Two new limonoids, 12-ethoxynimbolinins G and H (compounds 1 and 2), and one known compound, toosendanin (Chuanliansu) (compound 3), were isolated from the bark of Melia toosendan. Their structures were elucidated by spectroscopic analysis and X-ray techniques. The absolute configuration of toosendanin (3) was established by single-crystal X-ray diffraction. Compounds 1-3 were evaluated for their cytotoxicity against five tumor cell lines.
Cell Line, Tumor ; Cell Proliferation ; drug effects ; Humans ; Limonins ; isolation & purification ; Melia ; chemistry ; Molecular Structure ; Plant Bark ; chemistry ; Plant Extracts ; chemistry ; isolation & purification ; pharmacology ; X-Ray Diffraction

OBJECTIVEMyanmar has a long history of using medicinal plants for treatment of various diseases. To the best of our knowledge there are no previous reports on antiglycation activities of medicinal plants from Myanmar. Therefore, this study was aimed to evaluate the antioxidant, antiglycation and antimicrobial properties of 20 ethanolic extracts from 17 medicinal plants indigenous to Myanmar.

METHODSIn vitro scavenging assays of 2,2-diphenyl-1-picrylhydrazyl (DPPH), nitric oxide (NO), superoxide (SO) radicals were used to determine the antioxidant activities. Folin-Ciocalteu's method was performed to determine the total phenolic content. Antiglycation and antimicrobial activities were detected by bovine serum albumin-fluorescent assay and agar well diffusion method.

RESULTSTerminalia chebula Retz. (Fruit), containing the highest total phenolic content, showed high antioxidant activities with inhibition of 77.98% ± 0.92%, 88.95% ± 2.42%, 88.56% ± 1.87% and 70.74%± 2.57% for DPPH, NO, SO assays and antiglycation activity respectively. It also showed the antimicrobial activities against Staphylococcus aureus, Bacillus cereus, Escherichia coli, Pseudomonas aeruginosa and Candida albicans with inhibition zone of 19, 18, 17, 25 and 15 mm, respectively. Garcinia mangostana Linn. showed the strongest activities for SO and antiglycation assays with inhibition of 93.68% ± 2.63% and 82.37% ± 1.78%. Bark of Melia sp. was the best NO radical scavenger with inhibition rate of 89.39%± 0.60%.

CONCLUSIONThe results suggest that these plants are potential sources of antioxidants with free radical-scavenging and antiglycation activities and could be useful for decreasing the oxidative stress and glycation end-product formation in glycation-related diseases.

Anti-Bacterial Agents ; analysis ; pharmacology ; Anti-Infective Agents ; analysis ; pharmacology ; Antioxidants ; analysis ; pharmacology ; Bacteria ; drug effects ; growth & development ; Biphenyl Compounds ; metabolism ; Candida albicans ; drug effects ; growth & development ; Fruit ; Garcinia ; chemistry ; Glycation End Products, Advanced ; metabolism ; Humans ; Magnoliopsida ; chemistry ; Medicine, Traditional ; Melia ; chemistry ; Myanmar ; Nitric Oxide ; metabolism ; Oxidative Stress ; drug effects ; Phenols ; analysis ; pharmacology ; Phytotherapy ; Picrates ; metabolism ; Plant Bark ; Plant Extracts ; chemistry ; pharmacology ; Plants, Medicinal ; Superoxides ; Terminalia ; chemistry

