Medicinal plants are potential sources of anticancer agents screening. A large number of phytochemicals, including triterpenoids, have been reported to have significant cytotoxic effects on cancer cells. From the fruits of Ligustrum japonicum Thunb., thirteen triterpenoids (1 – 13) were isolated and evaluated for their cytotoxic activity against Hela and HL-60 cells. As results, 8 (oleanolic acid) showed significant effects on Hela with IC50 values of 5.5 µM, and moderate effects on HL-60 cells with IC₅₀ values of 55.9 µM. Meanwhile, 10 (oleanderic acid) and 11 (3β-acetoxy-urs-12-en-28-oic acid) exhibited moderate inhibitory effects on Hela with IC₅₀ value of 55.0 and 68.8 µM, respectively. Moreover, 10 showed cytotoxic effect on HL-60 cell line with IC₅₀ value of 63.9 µM. To our knowledge, this is the first report that oleanderic acid was isolated from L. japonicum and investigated in cytotoxic effects on Hela and HL-60 cells.
Antineoplastic Agents ; Fruit ; HL-60 Cells ; Humans ; Inhibitory Concentration 50 ; Ligustrum ; Mass Screening ; Nerium ; Oleaceae ; Phytochemicals ; Plants, Medicinal

By Silica gel, Sephadex LH-20 and other materials for isolation and purification and by physicochemical methods and spectral analysis for structural identification, 23 compounds were isolated and identified from ethyl acetate portion of alcohol extract solution of Osmanthus fragrans fruits. Their structures were identified as nicotinamide (1), D-allitol (2), 5-hydroxymethyl-2-furancarboxaldehyde (3), acetyloleanolic acid (4), benzoic acid (5), ergosta-7,22-dien-3-one (6), beta-sitosterol (7), borreriagenin (8), cerevistero (9), c-veratroylglycol (10), methyl-2-O-beta-glucopyranosylbenzoate (11), 3', 7-dihydroxy-4'-methoxyisoflavon (12), umbelliferone (13), caffeic acid methyl ester (14), oleanolic acid (15), (-) -chicanine (16), dillapiol (17), 3beta,5alpha, 9alpha-trihydroxyergosta-7-22-dien-6-one (18), 2alpha-hydroxy-oleanolic acid (19), betulinic acid (20), betulin (21), 3, 3'-bisdemethylpinoresinol (22), and lupeol (23). All compounds were isolated from the osmanthus fruit for the first time. Except for compounds 4, 7, 15, 19, 23, the rest ones were isolated from the this plant for the first time.
Drugs, Chinese Herbal ; chemistry ; Fruit ; chemistry ; Oleaceae ; chemistry

OBJECTIVETo investigate the preparation of Shuanghuanglian taste-masking microspheres by spray-drying.

METHODTraced the compounds bitterness source, marked its curve and optimized the microspheres preparation by taking taste evaluation, microspheres yield and inclusion rate as the indexes.

RESULTThe bitter taste of compounds comes from Forsythia suspensa. The best taste-masking material is Eudragit E100. The optimal spray-drying parameters: solvent concentration 2.0%, inlet air temperature 75 degrees C, aspirator 35.0 m3 x h(-1), spray flow 0.35 m3 x h(-1), pump speed 8.0 mL x min(-1).

CONCLUSIONThe spray-drying as a method of masking the traditional Chinese medicine compound taste have advantages of simple process and efficient masking.

Acrylates ; chemistry ; Desiccation ; Drug Combinations ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Forsythia ; chemistry ; Microspheres ; Oleaceae ; chemistry ; Plants, Medicinal ; chemistry ; Polymers ; chemistry ; Taste ; Technology, Pharmaceutical ; methods

OBJECTIVETo study the effect of different processing methods on the content and biological activity of main chemical constituents of Forsytiae Fructus, in order to provide the basis for rational processing of Forsytiae Fructus.

METHODThe content of extracts was determined by the extract determination method of Chinese Pharmacopoeia. The effects of chemical constituents of Forsytiae Fructus under different processing conditions were compared by HPLC method. Furthermore, free radical scavenging DPPH method was used to assess the antioxidation effect, and the antibacterial effect of Forsytiae Fructus was evaluated according to the inhibition effect on staphylococcus aureus.

RESULTConsidering various factors, the optimum boiling process is that adding six-fold water and boiling for 8 min.

CONCLUSIONThe content and activity of chemical constituents of Forsytiae Fructus are significantly different under different processing conditions.

