., 2004).
Design and synthesis of mucoadhesive nanogel containing farnesol: investigation of the effect on HWP1, SAP6 and Rim101 genes expression of Candida albicans in vitro
Published in Artificial Cells, Nanomedicine, and Biotechnology, 2019
Fatemeh Nikoomanesh, Shahla Roudbarmohammadi, Mehdi Khoobi, Farnoosh Haghighi, Maryam Roudbary
Farnesol is a natural organic compound which is produced from isoprene compounds in plants, animals and fungi [7]. This compound has been suggested to function as an antitumor, apoptosis-promoting effect and inducing growth-inhibitory [8,9]. In fungus such as Candida albicans, farnesol is quorum sensing molecules (QSMs) which can block filamentation and inhibit biofilm formation as well as suppressing the expression of virulence genes as along with biofilm formation [10–14]. The hyphae formation in C. albicans controlled by a network of genes includes aspartyl proteinase 6 (SAP6), Hyphal Wall Protein1 (HWP1) and Rim101 (alkaline-responsive transcriptional factor). The SAP6 gene is a member of aspartyl proteinase family known as secreted proteolytic enzymes. SAP6 and HWP1 genes are expressed strongly in germ tube and hyphal surfaces [15]. Rim101 is a transcription factor that governs virulence in many fungal pathogens. C. albicans Rim101 gene, promotes hyphal formation in response to alkaline growth conditions [16]. The importance of C. albicans hyphae formation and its role on invasion to the host cells have been well documented [17]. Therefore, effective antifungal agent and drug delivery that can prevent C. albicans hyphae form are urgently required. In our previous study by Nikoomanesh et al. [18], we showed that 300 µM concentration of farnesol was prevented from germ tube and hyphae formation of C. albicans. Hence, farnesol was deliberated as an antifungal agent by well-known mechanism. Therefore, hyphae morphology is a new target for novel drug delivery strategy.
In vivo antifungal activities of farnesol combined with antifungal drugs against murine oral mucosal candidiasis
Published in Biofouling, 2021
Chengxi Li, Zheng Xu, Siqi Liu, Yun Huang, Wei Duan, Xin Wei
The solutions for each drug were prepared following the instruction from the Clinical and Laboratory Standards Institute (CLSI) document M27 (Clinical and Laboratory Standards Institute (CLSI) 2017). The antifungal drugs included nystatin (Sigma Chemical Co.), itraconazole (Sigma Chemical Co.), and fluconazole (Sigma Chemical Co.). Stock solutions (100 mM) of farnesol ((E, E)-farnesol; Sigma Chemical Co., St Louis, MO, USA) were dissolved in 100% (v v−1) methanol and frozen at −70 °C until use. Antifungals and farnesol were added to RPMI-1640 at two-fold serially diluted concentrations. The antifungal drug concentration tested was based on previous studies: 50 μg ml−1 for nystatin (Wong et al. 2014); 0.16 mg kg−1 for itraconazole (Ishibashi et al. 2007); and 5 mg kg−1 and 35 mg kg−1 for fluconazole (Bozó et al. 2016). The concentrations tested for farnesol were 2, 4, 8, 10, 15, 20, 25, 50, and 100 μM (Katragkou et al. 2015; Kovács et al. 2016; Xia et al. 2017). Finally, the dose of farnesol administered was determined by the lowest effective concentration applied orally to Candida-infected mice when it was combined with nystatin, itraconazole, and fluconazole. All stock solutions were stored at −20 °C until use.
FXR modulators for enterohepatic and metabolic diseases
Published in Expert Opinion on Therapeutic Patents, 2018
Hong Wang, Qingxian He, Guangji Wang, Xiaowei Xu, Haiping Hao
FXR was originally known as an orphan NR. It was ‘adopted’ since the identification of farnesol and its related metabolites as their ligands. Owing to this successful identification, this NR was then named as farnesoid X-activated receptor [2]. Cafestol is the most potent cholesterol-elevating compound and several genes involved in cholesterol homeostasis, including CYP7A1, have previously been shown to be regulated by cafestol. Further studies demonstrate that cafestol is an agonist of FXR. Interestingly, cafestol does not affect FXR target genes in the liver but does increase expression of IBABP and FGF15 in the intestine, indicating that cafestol is an intestine-restricted FXR agonist like Fex [80]. Forskolin, a sterol bronchodilatory drug, has been proven to be a FXR agonist, which is more powerful than BAs with a 880-fold increase in FXR agonism [81].
Related Knowledge Centers
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