<Emphasis Type="Italic">Morinda citrifolia</Emphasis> Linn. (Rubiaceae) leaf extracts mitigate UVB-induced erythema

Morinda citrifolia Linn. (Rubiaceae) leaves have been used in tropical folk medicine to treat topical inflammation and burns. A carbomer gel base, containing the ethanol extract and juice pressed from the leaves, was evaluated for potential allergenic properties in a repeat-insult patch test in 49 volunteers. To investigate the topical photo-protective properties, the combined ethanol extract and leaf juice were evaluated in a UVB-induced erythema model in 25 volunteers. The crude ethanol extract of M. citrifolia leaves was also evaluated in vitro for potential anti-inflammatory activity in a histamine H-1 receptor antagonism assay. There was no evidence of allergenic potential in the repeat-insult patch test. When the combination of ethanol extract and leaf juice was applied, the UVB dose required to induce erythema was almost 3.5 times greater than with untreated skin (P < 0.001). In the histamine H-1 receptor-binding assay, the crude ethanol extract of M. citrifolia leaves inhibited receptor binding by 57%. These results suggest that M. citrifolia leaves are safe for topical use and may be useful in mitigating UVB-induced injury to the skin.     

Isolation and structural elucidation of chemical constituents from the fruits of<Emphasis Type="Italic">Morinda citrifolia</Emphasis> Linn

The fruits of Morinda citrifolia, Linn. afforded a new constituent, morinaphthalenone (1), and three known constituents, scopoletin (2), 1, 3-dimethoxy-anthraquinone (3) and 1, 2-dihydroxy-anthraquinone (4). The structures of these isolated compounds were determined by spectroscopic methods, including 1D- and 2D-NMR (COSY-45, HMQC, HMBC) techniques, as well as by comparison with published values.     

Inhibitory effects of constituents of <Emphasis Type="Italic">Morinda citrifolia</Emphasis> seeds on elastase and tyrosinase

A 50% ethanolic extract (MCS-ext) from seeds of Morinda citrifolia (“noni” seeds) showed more potent in vitro inhibition of elastase and tyrosinase, and 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity than extracts of M. citrifolia leaves or flesh. Activity-guided fractionation of MCS-ext using in vitro assays led to the isolation of ursolic acid as an active constituent of elastase inhibitory activity. 3,3′-Bisdemethylpinoresinol, americanin A, and quercetin were isolated as active constituents having both tyrosinase inhibitory and radical scavenging activities. Americanin A and quercetin also showed superoxide dismutase (SOD)-like activity. These active compounds were isolated from noni seeds for the first time.     

<Emphasis Type="Italic">Perilla frutescens</Emphasis> var. <Emphasis Type="Italic">frutescens</Emphasis> in northern Laos

Twenty-eight samples of mericarps of Perilla frutescens var. frutescens were collected through fieldwork performed in Phongsali and Xieng Khouang provinces in northern Laos. No perilla samples were collected from Savannakhet province in the south although more than 20 sites were investigated. Perilla plants are mostly grown mixed with dry-paddy rice by slash-and-burn cultivation in Laos. The most popular local name for perilla mericarps in the area was “Ma Nga Chan”. Weight of 1,000 grains and hardness of the mericarps were measured, and all mericarps were found to be large (weight of 1,000 grains around 2 g) and soft (limit load weight under 300 g), which were preferred for culinary use in Laos. The composition of the essential oils obtained from the herbaceous plants raised from the mericarps was divided into five types, perillaketone, elemicine plus myristicine, shisofuran, piperitenon, and myristicine, and GC–MS analysis of these Laotian perilla samples showed that they were similar to those of corresponding types of known Japanese perilla strains. One of the shisofuran-type perilla contained large amounts of putative α-naginatene, which is likely to be an intermediate of the biosynthesis of naginataketone. The farmers' indifference to the oil type of the leaf seems to leave Laotian perilla as a good genetic resource for studies of the biosynthesis of oil compounds.     

Antitubercular triterpenes and phytosterols from <Emphasis Type="Italic">Pandanus tectorius </Emphasis>Soland. var. <Emphasis Type="Italic">laevis</Emphasis>

Bioassay-guided chromatographic purification of the antitubercular chloroform extract of Pandanus tectorius Soland. var. laevis leaves afforded a new tirucallane-type triterpene, 24,24-dimethyl-5β-tirucall-9(11),25-dien-3-one (1), squalene and a mixture of the phytosterols stigmasterol and β-sitosterol. Microplate Alamar Blue Assay (MABA) showed that 1 inhibited the growth of Mycobacterium tuberculosis H₃₇Rv with a MIC of 64 μg/mL, while squalene and the sterol mixture have MICs of 100 and 128 μg/mL, respectively.     

