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Future and Novel Unexplored Indications of Retinoids
Published in Ayse Serap Karadag, Berna Aksoy, Lawrence Charles Parish, Retinoids in Dermatology, 2019
Retinyl propionate has been shown to reduce photoaging (100), especially in combination with climbazole, which boosts retinoid-related activity (101). A number of studies have used the “alternative topical retinoids.” One study evaluated the effectiveness and tolerability of a double-conjugate retinoid cream (AlphaRet Overnight Cream; AHA-Ret) in diminishing visible signs of photoaging versus 1.0% retinol or 0.025% tretinoin, and found that the use of the medication lead to early reductions in photodamage and improvements in hydration while inducing less erythema versus retinol and more tolerability versus retinol and tretinoin (102). Another study found that retinaldehyde 0.1% and 0.05% creams were well tolerated and improved skin hydration and texture; however, only retinaldehyde 0.1% cream improved the melanin index (103). It would have been more clinically relevant if a comparison with tretinoin was performed with all these “alternative retinoids” in aging when possibly there may not be an equivalent effect.
Hair cosmetology
Published in Pierre Bouhanna, Eric Bouhanna, The Alopecias, 2015
Claude Bouillon, Michèle Verschoore
Efficient and safe antifungal agents are available, mainly zinc pyrithione (ZPT), piroctone olamine, selenium sulfide, climbazole, and ketoconazole, used at 0.5–1.5 g% in anti-dandruff shampoos. Regular application (i.e., twice a week) of such active ingredients within a mild cleansing base significantly eliminates the symptoms and improves scalp condition.
Advances in the discovery of exosome inhibitors in cancer
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Huarui Zhang, Jun Lu, Jin Liu, Ge Zhang, Aiping Lu
Amrita et al. screened four currently existed compounds that can selectively inhibit the biogenesis and secretion of exosome to slow down cancer progression16. The first one, tipifarnib, is a potent farnesyl transferase inhibitor, it can interfere cell growth and induce cell apoptosis14,15. Its exosome inhibitory effect was evident, data showed that the level of exosome released from PCa cells which exposed to 0.25–1 μM of tipifarnib was significantly decreased. The underpinning mechanism of tipifarnib is inhibiting the expression of RAB27A, Alix and nSMase219. Additionally, the inhibitory effect of tipifarnib may be selective for cancer cells, because it only affects exosome release in C4-2B and PC-3 cells but not in the RWPE-1 cells (Human Prostate Epithelial cells). This property is crucial for the clinical use of exosome inhibitors. The interactions between tipifarnib and RAB27A are shown in Figure 1. The inhibitory effects of neticonazole and climbazole were also measured, both of them (20 µM) could significantly decrease exosome secretion by downregulating the level of Alix and Rab27a, additionally neticonazole also decreased nSMase2 levels. This team also screened a compound that has currently been approved by the United States for PCa patients, ketoconazole, could inhibit exosome release17. Ketoconazole (5 μM) decreased the level of exosome produced by C4-2B cells and PC-3 cells, and increasing concentrations (0–5 μM) led to a robust dose-dependent decrease in RAB27A, Alix and nSMase2 in both C4-2B and PC-3 cells, but not in the RWPE-1 cells. Interestingly, although the structures of these four compounds are different from each other, they all have the same parts, diazole and aromatic moiety, which suggests the importance of both to the structure of the drugs. Furthermore, the activities of these compounds are quite different, the efficacy of tipifarnib is much more active than the other three compounds.