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Herbs with Antidepressant Effects
Published in Scott Mendelson, Herbal Treatment of Major Depression, 2019
In vivo, administration of bakuchiol to rats that had received CCl4 attenuated lipid peroxidation and intracellular glutathione depletion in hepatocytes. Reduced serum levels of aspartate transaminase and alanine transaminase demonstrated the ability of the phytochemical to spare liver tissue from the CCl4-induced oxidative damage.6
Formulated Natural Selective Estrogen Receptor Modulators: A Key To Restoring Women’s Health
Published in Megh R. Goyal, Durgesh Nandini Chauhan, Plant- and Marine-Based Phytochemicals for Human Health, 2018
A. Anita Margret, S. Aishwarya, J. Theboral
Preliminary use of estrogenic nutraceuticals is based on isoflavones, which are used to develop SERMs from plant-based HRT. Phytoestrogens from P. corylifolia revealed ER-subtype selectivity in breast cancer cells. Moreover, psoralen and isopsoralen promoted the proliferation of MCF-7 cells, which confirmed the selectivity for ERs. Particularly, coumarin showed selectivity for ERα and flavonoids, and bakuchiol exhibit dual action on ERα and ERβ, and hence P. corylifolia may be used as a new source for SERMs.110 In another study, ER agonist activity of bakuchiol and psoralidin was further confirmed by luciferase activity, which was contributed by estrogenic transactivation. The results suggested that P. corylifolia may be valuable as a novel ER modulator and has the potential to be used in alternative HRT formulations.53 In addition to bakuchiol and psoralidin, the estrogenic activity of bavachin was characterized by ligand binding, reporter gene activation, and endogenous target gene regulation in CV-1 cells. Bavachin has the capability to increase the transcription level of estrogen-responsive genes and decrease the protein level, and hence effectively modulate cellular ER targets.76 These kinds of estrogenic activities of P. corylifolia were accomplished by the presence of bakuchiol, bavachalcone, isobavachalcone, bavachromene, and isobavachromene since they have prynylated phenolic groups. Among these compounds, bakuchiol is the key compound with five times higher estrogenic activity than other compounds, thus suggesting their use in attenuating various symptoms of estrogen deficiency in postmenopausal women.51 Corylin also has SERMlike behavior, which has not yet been studied in detail.92
Carboxylesterase Inhibitors: Relevance for Pharmaceutical Applications
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Besides the above-mentioned compounds, other compounds, including fatty acids, sterols, pyrethroids, and therapeutic drugs, also displayed strong inhibitory effects against carboxylesterase (Xu et al., 2016; Lei et al., 2017; Wang et al., 2017). Crow et al. found that most naturally occurring fatty acids strongly inhibited the hydrolytic activities of recombinant CES1, with the IC50 values at micromolar range Crow et al. (2010). Unsaturated fatty acids displayed potent inhibitory effects on CES1 than saturated ones, while they also display high specificity towards CES1 over CES2. 27-Hydroxycholesterol (27-HC), an oxidized form of cholesterol, also showed promising inhibitory activity against recombinant CES1 (IC50 46 nM) and high selectivity over CES2. 27-HC functioned as noncompetitive inhibitor against CES1, with the very low Ki value (10 nM) (Crow et al., 2010). Bakuchiol, a natural phenolic compound isolated from Fructus Psoraleae (Bu-gu-zhi in Chinese), strongly inhibited CES2 (Li et al., 2015). Pyrethroids are a class of organic compounds similar to the natural pyrethrins produced by the flowers of pyrethrums (Chrysanthemum cinerariaefolium). Pyrethroids are popular household insecticides for their relatively low toxicity to mammals in contrast to organophosphorus insecticides. Recently, Ge et al. found that six commonly used pyrethroids including deltamethrin showed moderate inhibitory effects against both CES1 and CES2 (Table 9.9) (Lei et al., 2017). Deltamethrin strongly inhibited CES1-mediated DME hydrolysis in HLM, with the IC50 value of 2.39 μM. Deltamethrin was a competitive inhibitor against CES1-mediated BMBT hydrolysis, but it functioned as a noncompetitive inhibitor against CES1-mediated DME or DMCB hydrolysis in HLM. Further investigations on inhibition kinetic analyses and docking simulations suggested that CES1 had at least two ligand-binding sites, and deltamethrin (DMT) could bind with the same ligand binding site as BMBT. Physostigmine, a natural alkaloid, was a highly specific CES2 inhibitor with the Ki value of 0.358 μM (Umehara et al., 2016). Physostigmine potently inhibited the hydrolysis of irinotecan but did not affect the hydrolysis of clopidogrel in human liver S9. By the catalytic asymmetric [3+2] cyclization of novel 4-isothiocyanato pyrazolones and isatin-derived ketimines, Wang and Zou et al. systhsized a wide range of intriguing dispirotriheterocyclic products in high yield with excellent diastereoselectivity and enantioselectivity (Bao et al., 2018). In addition, a chiral sulfoxide derivative (tert-butyl (3R,4′R)-1-benzyl-2′-((S)-methylsulfinyl)-2,5″-dioxo-1″-phenyl-3″-(p-tolyl)-1″,5″-dihydro-1′H-dispiro[indoline-3,5′-imidazole-4′, 4″-pyrazole]-1′-carboxylate) of this dispirocyclic product was identified to be a promising CES1 inhibitor. The IC50 of this chiral sulfoxide derivative was 0.39 μM, which activity was 20-fold stronger than its enantiomer.
Dermocosmetics: beneficial adjuncts in the treatment of acne vulgaris
Published in Journal of Dermatological Treatment, 2021
Elena Araviiskaia, Jose Luis Lopez Estebaranz, Carlo Pincelli
Antimicrobial agents, such as decanediol and tea tree oil, are used in dermocosmetics for acne (26–28). Decanediol has an antibacterial effect against C. acnes (29). This antibacterial action resulted in a significant reduction in pustules and sebum levels during an 8-week treatment period in patients with mild-to-moderately severe acne (29). Tea tree oil reduced the appearance and severity of both inflammatory and non-inflammatory acne lesions with few side effects (28,30). In the study by Bassett et al. (28), the onset of action for tea tree oil (5%) was slower than benzoyl peroxide (BPO); the efficacy of BPO has been well-documented in acne but is associated with skin irritation (31). Bakuchiol is another agent with antimicrobial efficacy against a number of bacteria including Staphylococcus (32,33), additional anti-aging, anti-inflammatory, photoprotective and sebum controlling effects have also been documented (34–36).