ALKALOIDS IN COSMETICS 237 extracts (Capsicum annuum L.) in concentration 100 mg/L have antibacterial activity against strains of Staphylococcus aureus, Salmonella typhimurium, and Vibrio cholerae. The concentration of capsaicin in the extract and IC 50 was not reported in the quoted article (42). Therefore, capsaicin can be considered a natural preparation with antimicrobial ac- tivity against selected bacterial strains. BERBERIN E IN COSMETICS Berberin e is an isoquinoline alkaloid present in the bark, root, and other organs of the species barberries (Berberis vulgaris) and goldenseal (Hydrastis canadensis). Berberine is ob- tained in the cosmetic industry also from roots and aerial parts of the abuta plant (Abuta grandifolia) (Figure 3) (43,44). Berberine at concentrations of 50, 100, and 200 μg/mL displayed a signifi cant antibacterial and antifungal activity against Staphylococcus aureus and different Candida spp. A decoction of the bark of this raw material is recommended in the treatment of mycosis of the skin (45). According to Cernáková and Kostálová (46), berberine was found to be moderately active against the tested bacteria, yeasts, and fungi. IC50 for S. aureus was 14.6 mg/L, for B. subtilis 143 mg/L, for P. aeruginosa S 39.8 mg/L, for P. aeruginosa 99.2 mg/L, for E. coli S 73.2 mg/L, for E. coli R 87.0 mg/L, and for Z. ramigera 145 mg/L. They tested different concentrations of berberine in the solid medium being 0 (control), 100, 250, 500, and 1,500 mg/L. Gram-positive and Gram- negative bacteria were grown in peptone water during static culture. The cultivation lasted 1 d at 37°C. The evaluation was performed by reading A630 after 1 d (for bacteria) and 2 d (for yeasts) the percent growth was calculated by comparing to A630 of the cor- responding control. The research has shown that berberine chloride inhibits activity Gram-positive bacteria stronger than Gram-negative bacteria, whereas antifungal prop- erties of this compound are based on the cell membrane damage (45,47). Berberine in a ddition to antimicrobial properties also exhibits on action anodyne, anti- infl ammatory, and antioxidative properties, and reduced pressure blood and control of cholesterol and sugar level in blood (44). Figure 3. Chemical structure of berberine (42).
JOURNAL OF COSMETIC SCIENCE 238 Berberine frui t masks are used to treat acne vulgaris as well as skin hyperpigmentation. Seki and Morohashi (48) noted that lipogenesis in the hamster sebaceous glands was sup- pressed 63% by 10-4 M berberine. They suggest that this alkaloid can be used for acne vulgaris because of inhibition of lipogenesis. Anti-infl ammato ry properties are associated with the process of inhibiting the activity of pro-infl ammatory lipoxygenase enzyme causing skin diseases (49,50). Kuo et al. (51) used cancer cell to evaluate anti-infl ammatory properties of berberine. In ca ncer cell line OC2 and KB cells, a 12-h berberine treatment (1, 10, and 100 mM) reduced prostaglan- din E2 production dose dependently with or without 12-O-tetradecanoylpho rbol- 13-acetate (TPA, 10 nM) induction. This berberine-induced effect occurred rapidly (3 h) as a result of reduced COX-2 protein. Further analysis showed that berberine inhibited activator protein 1 binding directly. Despite the evi denced potentiality of berberine in the treatment of skin diseases, its topical application is limited because of its high hydrophilicity, the approximate log p value of -1.5 hinder its delivery across the skin layers (44). According to Torky (52), to increase its dermal bioavailability, berberine can be formulated with sodium oleate as a compl exing agent. This complex displays about 250-fold higher saturation solubility in n-octanol, endorsing the improved lipid solubility of the complex compared with free alkaloid (52). They are a rich source of antioxidants. Zovko Koncic et al. (53 ) studied the antioxidant activities of the ethanolic extracts of roots, twigs, and leaves of Berberis vulgaris L. and Berberis croatica Horvat. For preparation of extracts, powdered herbal material (10 g) was extracted with 96% ethanol (50 mL) in ultrasonication bath at 45°C for 45 min. They noted that all the extracts were found to possess some radical-scavenging and antioxidant activities, as determined by the scavenging effect on the 2,2-diphenyl-1-picrylhydrazyl fre e radical, reducing power and β-carotene–linoleic acid model system. Toxicity of berberi ne depends on the route of administration and experimental animal species. The LD50 value of powdered root Berberis vulgaris is 2,600 mg/kg in mice on oral administration. On oral administration of root extract fraction of B. vulgaris, the LD50 values are 1,280 and 520 mg/kg in rat and mice, respectively. In mice, the LD50 values of pure berberine on intraperitoneal (IP) and oral administration are 23 and 329 mg/kg, respectively. Berberine sulfate isolated from Berberis aristata on IP administration in rats has LD50 value equal to 205 mg/kg (54). PIPERINE IN COSMETI CS Piperine (1-[5-(1,3 -benzodioxo-5-yl)-1-o xo-2,4-pentadienyl] piperidine) belongs to the group of piperidine alkaloids (Figure 4). Piperine can be obtained from black pepper (Piper nigrum L.). Black pepper contains approx. 2–3% of volatile oils (55) and about 5–9% of alkaloids such as piperine, piperidine, peperitin, and a who le range of other similar substances (56). The process of piperine isolation consists in the extraction of oleoresin from ground pepper with supercritical fl uid and then crystallization with etha- nol. This alkaloid can also be obtained by methods such as maceration, Soxhlet extrac- tion, or hydrotropic solubilization (57). Black pepper has a variety of physiological properties, ranging from stimulation of pan- creatic digestive enzymes, through anti-infl ammatory effects in many autoimmune
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