<Emphasis Type="Italic">In Vitro</Emphasis> hepatoprotective compounds from <Emphasis Type="Italic">Suaeda glauca</Emphasis>

Bioassay-guided fractionation of the MeOH extract of Suaeda glauca yielded four phenolic compounds, methyl 3,5-di-O-caffeoyl quinate (1) and 3,5-di-O-caffeoyl quinic acid (2), isorhamnetin 3-O-beta-D-galactoside (3), and quercetin 3-O-beta-D-galactoside (4). Compounds 1 and 2 were hepatoprotective against tacrine-induced cytotoxicity in human liver-derived Hep G2 cells with the EC(50) values of 72.7+/-6.2 and 117.2+/-10.5 microM, respectively. Silybin as a positive control showed an EC(50) value of 82.4+/-4.1 microM.     

A new <Emphasis Type="Italic">Erythrina</Emphasis> alkaloid from <Emphasis Type="Italic">Erythrina herbacea</Emphasis>

A new Erythrina alkaloid, 10-hydroxy-11-oxoerysotrine (1), has been isolated from the flowers of Erythrina herbacea together with five known compounds: erytharbine (2), 10,11-dioxoerysotrine (3), erythrartine (4), erysotramidine (5) and erysotrine-N-oxide (6). The structure of the new compound was elucidated on the basis of its spectral data, including 2-D NMR and mass (MS) spectra. The new compound is a rare C-10 oxygenated Erythrina alkaloid. The antioxidant activities of the isolated compounds 1–6 were evaluated by scavenging with peroxynitrite.     

<Emphasis Type="Italic">In Vitro</Emphasis> antioxidant and anti-inflammatory activities of Jaceosidin from <Emphasis Type="Italic">Artemisia princeps</Emphasis> Pampanini <Emphasis Type="Italic">cv.</Emphasis> Sajabal

Oxidized low-density lipoprotein (oxLDL) plays a key role in the inflammatory processes of atherosclerosis. Jaceosidin isolated from the methanolic extracts of the aerial parts of Artemisia princeps Pampanini cv. Sajabal was tested for antioxidant and anti-inflammatory activities. Jaceosidin inhibited the Cu²⁺-mediated LDL oxidation with IC₅₀ values of 10.2 μM in the thiobarbituric acid-reactive substances (TBARS) assay as well as the macrophage-mediated LDL oxidation. The antioxidant activities of jaceosidin were exhibited in the conjugated diene production, relative electrophoretic mobility, and apoB-100 fragmentation on copper-mediated LDL oxidation. Jaceosidin also inhibited the generation of reactive oxygen species (ROS) concerning in regulation of NF-κB signaling. And jaceosidin inhibited nuclear factor-kappa B (NF-κB) activity, nitric oxide (NO) production, and suppressed expression of inducible nitric oxide synthase (iNOS) in lipopolysaccharide (LPS)-induced RAW264.7 macrophages.     

Identification of <Emphasis Type="Italic">Curcuma</Emphasis> plants and curcumin content level by DNA polymorphisms in the <Emphasis Type="Italic">trn</Emphasis>S-<Emphasis Type="Italic">trn</Emphasis>fM intergenic spacer in chloroplast DNA

With the goal of developing an accurate plant identification method, molecular analysis based on polymorphisms of the nucleotide sequence of chloroplast DNA (cpDNA) was performed in order to distinguish four Curcuma species: C. longa, C. aromatica, C. zedoaria, and C. xanthorrhiza. Nineteen regions of cpDNA were amplified successfully via polymerase chain reaction (PCR) using total DNA of all Curcuma plants. Using the intergenic spacer between trnS and trnfM (trnSfM), all four Curcuma plant species were correctly identified. In addition, the number of AT repeats in the trnSfM region was predictive of the curcumin content in the rhizome of C. longa.     

Main phenolic compounds from the flower of <Emphasis Type="Italic">Trachelospermum asiaticum</Emphasis> var. <Emphasis Type="Italic">intermedium</Emphasis> (Apocynaceae)

Six phenolic compounds were isolated from the flowers of Trachelospermum asiaticum var. intermedium (Apocynaceae). These structures were determined on the basis of spectral data.     

Diacylglycerol acyltransferase-inhibitory compounds from <Emphasis Type="Italic">Erythrina senegalensis</Emphasis>

Inhibition of acyl CoA:diacylglycerol acyltransferase (DGAT) is proposed to be a drug target for the treatment of obesity and type 2 diabetes. Bioassay-guided fractionation of the CH₂Cl₂-soluble extract of the stem bark of Erythrina senegalensis, using an in vitro DGAT enzyme assay, resulted in the isolation of eight known prenylflavonoids, 8-prenylleutone (1), auriculatin (2), erysenegalensein O (3), erysenegalensein D (4), erysenegalensein N (5), derrone (6), alpinumisoflavone (7), and 6,8-diprenylgenistein (8). Compounds 1, 2–4, 6, and 8 inhibited DGAT activity, with IC₅₀ values ranging from 1.1 ± 0.3 to 15.1 ± 1.1 μg/mL. On the basis of the data obtained, we propose isoflavonoids with isoprenyl groups as a novel class of DGAT inhibitors.     

