No description available.

Four endemic medicinal plants from the Yucatan peninsula belonging to genera with little pharmacological and phytochemical reported information and used for medicinal purposes by local communities were selected. The species selected included Jacquinia flammea Millsp. ex Mez, Sideroxylon foetidissimum Jacq. subsp. gaumeri, Serjania yucatanensis Standl., and Serjania adiantoides Radlk. The root, stem/bank and leaves of each plant species were extracted using ethanol and the resulting crude extracts were tested for their cytotoxic effect using the modified MTT (3-[4,5-Dimethylthiazol-2-yl]-2,5-diphenyl-tetrazolium bromide) assay followed by a bioassay-guided fractionation of the most active extracts in order to identify the active metabolites. The initial cytotoxic evaluation against HeLa cells at two fixed concentrations (100 and 33.3 µg/mL) identified the root extracts f J. flammea, S. foetidissimum subsp. gaumeri and S. yucatanensis, and the stem/bank extract of S. adiantoides as the most active extracts. The crude extract of roots of J. flammea was subjected to solvent partition using solvents of ascending polarity (pet. ether, CHCI3, EtOAc, BuOH and water). The resulting fractions were tested for their cytotoxic activity. The water fraction of the solvent partition showed the strongest activity against HeLa cells (IC50 = 28.61 ± 2.27 µg/mL). When tested against RAW 264.7 cells, the water fraction also showed significant activity (IC50 = 10.60 ± 1.83 µg/mL). The water fraction was subjected to chromatographic fractionation using open silica gel columns resulting in the isolation of a saponin as the most active metabolite against RAW 264.7 cells (IC50 = 4.76 ± 0.32 µg/mL). The isolated compound was identified using 1D (1H and 13C and DEPT-135) and 2D (COSY, HMBC, HSQC and NOESY and ROESY) NMR and mass spectrometry analysis as sakurasosaponin. The molluscicidal and antifungal activities of sakurasosaponin have been reported but no studies on its cytotoxic activity have been previously reported. The crude extract of roots of S. foetidissimum subsp. gaumeri was subjected to solvent partition using solvents of ascending polarity (pet. ether, CHC13, EtOAc, and BuOH). The resulting fractions were tested for their cytotoxic activity. The BuOH extract of S. foetidissimum subsp. gaumeri showed the strongest activity against RAW 264.7 cells (IC50 = 35.12 ± 4.32 µg/mL) and it was subjected to further chromatographic fractionation using open silica gel columns yielding mixtures of saponin-containing fractions. The crude extract of roots of S. yucatanensis was subjected to solvent partition using solvents of ascending polarity (pet. ether, CHCI3, EtOAc, and BuOH). The resulting fractions were tested for their cytotoxic activity. The crude extract of S. adiantoiodes did not show cytotoxic activity when tested against RAW 264.7 cells.

In Thailand, Acanthus ebracteatus Vahl and Clerodendrum petasites S. Moore have been prescribed to treat skin diseases, such as rash, abscess, and urticaria, for at least 30 years. However, there is limited scientific support and no clinical trials that identify and verify the compounds that elicit useful pharmacological effects following their topical delivery. Vanillic acid was identified for the first time in A. ebracteatus together with verbascoside; furthermore, nine phenolic compounds, vanillic acid, 4-coumaric acid, ferulic acid, verbascoside, nepetin, luteolin, chrysin, naringenin, and hesperetin, and two reported, apigenin and hispidulin, were found in C. petasites. C. petasites (CP) was therefore chosen as the principal plant to be studied in this thesis. Hispidulin was quantified as a predominant compound, being present at 39 μmol/g (1.2% w/w) in a dried ethanolic extract. Various formulations of CP extracts were examined (a) in in vitro skin penetration experiments using Franz diffusion cells, and (b) in vivo using the tape-stripping method. Hispidulin penetrated through the skin within 3 hours; vanillic acid and nepetin were absorbed after 6 hours. In contrast, verbascoside was only taken up into the superficial layers of SC. There was no difference in the permeation of hispidulin, nepetin and vanillic acid from 10% w/w CP cream and lotion formulations. Hispidulin was percutaneously absorbed through the skin and taken up into the stratum corneum in the greatest amount, followed by vanillic acid and nepetin. It was found that the in vitro model was useful for preliminary formulation development, and that the tape-stripping method was robust and effective. Verbascoside, although a poor penetrant, was well released from the formulations in an in vitro release test, suggesting that it might be a potential skin surface-active compound, such as an antimicrobial. Hispidulin, nepetin and vanillic acid, based on their uptake and penetration into the skin, together with their known biological activities, may be considered as feasible candidates for the development of novel and effective antimicrobial, anti-inflammatory, and antioxidant formulations.