Chemistry, Pharmaceutical ; methods ; Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal ; chemistry ; Fruit ; chemistry ; Oleaceae ; chemistry

AIM: To investigate the in vitro antioxidant activity and total phenolic content of the methanolic leaf extract of Nyctanthes arbor-tristis L. (NA). METHODS: The sample was tested using five in vitro antioxidant methods (1, 1-diphenyl-2-picryl hydrazine radical scavenging activity (DPPH), hydroxyl radical-scavenging activity (-OH), nitric oxide scavenging activity (NO), superoxide radical-scavenging activity, and total antioxidant activity) to evaluate the in vitro antioxidant potential of NA and the total phenolic content (Folin-Ciocalteu method). The extract showed good free radical scavenging property which was calculated as an IC50 value. RESULTS: IC50 (Half maximal inhibitory concentration) of the methanolic extract was found to be 57.93 μg·mL(-1) for DPPH, 98.61 μg·mL(-1) for -OH, 91.74 μg·mL(-1) for NO, and 196.07 μg·mL(-1) for superoxide radical scavenging activity. Total antioxidant capacity of the extract was found to be (1198 ± 24.05) mg ascorbic acid for the methanolic extract. Free radical scavenging activity observed in the extracts of NA showed a concentration-dependent reaction. The in vitro scavenging tested for free radicals was reported to be due to high phenolic content in the leaf extract. The leaf extract of NA showed the highest total phenolic content with a value of 78.48 ± 4.2 equivalent mg TAE/g (tannic acid equivalent). CONCLUSIONS N. arbor-tristis leaf extract exhibited potent free radical scavenging activity. The finding suggests that N. arbor-tristis leaves could be a potential source of natural antioxidant.
Antioxidants ; chemistry ; Oleaceae ; chemistry ; Phenols ; chemistry ; Plant Extracts ; chemistry ; Plant Leaves ; chemistry

By Silica gel, Sephadex LH-20 and other materials for isolation and purification and by physicochemical methods and spectral analysis for structural identification, 32 compounds were isolated and identified from ethyl acetate portion of alcohol extract of the Osmanthus fragrans. Their structures were identified as boschniakinic acid (1), ursolaldehyde (2), augustic acid (3), arjunolic acid (4), 5-hydroxymethyl-2-furancarboxaldehyde (5), isoscutellarein (6), 6, 7-dihydroxycoumarin (7), 2α-hydroxy-oleanolic acid (8), quercetin-3-0-β-D-glu-copyranoside (9), D-allito (10), 5, 4'-dihydroxy-7- methoxyflavone-3-0-β-D-glucopyranoside (11), 5,7-dihydroxychromone (12), lupeol (13), naringenin (14), acetyloleanolic acid (15), chlorogenic acid (16), kaempferol-3-0-β- D-glucopyranoside (17), oleanolic acid (18), kaempferol-3-0-β-D-galactopyanoside (19), 3', 7-dihydroxy-4'-methoxyisoflavon (20), ergosta-4,6,8 (14), 22-tetraen-3-one (21), p-hydroxycinnamic acid (22), syringaresinol (23), 3,4-dihydroxyacetophenonel (24), β-sitosterol (25), ethyl p-hydroxyphenylacetate (26), benzoic acid (27), caffeic acid (28), coelonin (29), p-hydorxy-phenylacetic acid (30), p-hydroxyacetophenone (31), and methyl-p-hydroxphenylacetate (32). Except for compounds 2, 4, 5, 8-11, 13, 15, 18, 20, 25, and 27, the rest were isolated from the Osmanthus fragrans for the first time.
Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Molecular Structure ; Oleaceae ; chemistry ; Plants, Medicinal ; chemistry ; Spectrometry, Mass, Electrospray Ionization

OBJECTIVETo study the modulation effect of pro- and anti-inflammatory cytokines following long term use of water soluble ethanol extracts from different organs of Nyctanthes arbortristis (NAT) in mouse model of arthritis.

METHODSArthritis was induced in mice by two injections of Freund's complete adjuvant on days 0 and 12 in the sub-planter surface of the right hind paw.

RESULTSInjection of adjuvant resulted in a maximum primary edema of the footpad with erythema, and edema and distortion of joints of the right hind paw after 24-48 hours. Second injection of FCA led to the formation of secondary swellings persisting more than four weeks that spread onto the other hind limb but to a lesser extent. Histological analysis of the ankle on day 47 showed marked evidence of cartilage destruction in association with pannus formation and moderate bone resorption. Proinflammatory cytokine levels in the inflamed joint homogenate were elevated on days 2, 14, and 47. Oral administration of leaf and fruit extracts in arthritic mice reduced joint homogenate levels of tumor necrosis factor-alpha, interleukin-1beta, and interleukin-6 on days 2, 14, and 47 in comparison to untreated arthritic mice. Interleukin-10 level was elevated in the inflamed joint on days 2, 14, and 47 in comparisons to untreated arthritic mice.

CONCLUSIONEvidence of lesser inflammation of the footpad and joint and associated histological observation support the therapeutic benefit of leaf and fruit extracts from Nyctanthes arbortristis. This study helps in understanding the mechanism of anti-inflammatory action of Nyctanthes arbortristis in the light of pro- and anti-inflammatory cytokine balance.

Animals ; Arthritis, Experimental ; drug therapy ; immunology ; pathology ; Cytokines ; metabolism ; Disease Models, Animal ; Female ; Mice ; Mice, Inbred BALB C ; Oleaceae ; chemistry ; Phytotherapy ; Plant Extracts ; isolation & purification ; therapeutic use

OBJECTIVETo investigate the pharmacological effect of Nyctanthes arbortristis (NAT) leaf extract in the prevention of lung injury induced by silica particles.

