Sideritis Perfoliata (Subsp. Perfoliata) Nutritive Value and Its Potential Medicinal Properties.

Sideritis perfoliata L. subsp. perfoliata is an endemic species of the Eastern Mediterranean region with several uses in traditional medicine. The present study aims to explore the unknown properties of S. perfoliata investigating the nutritional content as well as the antioxidant, anticancer, antituberculosis, antiwrinkle, anti-acne, hyper/hypo-pigmentation and antibacterial activities. Mineral content, nutritional value, the composition and antioxidant properties of the essential oil, the antityrosinase, the antibacterial activity and anti-elastase potential of the extract, were evaluated. The antiproliferative activity of S. perfoliata against cervical cancer (HeLa), human melanoma (UCT-Mel-1), human hepatocellular carcinoma (HepG2) and human epidermoid carcinoma (A431) was investigated. Cytotoxic effects on normal human keratinocyte (HaCat) and kidney epithelial (Vero) cell lines were also determined. Sideritis perfoliata exhibited high nutritional value of proteins and minerals (K, P, Mg, Fe, Zn, Cu). The most abundant components of the essential oil were found to be α-pinene, ß-phelladrene, valeranone, ß-pinene and sabinene. The ethanolic extract of S. perfoliata displayed moderate antioxidant potential and antibacterial activity against Prevotella intermedia. Noteworthy elastase and moderate anticancer potential against the human liver cancer cell line (HepG2) was observed with IC50 values of 57.18 ± 3.22 µg/mL and 64.27 ± 2.04 µg/mL respectively. The noteworthy in vitro activity of S. perfoliata could be due to the presence of flavonoids and phenols in the leaves, having high nutritional value. Sideritis perfoliata could potentially be useful to reduce the appearance of wrinkles and for the treatment of liver cancer. The moderate antibacterial, antioxidant and elastase activity of the plant can be linked to the traditional use of S. perfoliata for the treatment of wounds and inflammation.

In Vitro Antioxidant, Anti-Inflammatory and Skin Permeation of Myrsine africana and Its Isolated Compound Myrsinoside B.

Dermal aging is characterized by states of oxidative stress, chronic inflammation, and abnormal proteolytic degradation due to the action of hydrogen peroxide, superoxide, 5-lipoxygenase, and elastase, respectively. Noteworthy elastase inhibition has previously been reported, and so this study aimed to investigate the ability of Myrsine africana and myrsinoside B to reduce the activity of hydrogen peroxide, superoxide, and 5-lipoxygenase as supplementary mechanisms of action by which M. africana may reduce the appearance of wrinkles. The use of maltose microneedles were also investigated as a means to enhance the delivery of myrsinoside B into the skin as this is a crucial aspect to investigate when characterizing the efficacy of an active ingredient. Myrsine africana has traditionally been used for skin allergies, boils, and to purify blood (as an astringent) and was selected for this study based on it use in skincare. The crude extract exhibited IC50's of 56.08 ± 2.88 and 132.74 ± 1.64 µg/ml against the hydrogen peroxide and superoxide radicals, while myrsinoside B exhibited IC50's of 52.19 ± 4.16 and 192.14 ± 3.52 µg/ml, respectively. The IC50 of the extract and compound against 5-lipoxygenase was 29.65 ± 2.92 and 29.33 ± 3.08 µg/ml, respectively. No toxicity was observed in vitro at the highest concentration tested. Microneedle treatment increased the permeation of the active through the skin after 24 h to 12.46 ± 5.14 µg/cm2 compared to the passive group (1.30± 0.85 µg/cm2). The amount of active retained in the epidermis and dermis was 8.97 ± 0.90 and 6.98 ± 0.73 µg/cm2 respectively, greater than the retention observed in the passive group (3.24 ± 1.41 and 3.27 ± 1.47 µg/cm2, respectively). M. africana and myrsinoside B showed promising antioxidant and anti-inflammatory activity thus supporting the potential of M. africana and myrsinoside B as anti-wrinkle agents. Further, treatment of dermatomed human skin with maltose microneedles facilitated topical delivery of myrsinoside B and provided an effective means for compound delivery to ensure maximum effect.

Selected essential oils inhibit key physiological enzymes and possess intracellular and extracellular antimelanogenic properties in vitro.