The present study was designed to characterize the polyphenols isolated from Acacia mearnsii bark crude extract (B) and fractions (B1-B7) obtained by high-speed counter-current chromatography (HSCCC) and evaluate their anti-inflammatory and carbolytic enzymes (α-glucosidase and α-amylase) inhibitory activities. Fractions B4, B5, B6, B7 (total phenolics 850.3, 983.0, 843.9, and 572.5 mg·g, respectively; proanthocyanidins 75.7, 90.5, 95.0, and 44.8 mg·g, respectively) showed significant activities against reactive oxygen species (ROS), nitric oxide (NO) production, and expression of pro-inflammatory genes interleukin-1β (IL-1β) and inducible nitric oxide synthase (iNOS) in a lipopolysaccharide (LPS)-stimulated mouse macrophage cell line RAW 264.7. All the extracts suppressed α-glucosidase and α-amylase activities, two primary enzymes responsible for carbohydrate digestion. A. mearnsii bark samples possessed significantly stronger inhibitory effects against α-glucosidase enzyme (IC of 0.4-1.4 μg·mL) than the pharmaceutical acarbose (IC 141.8 μg·mL). B6 and B7 (IC 17.6 and 11.7 μg·mL, respectively) exhibited α-amylase inhibitory activity as efficacious as acarbose (IC 15.4 μg·mL). Moreover, B extract, at 25 µg·mL, significantly decreased the non-mitochondrial oxidative burst that is often associated with inflammatory response in human monocytic macrophages.
Acacia ; chemistry ; Animals ; Anti-Inflammatory Agents ; isolation & purification ; pharmacology ; Carbohydrate Metabolism ; drug effects ; Glycoside Hydrolase Inhibitors ; pharmacology ; Inflammation ; metabolism ; Interleukin-1beta ; metabolism ; Lipopolysaccharides ; Macrophages ; drug effects ; Mice ; Nitric Oxide ; metabolism ; Nitric Oxide Synthase Type II ; metabolism ; Plant Bark ; chemistry ; Plant Extracts ; chemistry ; pharmacology ; Polyphenols ; isolation & purification ; pharmacology ; Proanthocyanidins ; pharmacology ; RAW 264.7 Cells ; alpha-Amylases ; antagonists & inhibitors ; alpha-Glucosidases ; metabolism

Two new phragmalin-type limonoids orthoesters, encandollens A and B (1 and 2), were isolated from the stem barks of Entandrophragma candollei collected in Ghana. The structures of these compounds were elucidated on the basis of HR-ESI-MS, H and C NMR, HSQC, HMBC, and ROESY data. Compound 1 was a rare C-15 enolic acyl phragmalin-type limonoid orthoester. Compounds 1 and 2 exhibited weak inhibitory effects on NO production in lipopolysaccharide (LPS)-induced RAW 264.7 cells.
Animals ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; pharmacology ; Limonins ; chemistry ; isolation & purification ; pharmacology ; Macrophages ; drug effects ; metabolism ; Meliaceae ; chemistry ; Mice ; Molecular Structure ; Nitric Oxide ; metabolism ; Plant Bark ; chemistry ; RAW 264.7 Cells

Stress and emotion are associated with several illnesses from headaches to heart diseases and immune deficiencies to central nervous system. Terminalia arjuna has been referred as traditional Indian medicine for several ailments. The present study aimed to elucidate the effect of T. arjuna bark extract (TA) against picrotoxin-induced anxiety. Forty two male Balb/c mice were randomly divided into six experimental groups (n = 7): control, diazepam (1.5 mg·kg), picrotoxin (1 mg·kg) and three TA treatemt groups (25, 50, and 100 mg/kg). Behavioral paradigms and PCR studies were performed to determine the effect of TA against picrotoxin-induced anxiety. The results showed that TA supplementation increased locomotion towards open arm (EPM) and illuminated area (light-dark box test), and increased rearing frequency (open field test) in a dose dependent manner, compared to picrotoxin (P < 0.05). Furthermore, TA increased number of licks and shocks in Vogel's conflict. PCR studies showed an up-regulation of several genes, such as BDNF, IP, DL, CREB, GABA, SOD, GPx, and GR in TA administered groups. In conclusion, alcoholic extract of TA bark showed protective activity against picrotoxin in mice by modulation of genes related to synaptic plasticity, neurotransmitters, and antioxidant enzymes.
Animals ; Antioxidants ; metabolism ; Anxiety Disorders ; drug therapy ; genetics ; metabolism ; psychology ; Brain-Derived Neurotrophic Factor ; genetics ; metabolism ; Dopamine Agents ; administration & dosage ; GABA Agents ; administration & dosage ; Glutathione Peroxidase ; genetics ; metabolism ; Humans ; Male ; Mice ; Mice, Inbred BALB C ; Neuronal Plasticity ; drug effects ; Neurotransmitter Agents ; metabolism ; Phytotherapy ; Picrotoxin ; adverse effects ; Plant Bark ; chemistry ; Plant Extracts ; administration & dosage ; Serotonin Agents ; administration & dosage ; Superoxide Dismutase-1 ; genetics ; metabolism ; Terminalia ; chemistry

