BACKGROUND: Metronidazole has been known as the most effective drug for treatment of Trichomonas vaginalis-related diseases. However, it has been reported that metronidazole has adverse effects and incidence of metronidazole-resistant T. vaginalis (CDC085) has increased. Development of new drug, which is effective against metronidazole-resistant T. vaginalis and showing no adverse effects, has been required. METHODS: The purpose of this study was to investigate effects of various extracts from herbs such as Quisqualis indica, Gleditsia sinensis, Prunus armeniaca, Morus alba, Platycodon grandiflorum, Ailanthus altissima, Stemona japonica, Biota orientalis, Dryobalanops aromatica, and Cimicifuga heracleifolia on metronidazole resistant strain of T. vaginalis in vitro (CDC085). RESULTS: Anti-Trichomonas activities were observed in T. vaginalis treated with G. sinensis, P. armeniaca, and P. grandiflorum on the growth and fine structure of metronidazole resistant strain of T. vaginalis. Of the three standard extracts that showed the most effective anti-trichomonas activity, G. sinensis was the most effective. The inhibitory effects of fraction extracts of this drug were shown on the growth of T. vaginalis. The fine structure of the cytoplasm was changed after application of G. sinensis extract. The number of polyribosome and hydrogenosome decreased whereas the number of food vacuole and vacuole in the cytoplasm increased, compared with that of untreated control group. CONCLUSION: The results of our study indicate that G. sinensis may induce the inhibition of cell multiplication as well as impairment of protein synthesis of metronidazole resistant strain of T. vaginalis in vitro.
Ailanthus ; Cell Proliferation ; Cimicifuga ; Cytoplasm ; Dipterocarpaceae ; Gleditsia ; Incidence ; Metronidazole* ; Morus ; Platycodon ; Polyribosomes ; Prunus armeniaca ; Stemonaceae ; Thuja ; Trichomonas vaginalis* ; Trichomonas* ; Vacuoles

BACKGROUND: Metronidazole has been known as the most effective drug for treatment of Trichomonas vaginalis-related diseases. However, it has been reported that metronidazole has adverse effects and incidence of metronidazole-resistant T. vaginalis (CDC085) has increased. Development of new drug, which is effective against metronidazole-resistant T. vaginalis and showing no adverse effects, has been required. METHODS: The purpose of this study was to investigate effects of various extracts from herbs such as Quisqualis indica, Gleditsia sinensis, Prunus armeniaca, Morus alba, Platycodon grandiflorum, Ailanthus altissima, Stemona japonica, Biota orientalis, Dryobalanops aromatica, and Cimicifuga heracleifolia on metronidazole resistant strain of T. vaginalis in vitro (CDC085). RESULTS: Anti-Trichomonas activities were observed in T. vaginalis treated with G. sinensis, P. armeniaca, and P. grandiflorum on the growth and fine structure of metronidazole resistant strain of T. vaginalis. Of the three standard extracts that showed the most effective anti-trichomonas activity, G. sinensis was the most effective. The inhibitory effects of fraction extracts of this drug were shown on the growth of T. vaginalis. The fine structure of the cytoplasm was changed after application of G. sinensis extract. The number of polyribosome and hydrogenosome decreased whereas the number of food vacuole and vacuole in the cytoplasm increased, compared with that of untreated control group. CONCLUSION: The results of our study indicate that G. sinensis may induce the inhibition of cell multiplication as well as impairment of protein synthesis of metronidazole resistant strain of T. vaginalis in vitro.
Ailanthus ; Cell Proliferation ; Cimicifuga ; Cytoplasm ; Dipterocarpaceae ; Gleditsia ; Incidence ; Metronidazole* ; Morus ; Platycodon ; Polyribosomes ; Prunus armeniaca ; Stemonaceae ; Thuja ; Trichomonas vaginalis* ; Trichomonas* ; Vacuoles

To synthesize a series of 3-, 4-, and/or 11-trihydroxy modified bergenin derivatives and evaluated their cytotoxic activity in vitro. The phenolic hydroxyl groups of bergenin were protected by benzyl groups with benzyl bromide. Treatment of dibenzyl bergenin with the corresponding acid in the presence of EDC·HCl and DMAP in CH2Cl2, followed by hydrogenation over Pd/C catalysts, afforded derivatives of bergenin esters. All of the target compounds were identified by IR, MS, and (1)H NMR. Twenty-six novel and three known derivatives of bergenin esters were synthesized. Their cytotoxicity values were evaluated by the MTT assay on the inhibition of DU-145 and BGC-823 cells in vitro. Several triply-substituted (3a, 4a, 5a, 6a, 7a) and doubly-substituted (8b, 9b) bergenin derivatives exhibited higher cytotoxic activity than bergenin. The result showed that the size of substituents and the lipophilicity of the bergenin esters displayed an important role on their cytotoxic activity.
Antineoplastic Agents, Phytogenic ; chemical synthesis ; pharmacology ; therapeutic use ; Benzopyrans ; pharmacology ; therapeutic use ; Cell Line, Tumor ; Dipterocarpaceae ; chemistry ; Humans ; Male ; Molecular Structure ; Phytotherapy ; Plant Extracts ; pharmacology ; therapeutic use ; Prostatic Neoplasms ; drug therapy ; Stomach Neoplasms ; drug therapy ; Structure-Activity Relationship

The present study was designed to examine the anti-hyperuricemic and anti-inflammatory effects and possible mechanisms of vaticaffinol, a resveratrol tetramer isolated from ethanol extracts of Dipterocarpus alatus, in oxonate-induced hyperuricemic mice. At 1 h after 250 mg·kg potassium oxonate was given, vaticaffinol at 20, 40, and 60 mg·kg was intragastrically administered to hyperuricemic mice once daily for seven consecutive days. Vaticaffinol significantly decreased serum uric acid levels and improved kidney function in hyperuricemic mice. It inhibited hepatic activity of xanthine dehydrogenase (XDH) and xanthine oxidase (XOD), regulated renal mRNA and protein levels of urate transporter 1 (URAT1), glucose transporter 9 (GLUT9), organic anion transporter 1 (OAT1), organic cation transporter 1 (OCT1), OCT2, organic cation/carnitine transporter 1 (OCTN1), and OCTN2 in hyperuricemic mice. Moreover, vaticaffinol markedly down-regulated renal protein levels of NOD-like receptor 3 (NLRP3), apoptosis-associated speck-like (ASC), and Caspase-1, resulting in the reduction of interleukin (IL)-1β, IL-18, IL-6 and tumor necrosis factor-α (TNF-α) levels in this animal model. Additionally, HPLC and LC-MS analyses clearly testified the presence of vaticaffinol in the crude extract. These results suggest that vaticaffinol may be useful for the prevention and treatment of hyperuricemia with kidney inflammation.
Animals ; Anti-Inflammatory Agents ; administration & dosage ; Dipterocarpaceae ; chemistry ; Humans ; Hyperuricemia ; blood ; drug therapy ; immunology ; Interleukin-18 ; genetics ; immunology ; Interleukin-1beta ; genetics ; immunology ; Interleukin-6 ; genetics ; immunology ; Kidney ; drug effects ; immunology ; Male ; Mice ; Organic Anion Transport Protein 1 ; genetics ; immunology ; Plant Extracts ; administration & dosage ; Stilbenes ; administration & dosage ; Tumor Necrosis Factor-alpha ; genetics ; immunology ; Uric Acid ; blood