Resveratrol is a naturally occurring stilbene, a kind of polyphenolic compounds, found in a limited number of plant species such as grape, peanut, and pine. It has been considered as a phytoalexin in plants, and many studies have also shown its health benefits such as antioxidant activities, cancer prevention, blood thinning, and life span extension. This paper reviews the characteristics of resveratrol in aspects of synthesis, extraction, purification, and determination. In particular, the new outcomes of physiology function and the transgenic approaches have been presented. The challenges and chances for genetic engineering and health-related industries were also discussed.
Genetic Engineering ; Plants ; chemistry ; Stilbenes ; chemical synthesis ; metabolism ; pharmacology

Pterostilbene (3,5-dimethoxy-4'-hydroxystilbene) is a polyphenolic compound primarily found in blueberries, grapes, and a tree wood, pterocarpus marsupium. Studies demonstrate that pterostilbene inhibits a variety of cancers, such as lung, breast, stomach, colon, etc. The anti-cancer activities are related to the regulation of several hallmarks of cancer. Moreover, pterostilbene exhibits much greater bioavailability and bioactivity than resveratrol which warrants further investigation in the anti-cancer functions and mechanisms.
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Animals ; Antineoplastic Agents, Phytogenic ; chemistry ; pharmacology ; Humans ; Neoplasms ; drug therapy ; Plant Extracts ; chemistry ; pharmacology ; Stilbenes ; chemistry ; pharmacology

The investigation on the stem bark of Morus wittiorum was carried out to find its chemical constituents possessing anti-oxidative activity. The isolation and purification were performed by various chromatographies such as silica gel, Sephadex LH-20, RP-C18 column chromatography and so on. Based on the spectral analysis such as NMR, MS, etc., seven 2-arylbenzofuran derivatives were identified as wittifuran D (1), wittifuran E (2), moracin C (3), moracin M (4), moracin P (5), 2-(3,5-dihydroxyphenyl)-5,6-dihydroxybenzofuran (6) and mulberroside C (7). Compounds 1-7 were isolated from this plant for the first time. Among them, 1 and 2 were new compounds. Compounds 3-7 were used to assay antioxidant activity, the inhibitory ratios of compounds 3, 4, 6, at a concentration of 1 x 10(-5) mol x L(-1), to malondialdehyde (MDA) produced during microsomal lipid peroxidation induced by ferrous-cysteine were 73%, 69% and 89% respectively.
Antioxidants ; isolation & purification ; pharmacology ; Benzofurans ; chemistry ; isolation & purification ; pharmacology ; Lipid Peroxidation ; Malondialdehyde ; chemistry ; Molecular Structure ; Morus ; chemistry ; Plant Bark ; chemistry ; Plants, Medicinal ; chemistry ; Stilbenes ; chemistry ; isolation & purification ; pharmacology

OBJECTIVETo isolate and identify the Diels-Alder type adducts from stem barks of Morus yunanensis.

METHODThe compounds were isolated and purified by silicagel, Sephadex LH-20 and RP-18 colum chromatography. Their chemical structures were elucidated on the basis ofphysicochemical properties and spectral data.

RESULTNine compounds were isolated and identified as: kuwanon G (1), sanggenol M (2), mulberrofuran J (3), guangsangon B (4), resveratrol (5), kuwanon X (6), kuwanon P (7), mulberrofuran O (8), mulberrofuran Q (9).

CONCLUSIONAll the compounds are isolated from the plant for the first time, and compounds 4, 5 have anti-inflammation activities with inhibitory ratios of 57.3%, 50.5% respectively at a concentration of 10 microg mL(-1).