Two new antibacterial norabietane diterpenoids from cyanobacteria, <Emphasis Type="Italic">Microcoleous </Emphasis><Emphasis Type="Italic">lacustris</Emphasis>

Two abietane diterpenes were isolated from cyanobacteria Microcoleous lacustris, 20-nor-3α-acetoxyabieta-5,7,9,11,13-pentaene and 20-nor-3α-acetoxy-12-hydroxy-abieta-5,7,9,11,13-pentaene. These compounds were assayed against Staphylococcus aureus, Staphylococcus epidermidis, Salmonella typhi, Vibrio cholerae, Bacillus subtilis, Bacillus cereus, Escherichia coli, and Klebsiella pneumoniae. Both compounds showed activity against S. aureus, S. epidermidis, S. typhi, and V. cholerae, but not against the other bacteria.     

Chemical constituents of <Emphasis Type="Italic">Hypericum erectum</Emphasis> Thunb.

Twenty-two known constituents, including four xanthones, nine flavonoids and nine phenolic glycosides, were isolated from Hypericum erectum Thunb. Their structures were elucidated on the basis of spectral evidence.     

Molecular analysis of constitutive mutations in <Emphasis Type="Italic">ermB</Emphasis> and <Emphasis Type="Italic">ermA</Emphasis> selected <Emphasis Type="Italic">In Vitro</Emphasis> from inducibly MLS<Subscript>B</Subscript>-resistant enterococci

Frequencies of spontaneous mutation from inducible resistance to constitutive resistance were determined for the four clinical isolates of erythromycin-resistant enterococci, including one isolate with ermB gene and three clinical isolates with ermA gene. The rate of ermB mutation was higher than that of ermA mutation by more than 10 fold. Sequence analysis of the regulatory regions of erm genes revealed that mutation type of ermB was just point mutation, by contraries the mutation type of ermA was either deletion or tandem duplication. These results showed distinct characteristics in mutation patterns of ermB and ermA.     

Essential oil compounds from<Emphasis Type="Italic">Agastache rugosa</Emphasis> as antifungal agents against<Emphasis Type="Italic">Trichophyton</Emphasis> species

The antifungal activities of the essential oil from Agastache rugosa and its main component, estragole, combined with ketoconazole, one of the azole antibiotics commonly used to treat infections caused by Trichophyton species, were evaluated in this study. The combined effects were measured by the checkerboard microtiter and the disk diffusion tests, against T. erinacei, T. mentagrophytes, T. rubrum, T. schoenleinii and T. soudanense. Susceptibility of the five Trichophyton species to the oil alone, or ketoconazole alone, differed distinctly. The fractional inhibitory concentration indices (FICI) of ketoconazole combined with estragole or A. rugosa essential oil, against the tested Trichophyton species, were between 0.05 and 0.27, indicating synergistic effects. These drug combinations exhibited the most significant synergism against T. mentagrophytes, with FICIs of 0.05 and 0.09 for estragole and the essential oil fraction from A. rugosa, respectively. Isobolograms based on the data from checkerboard titer tests also indicated significant synergism between ketoconazole and the Agastache oil fraction or estragole, against the Trichophyton species evaluated. Trichophyton susceptibility to ketoconazole was significantly improved by combination with the Agastache rugosa oil fraction or its main component, estragole.     

A new lignan glucoside from the stems of <Emphasis Type="Italic">Callicarpa japonica</Emphasis> Thunb. var. <Emphasis Type="Italic">luxurians</Emphasis> Rehd.

A new lignan glucoside (1) was isolated from the stems of Callicarpa japonica Thunb. var. luxurians Rehd. (Verbenaceae), along with six known lignan glucosides and three known triterpenoids. The chemical structure of 1 was characterized as (+)-lyoniresinol 3α-O-(6″-3,5-dimethoxy-4-hydroxybenzoyl)-β-d-glucopyranoside on the basis of spectroscopic data. In addition, the radical-scavenging effect of four lignans on the stable free radical 1,1-diphenyl-2-picrylhydrazyl was examined. Among the tested compounds, three compounds, including 1, showed almost the same scavenging activity as that of α-tocopherol.     

A rapid method for isolation of piperine from the fruits of <Emphasis Type="Italic">Piper nigrum</Emphasis> Linn.

A simple, rapid and efficient method has been developed for the isolation of piperine from the fruits of Piper nigrum. The method involves extraction of the fruit powder with glacial acetic acid, from which piperine is partitioned into chloroform and subsequently crystallized. The identity of the compound was confirmed by its melting point, comparison of UV, IR, and mass spectral data with those from a reference standard, and co-chromatography with the reference standard using thin-layer chromatography (TLC). The purity of the compound was ascertained by TLC, by recording UV absorption spectra at the start, middle, and end positions of the spot on the plate, and by differential scanning calorimetry (DSC).     

Intermedins A and B; New metabolites from <Emphasis Type="Italic">Schisandra propinqua</Emphasis> var. <Emphasis Type="Italic">intermedia</Emphasis>

A new dibenzocyclooctadiene lignan, intermedin A (1), and a new natural bisabolane sesquiterpenoid, intermedin B (2), were isolated from the aerial parts of Schisandra propinqua var. intermedia. Their structures were elucidated on the basis of extensive spectroscopical analysis.