Considering the great potential of natural products as anticancer agents, the present study was designed to explore the molecular mechanisms responsible for anticancer activities of Mesua ferrea stem bark extract against human colorectal carcinoma. Based on MTT assay results, bioactive sub-fraction (SF-3) was selected for further studies using HCT 116 cells. Repeated column chromatography resulted in isolation of less active α-amyrin from SF-3, which was identified and characterized by GC-MS and HPLC methods. α-amyrin and betulinic acid contents of SF-3 were measured by HPLC methods. Fluorescent assays revealed characteristic apoptotic features, including cell shrinkage, nuclear condensation, and marked decrease in mitochondrial membrane potential in SF-3 treated cells. In addition, increased levels of caspases-9 and -3/7 levels were also observed in SF-3 treated cells. SF-3 showed promising antimetastatic properties in multiple in vitro assays. Multi-pathway analysis revealed significant down-regulation of WNT, HIF-1α, and EGFR with simultaneous up-regulation of p53, Myc/Max, and TGF-β signalling pathways in SF-3 treated cells. In addition, promising growth inhibitory effects were observed in SF-3 treated HCT 116 tumour spheroids, which give a hint about in vivo antitumor efficacy of SF-3 phytoconstituents. In conclusion, these results demonstrated that anticancer effects of SF-3 towards colon cancer are through modulation of multiple molecular pathways.
Antineoplastic Agents ; pharmacology ; Apoptosis ; drug effects ; Cell Line, Tumor ; Colorectal Neoplasms ; drug therapy ; metabolism ; pathology ; physiopathology ; ErbB Receptors ; genetics ; metabolism ; HCT116 Cells ; Humans ; Hypoxia-Inducible Factor 1, alpha Subunit ; genetics ; metabolism ; Magnoliopsida ; chemistry ; Neoplasm Metastasis ; prevention & control ; Plant Bark ; chemistry ; Plant Extracts ; pharmacology ; Signal Transduction ; drug effects ; Wnt Proteins ; genetics ; metabolism

The present study carried out a phytochemical investigation on the root barks of Dictamnus dasycarpus Turcz, leading to the isolation and characterization of two new aromatic ring butyrolactone derivatives, dasycarpusphenol acid A (1) and dasycarpusphenol acid B (2). Their structures were elucidated by using spectroscopic techniques and HR-FAB-MS. Compounds 1 and 2 exhibited antioxidant activity, with their IC values being 28.95 and 41.76 mg·mL, respectively.
4-Butyrolactone ; chemistry ; isolation & purification ; Antioxidants ; chemistry ; isolation & purification ; Dictamnus ; chemistry ; Molecular Structure ; Plant Bark ; chemistry ; Plant Extracts ; chemistry ; isolation & purification

OBJECTIVETo test the antioxidant, antidiabetic, anticancer and antibacterial activities along with phytochemicals of Sonneratia apetala Buch.-Ham.

METHODSThe antibacterial activity was determined by agar well diffusion method. The antioxidant activity was determined by standard assay. The antidiabetic activity was evaluated by α-glucosidase inhibition assay and in vivo anticancer property was determined against Ehrlich ascites carcinoma (EAC) cells in Swiss Albino mice. Further partial characterization of the methanol extracts was carried out by thin layer chromatography, high performance liquid chromatography, (1)H nuclear magnetic resonance spectroscopy and Fourier transform-infra red spectrum spectral analysis.

RESULTSFour solvent extracts (acetone, ethanol, methanol and aqueous) of leaf and bark possess strong antioxidant properties. In vivo anticancer activity of methanol extract leaf indicated positive activity showing 34% inhibition against EAC cells in Swiss Albino mice. All extracts exhibited α-glucosidase inhibitory activity in a dose-dependent manner indicating presence of promising antidiabetic properties. The extracts possess strong antibacterial activity against the selected pathogenic bacteria (minimal inhibitory concentration ranging from 1.25-5.00 mg/mL). The partial characterization of the methanol extracts of leaf and bark revealed the presence of phenolics as the lead compound responsible for studied bioactivities of the plant extracts.

CONCLUSIONSonneratia apetala extracts have potent antibacterial, antioxidant, antidiabetic and anticancer properties which can be further exploited for its pharmaceutical applications.

Animals ; Anti-Bacterial Agents ; chemistry ; pharmacology ; Antineoplastic Agents, Phytogenic ; chemistry ; pharmacology ; Antioxidants ; chemistry ; pharmacology ; Drug Evaluation, Preclinical ; India ; Lythraceae ; chemistry ; Mice ; Microbial Sensitivity Tests ; Phytotherapy ; Plant Bark ; chemistry ; Plant Extracts ; chemistry ; pharmacology ; Plant Leaves ; chemistry ; Tumor Cells, Cultured

OBJECTIVETo isolate antifungal compound from Paeonia suffruticosa, and to find the antifungal mechanisms by observing the ultrastructural modifications of yeasts in growth phase produced by 1,2,3,4,6-penta-O-galloyl-beta-D-glucose (PGG).