Anti-Inflammatory Agents ; pharmacology ; Antioxidants ; pharmacology ; Drugs, Chinese Herbal ; Flavonoids ; analysis ; Morus ; chemistry ; Plant Bark ; chemistry ; Plant Extracts ; pharmacology ; Plant Stems ; chemistry ; Stilbenes ; analysis

Animals ; Anti-Inflammatory Agents, Non-Steroidal ; chemistry ; pharmacology ; Antineoplastic Agents, Phytogenic ; chemistry ; pharmacology ; Antiviral Agents ; chemistry ; pharmacology ; Humans ; Magnetic Resonance Spectroscopy ; Molecular Conformation ; Molecular Structure ; Plants, Medicinal ; chemistry ; Stilbenes ; chemistry ; isolation & purification ; pharmacology

Microtubule is one of the key components of the cytoskeleton and plays an important role in the maintenance of cell shape and the process of signal transduction and mitosis. Due to the extreme importance of microtubule in the process of mitosis, tubulin becomes one of the most important targets for development of new anticancer drugs and tubulin inhibitors are used for the treatment of cancer nowadays. These inhibitors have antitumor activity by inhibiting or promoting the assembly of tubulin to microtubules and interfering the process of cell mitosis. This review summarized the research progress of the tubulin inhibitors, especially the introduction of the tubulin inhibitors of pharmacological activities and the progress of clinical research. Also, the development trend of these inhibitors is discussed.
Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; Humans ; Microtubules ; drug effects ; metabolism ; Mitosis ; drug effects ; Molecular Structure ; Neoplasms ; drug therapy ; Stilbenes ; chemical synthesis ; chemistry ; pharmacology ; Structure-Activity Relationship ; Tubulin ; metabolism ; Tubulin Modulators ; chemical synthesis ; chemistry ; pharmacology

Vascular disrupting agents (VDAs) have presented a new kind of anti-cancer drug in recent years. VDAs take advantage of the weakness of established tumor endothelial cells and their supporting structures. In contrast to anti-angiogenic therapy, which inhibits the outgrowth of new blood vessels, vascular targeting treatments selectively attack the existing tumor vasculature. Here we summarized the anti-tumor activities, mechanisms and clinical applications of small molecule VDAs.
Angiogenesis Inhibitors ; chemistry ; pharmacology ; therapeutic use ; Animals ; Antineoplastic Agents ; chemistry ; pharmacology ; therapeutic use ; Bibenzyls ; chemistry ; pharmacology ; therapeutic use ; Diphosphates ; chemistry ; pharmacology ; therapeutic use ; Endothelial Cells ; drug effects ; Humans ; Molecular Structure ; Neoplasms ; drug therapy ; pathology ; Neovascularization, Pathologic ; Oligopeptides ; chemistry ; pharmacology ; therapeutic use ; Organophosphorus Compounds ; chemistry ; pharmacology ; therapeutic use ; Serine ; analogs & derivatives ; chemistry ; pharmacology ; therapeutic use ; Stilbenes ; chemistry ; pharmacology ; therapeutic use ; Tubulin Modulators ; chemistry ; pharmacology ; therapeutic use ; Xanthones ; chemistry ; pharmacology ; therapeutic use

This study was intended to look for anti-HIV chemical constituents of aerial parts of Caragana rosea Turcz. Column chromatographic technique was used for the isolation and purification of constituents of Caragana rosea under the guide of anti-HIV assay. The structures were established on the basis of physical and chemical properties and spectroscopic data. Five compounds were obtained from the EtOAc fraction of aerial parts of Caragana rosea and identified as myricetin (1), mearnsetin (2), p-hydroxy cinnamic acid (3), cararosinol A (4) and cararosinol B (5). At the same time, one possible transformation route between cararosinol B and kobophenol A, another resveratrol tetramer isolated from this plant previously, was proposed. Compounds 4, 5 are new resveratrol tetramers, compounds 1 -3 were isolated from this plant for the first time. All compounds showed no activities in an in vitro assay against HIV-1.
Anti-HIV Agents ; chemistry ; isolation & purification ; pharmacology ; Benzofurans ; chemistry ; isolation & purification ; pharmacology ; Caragana ; chemistry ; Coumaric Acids ; chemistry ; isolation & purification ; pharmacology ; Flavonoids ; chemistry ; isolation & purification ; pharmacology ; HIV-1 ; drug effects ; Molecular Structure ; Plant Components, Aerial ; chemistry ; Plants, Medicinal ; chemistry ; Propionates ; Stilbenes ; chemistry ; isolation & purification ; pharmacology