Essential oils (EOs) extracted from six medicinal herbs and food plants [Cinnamomum zeylanicum (CZ), Psiadia arguta (PA), Psiadia terebinthina (PT), Citrus grandis (CGp), Citrus hystrix (CH), and Citrus reticulata (CR)] were studied for any inhibitory potential against key physiological enzymes involved in diabetes (α-glucosidase), skin aging (collagenase and elastase), and neurodegenerative disorders (acetylcholinesterase). Kinetic studies of the active EOs on the aforementioned enzymes were determined using Lineweaver-Burk plots. The intracellular and extracellular antimelanogenic potential of the EOs were evaluated on B16F10 mouse melanocytes. CH and CR were found to significantly inhibit (2.476 ± 0.13 µg/mL and 3.636 ± 0.10 µg/mL, respectively) acetylcholinesterase, compared with galantamine (3.989 ± 0.16 µg/mL). CH inhibited collagenase (50% inhibitory concentration 28.71 ± 0.16 µg/mL) compared with the control (24.45 ± 0.19 µg/mL). The percentage inhibition in the elastase assay of CH was 63.21% compared to the positive control (75.09%). In addition, CH, CR, CGp, CZ, and PT were found to significantly inhibit α-glucosidase (276.70 ± 0.73 µg/mL, 169.90 ± 0.58 µg/mL, 240.60 ± 6.50 µg/mL, 64.52 ± 0.69 µg/mL, and 313.0 ± 5.0 µg/mL, respectively), compared to acarbose (448.80 ± 0.81 µg/mL). Active EOs showed both uncompetitive and competitive types of inhibition. The EOs also inhibited intracellular (50% inhibitory concentration 15.92 ± 1.06 µg/mL, 23.75 ± 4.47 µg/mL, and 28.99 ± 5.70 µg/mL for CH, CR, and CGp, respectively) and extracellular (< 15.625 µg/mL for CH, CR, CGp, and PT) melanin production when tested against B16F10 mouse melanocytes. Results from the present study tend to show that EOs extracted from these medicinal plants can inhibit key enzymes and may be potential candidates for cosmetic and pharmaceutical industries.

In vitro and In vivo Activity of Myrsine africana on Elastase Inhibition and Anti-wrinkle Activity.

BACKGROUND: Myrsine africana (MA) is a plant traditionally used in South Africa to treat various diseases. OBJECTIVE: The ethanolic extract of MA, was used for in vitro and in vivo studies to determine its elastase inhibitory activity. MATERIALS AND METHODS: MA and its isolated compound, myrsinoside B, were tested in vitro for their elastase inhibitory activity. The MA extract was also evaluated for mutagenicity using two strains of Salmonella typhimurium (TA 98 and TA 100), microbial count, metal analysis, and stability. In vivo studies included irritancy and wrinkle reduction trials using Visioscan and Visioface. RESULTS: The leaf extract showed good elastase inhibition with a 50% inhibitory concentration (IC50) of 28.04 µg/ml. Myrsinoside B inhibited the elastase enzyme at an IC50 of 4.68 ± 0.34 µg/ml. No colony growth observed during mutagenicity studies and it was concluded that MA ethanolic extract is a nonmutagen. MA extract was found to be a nonirritant during the patch test clinical trial. MA was found to contain negligible amounts of microorganisms and heavy metals. Gel cream containing MA crude extract was found to be stable for 2 years when kept at temperatures below 30°C. In clinical trials (in vivo), it was found that the test product containing 5% ethanolic extract of MA was effective in reducing wrinkles after application 2 times a day for 14 days and 28 days compared to the placebo aqueous cream. CONCLUSION: MA is effective in reducing the appearance of wrinkles. SUMMARY: This is a first time report of the elastase inhibitory potential of Myrsine africana and myrsinoside B and the anti-wrinkle potential of Myrsine africanaMyrsine africana ethanolic extract effectively inhibited the elastase enzymeMyrsine africana was effective in in vivo studies to reduce the appearance of wrinkles after 14 days. Abbreviations used: 4-NQO: 4-nitroquinoline, D14-BL: Baseline to day fourteen, D28-BL: Baseline to day twenty-eight, CFU: Colony forming units, IC50: 50% inhibitory concentration, MA: Myrsine africana, MOU: Measurement of uncertainty, NaCl: Sodium chloride, NaH2 PO4.H2O: Sodium phosphate monobasic monohydrate, SEM: Standard error of the mean, TA 98: Salmonella typhimurium strain 98, TA 100: S. typhimurium strain 100, TLC: Thin layer chromatography, TMA: Total microbial activity, XVB salt: Vogel-Bonner medium E.