METHODSPeony (Paeonia suffruticosa) root bark (PRB) was separated by solvent extraction and purified by high performance liquid chromatography (HPLC) method using analytical and preparative reversed phase C18 column on the basis of bio-assay method. In order to investigate the antifungal mechanism of PGG, Yeasts were submitted to different concentrations [3 × minimum inhibition concentration (MIC), 0.3 × MIC] for 1 h under constant stirring at 30 °C, and transmission electron microscopy was performed.

RESULTSBased on the antifungal activity of PRB on Candida glabrata CBS138, the antifungal compound were isolated in ethyl acetate layer of PRB and identified as PGG by mass spectrometry, 1H nuclear magnetic resonance (NMR) analyses, with molecular weight of 940 and molecular formular as C41H32O26. Transmission electron microscopy showed that PGG degraded the cell wall envelope.

CONCLUSIONThe results suggest that PGG may be responsible for the antifungal activity of PRB by disrupting the structure of cell wall directly.

Antifungal Agents ; chemistry ; isolation & purification ; pharmacology ; Candida ; drug effects ; ultrastructure ; Chromatography, High Pressure Liquid ; Hydrolyzable Tannins ; chemistry ; isolation & purification ; pharmacology ; Mass Spectrometry ; Microbial Sensitivity Tests ; Paeonia ; chemistry ; Plant Bark ; chemistry ; Plant Extracts ; isolation & purification ; pharmacology ; Plant Roots ; chemistry ; Proton Magnetic Resonance Spectroscopy

OBJECTIVEZanthoxylum heitzii is a medicinal plant widely used in central Africa for the treatment of many diseases, especially cardiovascular diseases and hypertension. The diuretic effects of crude stem bark extraction were determined and its safety in rats was evaluated.

METHODSThe diuretic effects of crude stem bark extraction of Z. heitzii 250 g ± 10 g) of both sexes. The crude stem bark extraction of Z. heitzii at the doses of 225, 300 and 375 mg/kg was administered to rats at 5 mL/kg body weight. Urine volume was determined 1, 2, 3, 4, 5, 6 and 24 h after administration of the extract. Kinetics of electrolyte elimination in response to a single oral administration dose of acute treatment was measured. The experiments were performed under the same conditions with two synthetic pharmacological diuretics considered as reference (furosemide and hydrochlorothiazide). Urinary and plasma concentrations of sodium and potassium ions were determined using flame photometry. Concentrations of creatinine, urea, glucose, albumin and electrolytes in the plasma and urine samples were evaluated using a two-way digital bidirectional spectrophotometer. The osmolarity of plasma and urine samples was measured by cytometry using an osmometer. Aldosterone was measured by radioimmunoassay.

RESULTSThe plant extract accelerated the elimination of overloaded fluid and increased urine volume and the excretion of Na+, K+ and Cl- 24 h after administration (P<0.05). The increase in elimination of Na+, K+, and Cl- induced by caused alkalinization of the urine, and showed a strong inhibitory effect on carbonic anhydrase and saluretic. These effects were mainly observed at the dose of 375 mg/kg. At the maximum diuretic response, urinary osmolarity decreased significantly (P<0.05) when compared to controls. The stability of aldosterone level, the absence of correlation with the plasma levels of Na+, and increased clearance of free water in the animals treated with indicated that increased diuresis and natriuresis were tubular in origin. No significant (P>0.05) changes were observed in the body temperature of the animals.

CONCLUSIONThe significant increase in urine volume 24 h after treatment followed a dose-response pattern. The excretion of Na+, K+ and Cl- caused a decrease in urine osmolarity. The stability of aldosterone, the absence of correlation with the plasma levels of sodium, and increased clearance of free water in animals treated with aqueous extract suggest that increased diuresis and moderate natriuresis elevation were of tubular origin.

Animals ; Carbonic Anhydrase Inhibitors ; pharmacology ; Diuretics ; pharmacology ; Electrolytes ; metabolism ; Female ; Furosemide ; pharmacology ; Hydrochlorothiazide ; pharmacology ; Kidney ; drug effects ; physiology ; Male ; Plant Bark ; Plant Extracts ; pharmacology ; Rats ; Rats, Wistar ; Zanthoxylum ; chemistry