Antifungal drug resistance is a significant clinical problem, and antifungal agents that can evade resistance are urgently needed. In infective niches, resistant organisms often co-existed with sensitive ones, or a subpopulation of antibiotic-susceptible organisms may evolve into resistant ones during antibiotic treatment and eventually dominate the whole population. In this study, we established a co-culture assay in which an azole-resistant Candida albicans strain was mixed with a susceptible strain labeled with green fluorescent protein to mimic in vivo conditions and screen for antifungal drugs. Fluconazole was used as a positive control to verify the validity of this co-culture assay. Five natural molecules exhibited antifungal activity against both susceptible and resistant C. albicans. Two of these compounds, retigeric acid B (RAB) and riccardin D (RD), preferentially inhibited C. albicans strains in which the efflux pump MDR1 was activated. This selectivity was attributed to greater intracellular accumulation of the drugs in the resistant strains. Changes in sterol and lipid compositions were observed in the resistant strains compared to the susceptible strain, and might increase cell permeability to RAB and RD. In addition, RAB and RD interfered with the sterol pathway, further aggregating the decrease in ergosterol in the sterol synthesis pathway in the MDR1-activated strains. Our findings here provide an alternative for combating resistant pathogenic fungi.
ATP-Binding Cassette Transporters ; genetics ; metabolism ; Antifungal Agents ; chemistry ; metabolism ; pharmacology ; Azoles ; pharmacology ; Biosynthetic Pathways ; drug effects ; genetics ; Candida albicans ; chemistry ; drug effects ; metabolism ; Cell Membrane ; chemistry ; metabolism ; Coculture Techniques ; Drug Resistance, Fungal ; drug effects ; Ergosterol ; metabolism ; Fungal Proteins ; genetics ; metabolism ; Lipids ; chemistry ; Molecular Structure ; Permeability ; Phenyl Ethers ; chemistry ; metabolism ; pharmacology ; Sterols ; chemistry ; metabolism ; Stilbenes ; chemistry ; metabolism ; pharmacology ; Triterpenes ; chemistry ; metabolism ; pharmacology

OBJECTIVETo optimize the extraction process of root of Polygoni multflori and validate the interrelation between antioxdative capacity and the content of 2,3,4,5-tetrahydroxystilbene-2-O-beta-D-glucoside in root of P. multiflori.

METHODThe optimum extraction was abserved with the orthogonal design; 2,3,4,5-tetrahydroxystilbene-2-O-beta-D-glucoside was determined by HPLC and the antioxidative capacity by using photochemiluminescence detection method with the Photochem supplied by Analytik Jena AG; the concentration of ethanol, amount of ethanol, extraction time and extraction times were the four factors in the extraction.

RESULTThe concentration of ethanol and extraction times had significant effect on the content of 2,3,4,5-tetrahydroxystilbene-2-O-beta-D-glucoside and the antioxidative capacity of the crude extract.

CONCLUSIONThe best extraction process is to extract three times by using 10 fold EtOH(60%), refluxing at 85 degrees C and to extract one and half hours each time.

Antioxidants ; isolation & purification ; pharmacology ; Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal ; isolation & purification ; pharmacology ; Ethanol ; Glucosides ; analysis ; isolation & purification ; Plant Roots ; chemistry ; Plants, Medicinal ; chemistry ; Polygonum ; chemistry ; Stilbenes ; analysis ; isolation & purification ; Technology, Pharmaceutical ; methods ; Time Factors