Chemical constituents of Breynia glauca leaves

From the leaves of Breynia glauca, eight compounds including friedelin (1), 3-oxo- 4,5-sitosterone (2), friedelan-3β-ol (3), β-sitosterol (4), kaempferol (5), arbutin (6), kaempferol-3-O-rutinoside (7) and quercetion-3-O-glucoside (8) were isolated. The presence of these compounds supports the traditional use of this plant as a detoxifying agent. In addition, all of these chemical constituents were tested for antiviral potential against herpes simplex virus types 1 and 2, but were found to be inactive at 50 μg/ml

Oxyresveratrol from Mulberry as a dihydrate

The title compound {systematic name: 4-[(E)-2-(3,5-dihy­droxy­phen­yl)ethen­yl]benzene-1,3-diol dihydrate}, C14H12O4·2H2O, a derivative of resveratrol, was isolated from mulberry. The linking C=C double bond has a trans conformation and allows the formation of a conjugated system throughout the mol­ecule. The dihedral angle between the benzene rings is 9.39 (9)°. In the crystal, mol­ecules are connected into a three-dimensional architecture through O—H⋯O hydrogen bonds between hy­droxy groups of oxyresveratrol and solvent water mol­ecules

Bergenin from Cissus javana DC. (Vitaceae) root extract enhances glucose uptake by rat L6 myotubes

Purpose: To examine the glucose uptake stimulatory activity of the root extract of Cissus javana DC. (Vitaceae) in Lδ myotubes of rat, and also to identify the extract’s active principles.Methods: The methanol extract was prepared from Cissus javana tuberous roots and evaluated for glucose uptake stimulatory effects on Lδ rat muscle cells and inhibitory activity against α-glucosidase. The chemical components were isolated using several chromatographic techniques, and their structures characterized by spectroscopic methods. Each isolate was then assayed for glucose uptake stimulatory and α-glucosidase inhibitory activities.Results: The extract (100 μg/ml) exhibited glucose uptake stimulatory effect (70.9 % enhancement) and α-glucosidase enzyme inhibitory activity (100 % inhibition). Through chromatographic separation, bergenin, stigmast-4-en-3-one and β-sitosterol were isolated and identified. Bergenin, at 100 μg/ml (0.3046 mM), increased glucose uptake by Lδ myotubes by 50.5 % without toxicity. At the same concentration, bergenin showed no inhibition on α-glucosidase enzyme, while stigmast-4-en-3-one and β-sitosterol exhibited 98.6 and 40.6 %, inhibition, respectively.Conclusion: This study is the first report on the chemical constituents, and the glucose uptake stimulatory and α-glucosidase inhibitory activities of Cissus javana DC. roots. The findings reveal the antidiabetic potential of the plant and the glucose-uptake enhancing activity of bergenin. Keywords: Cissus javana, α-Glucosidase, Antidiabetes, Rat skeletal muscle cells, Bergeni

Effects of oxyresveratrol and its derivatives on cultured P19-derived neurons

Purpose: To modify the structure of oxyresveratrol and evaluate the obtained derivatives for effects on neuronal cells.Methods: Electron-withdrawing groups were selectively introduced to the aromatic ring of the core stilbene structure. Oxyresveratrol and derivatives were then evaluated for their ability to enhance the survival of P19 derived neuronal cells by XTT method, in comparison with the widely known antioxidants, Trolox and ascorbic acid. Phase-contrast microscopic images of the neurons under various conditions were also taken and analyzed.Results: Oxyresveratrol, at a very low concentration (1 ng/mL), enhanced the survival of neurons in both normal and serum-deprivation conditions. Higher activity was observed for the 5-formylated and t 5-carboxylated products. The potencies of these polyoxygenated stilbenes were far greater than those of Trolox and ascorbic acid. These observations were supported by results from the examination of the phase-contrast micrographs of the neuronal cells.Conclusion: Oxyresveratrol and some derivatives prepared in this study demonstrate significant cell protective activity and may be of therapeutic value, but further investigations in animals are required to verify their neuroprotective potentials.Keywords: Oxyresveratrol, Artocarpus lacucha, Artocarpus lakoocha, Polyoxygenated stilbenes, Cell protection, Neuro

Immune modulatory effect of a novel 4,5-dihydroxy-3,3´,4´-trimethoxybibenzyl from Dendrobium lindleyi