METHODLung injury was induced in Swiss mice through inhalation exposure to silica particles (< 5 mu) using a Flow Past Nose Only Inhalation Chamber at the rate of -10 mg/m3 respirable mass for 5 h. Lung bronchoalveolar lavage (BAL) fluid collected between 48 and 72 h was subjected to protein profiling by electrophoresis and cytokine evaluation by solid phase sandwich ELISA. Lung histopathology was performed to evaluate lung injury.

RESULTSInhalation of silica increased the level of tumor necrosis factor-alpha (TNF-alpha), and of the 66 and 63 kDa peptides in the BAL fluid in comparison to sham-treated control. Pre-treatment of silica exposed mice with NAT leaf extract significantly prevented the accumulation of TNF-alpha in the BAL fluid, but the 66 and 63 kDa peptides remained unchanged. The extract was also effective in the prevention of silica-induced early fibrogenic reactions like congestion, edema and infiltration of nucleated cells in the interstitial alveolar spaces, and thickening of alveolar septa in mouse lung.

CONCLUSIONNAT leaf extract helps in bypassing silica induced initial lung injury in mice.

Administration, Oral ; Animals ; Bronchoalveolar Lavage Fluid ; Disease Models, Animal ; Enzyme-Linked Immunosorbent Assay ; Inhalation Exposure ; Male ; Mice ; Oleaceae ; chemistry ; Phytotherapy ; Plant Extracts ; pharmacology ; Pulmonary Fibrosis ; etiology ; prevention & control ; veterinary ; Silicon Dioxide ; adverse effects ; Silicosis ; prevention & control ; veterinary

Bee propolis ethanolic extract with some plant essential oils was investigated for its antidermatophytic properties. The tested plant essential oils included jasmine, clove, lemon, Arabian jasmine, mint, rosa, olive and basil. The antidermatophytic activity has been compared to Naftifine-HCl and Clotrimazole used for dermatophyte treatment. Experimental model has been tested using sheep hoof plate for the in vitro tests to stimulate human nails. Mint, clove and basil with 4 mg/ml of bee propolis have a comparable efficacy to those of Naftifine-HCl and Clotrimazole. There is a great necessity for new effective low price and safe antidermatophyte agents to avoid recurrent infection. Propolis synergistic could be of great importance with essential oils of plants in dermatophyte therapy.
Animals ; Arthrodermataceae ; Bees* ; Clotrimazole ; Ethanol ; Syzygium ; Hoof and Claw* ; Humans ; Jasminum ; Mentha ; Models, Theoretical* ; Ocimum basilicum ; Oils, Volatile* ; Olea ; Plants* ; Propolis* ; Rosa ; Sheep*

BACKGROUND: Osmanthus matsumuranus, a species of Oleaceae, is found in East Asia and Southeast Asia. The bioactivities of O. matsumuranus have not yet been fully understood. Here, we studied on the molecular mechanisms underlying anti-cancer effect of ethanol extract of O. matsumuranus (EEOM). METHODS: Inhibitory effect of EEOM on cell growth and proliferation was determined by WST assay in various cancer cells. To investigate the mechanisms of EEOM-mediated cytotoxicity, HepG2 cells were treated with various concentration of EEOM and analyzed the cell cycle arrest and apoptosis induction by flow cytometry, Western blot analysis, 4,6-diamidino-2-phenylindole (DAPI) staining and DNA fragmentation. RESULTS: EEOM showed the cytotoxic activities in a dose-dependent manner in various cancer cell lines but not in normal cells, and HepG2 cells were most susceptible to EEOM-induced cytotoxicity. EEOM induced G2/M arrest in HepG2 cells associated with decreased expression of cyclin-dependent kinase 1 (CDK1), cyclin A and cylcin B, and increased expression of phospho-checkpoint kinase 2, p53 and CDK inhibitor p21. Immunofluorescence staining showed that EEOM-treated HepG2 increased doublet nuclei and condensed actin, resulting in cell rounding. Furthermore, EEOM-mediated apoptosis was determined by Annexin V staining, chromatin condensation and DNA fragmentation. EEOM caused upregulation of FAS and Bax, activation of caspase-3, -8, -9, and fragmentation of poly ADP ribose polymerase. CONCLUSIONS: These results suggest that EEOM efficiently inhibits proliferation of HepG2 cells by inducing both G2/M arrest and apoptosis via intrinsic and extrinsic pathways, and EEOM may be used as a cancer chemopreventive agent in the food or nutraceutical industry.
Actins ; Annexin A5 ; Apoptosis* ; Asia, Southeastern ; Blotting, Western ; Carcinoma, Hepatocellular* ; Caspase 3 ; CDC2 Protein Kinase ; Cell Cycle Checkpoints ; Cell Line ; Chromatin ; Cyclin A ; Dietary Supplements ; DNA Fragmentation ; Ethanol ; Far East ; Flow Cytometry ; Fluorescent Antibody Technique ; Hep G2 Cells* ; Humans* ; Oleaceae ; Phosphotransferases ; Poly(ADP-ribose) Polymerases ; Up-Regulation