Dendrobium bibenzyls and phenanthrenes such as chrysotoxine, cypripedin, gigantol and moscatilin have been reported to show promising inhibitory effects on lung cancer growth and metastasis in ex vivo human cell line models, suggesting their potential for clinical application in patients with lung cancer. However, it remains to be determined whether these therapeutic effects can be also seen in primary human cells and/or in vivo. In this study, we comparatively investigated the immune modulatory effects of bibenzyls and phenanthrenes, including a novel Dendrobium bibenzyl derivative, in primary human monocytes. All compounds were isolated and purified from a Thai orchid Dendrobium lindleyi Steud, a new source of therapeutic compounds with promising potential of tissue culture production. We detected increased frequencies of TNF- and IL-6-expressing monocytes after treatment with gigantol and cypripedin, whereas chrysotoxine and moscatilin did not alter the expression of these cytokines in monocytes. Interestingly, the new 4,5-dihydroxy-3,3′,4′-trimethoxybibenzyl derivative showed dose-dependent immune modulatory effects in lipopolysaccharide (LPS)-treated CD14lo and CD14hi monocytes. Together, our findings show immune modulatory effects of the new bibenzyl derivative from Dendrobium lindleyi on different monocyte sub-populations. However, therapeutic consequences of these different monocyte populations on human diseases including cancer remain to be investigated

Cytotoxic and Antimigratory Activities of Phenolic Compounds from Dendrobium brymerianum

Chromatographic separation of a methanol extract prepared from the whole plant of Dendrobium brymerianum led to the isolation of eight phenolic compounds. Among the isolated compounds (1–8), moscatilin (1), gigantol (3), lusianthridin (4), and dendroflorin (6) showed appreciable cytotoxicity against human lung cancer cell lines with IC50 values of 196.7, 23.4, 65.0, and 125.8 μg/mL, respectively, and exhibited antimigratory property at nontoxic concentrations. This study is the first report on the biological activities of this plant

Analysis of additivity and synergism in the anti-plasmodial effect of purified compounds from plant extracts

In the search for antimalarials from ethnobotanical origin, plant extracts are chemically fractionated and biological tests guide the isolation of pure active compounds. To establish the responsibility of isolated active compound(s) to the whole antiplasmodial activity of a crude extract, the literature in this field was scanned and results were analysed quantitatively to find the contribution of the pure compound to the activity of the whole extract. It was found that, generally, the activity of isolated molecules could not account on their own for the activity of the crude extract. It is suggested that future research should take into account the “drugs beside the drug”, looking for those products (otherwise discarded along the fractionation process) able to boost the activity of isolated active compounds

Induced production of antifungal naphthoquinones in the pitchers of the carnivorous plant Nepenthes khasiana

Nepenthes spp. are carnivorous plants that have developed insect capturing traps, evolved by specific modification of the leaf tips, and are able to utilize insect degradation products as nutritional precursors. A chitin-induced antifungal ability, based on the production and secretion to the trap liquid of droserone and 5-O-methyldroserone, is described here. Such specific secretion uniquely occurred when chitin injection was used as the eliciting agent and probably reflects a certain kind of defence mechanism that has been evolved for protecting the carnivory-based provision of nutritional precursors. The pitcher liquid containing droserone and 5-O-methyldroserone at 3:1 or 4:1 molar ratio, as well as the purified naphthoquinones, exerted an antifungal effect on a wide range of plant and human fungal pathogens. When tested against Candida and Aspergillus spp., the concentrations required for achieving inhibitory and fungicidal effects were significantly lower than those causing cytotoxicity in cells of the human embryonic kidney cell line, 293T. These naturally secreted 1,4-naphthoquinone derivatives, that are assumed to act via semiquinone enhancement of free radical production, may offer a new lead to develop alternative antifungal drugs with reduced selectable pressure for potentially evolved resistance

An Updated Review of Tyrosinase Inhibitors

Tyrosinase is a multifunctional, glycosylated, and copper-containing oxidase, which catalyzes the first two steps in mammalian melanogenesis and is responsible for enzymatic browning reactions in damaged fruits during post-harvest handling and processing. Neither hyperpigmentation in human skin nor enzymatic browning in fruits are desirable. These phenomena have encouraged researchers to seek new potent tyrosinase inhibitors for use in foods and cosmetics. This article surveys tyrosinase inhibitors newly discovered from natural and synthetic sources. The inhibitory strength is compared with that of a standard inhibitor, kojic acid, and their inhibitory mechanisms are discussed