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Objective: To investigate the efficacy and mechanism of EGDT against NPC cell lines. Methods: MTT assay was used to assess cell proliferation inhibition of EGDT. The apoptotic induction and cell cycle arrest were detected by flow cytometry. Western blot was adopted to detect the protein levels. Quantitative Real-time PCR was used to determine the mRNA expressions. The NPC xenografts were established to evaluate the tumor growth inhibition of EGDT. Immunohistochemistry was applied to analyze the EGFR expression in the tumor tissues. Results: EGDT showed proliferation inhibition on the NPC cell, induced G0/G1 phase arrest and cell apoptosis in vitro. EGDT decreased the protein and mRNA levels of EGFR and its downstream RAF/MEK/ERK and PI3K/AKT pathways in time- and dose-dependent manner. Furthermore, EGDT also showed a sound antitumor activity in NPC xenograft in vivo. Conclusion: The treatment of EGDT displays EGFR and its mediated downstream signaling pathway blockade through decreasing the protein and mRNA levels, suggesting a promising strategy in treating human NPC.
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OBJECTIVE: To study the chemical constituents of Catharanthus roseus. METHODS: Various column chromatograghic methods on silica gel, Rp-18, and Sephadex LH-20 were applied for the isolation and purification of the 95% ethanol extract. The structures were elucidated by their physicochemical properties and spectral data. RESULTS: Twenty-two compounds were obtained and identified as ursolic acid (1), daucesterol (2), tetrahydroalstonine (3), 7α-hydroxy-β-sitosterol (4), vindoline (5), β-sitosterol (6), aurantiamide acetate (7), lochnericine (8), oleanolic acid (9), ajmalicine (10), (22E, 24R)-ergosta-7, 22-dien-3β, 5α, 6β-triol (11), betulinic acid (12), stigmasterol (13), quercetin (14), keampferol (15), vindorosine (16), catharanthine (17), diaaurantiamide acetate (18), reserpine (19), panarine (20), serpentine (21), and 16R-E-isositsirikine (22). CONCLUSION: Compounds 4, 7, 11, 13, 18, and 20 are isolated from C. roseus for the first time.
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Objective: To study chemical components of rhizome of Arundo donax, a folk medicine. Methods: Using different methods such as chromatography and recrystallization purification to get chemical components, and the structures were identified by physical and chemical properties and spectral data. Results: Twenty-three compounds were isolated and identified as following: hexadecanoic acid (1), n-docosane (2), myristic acid glycerides (3), 5,6-epoxy-22,24-ergosta-8(14),22-diene-3,7-diol (4), 5,6-epoxy-22,24-ergosta-8(9),22-diene-3,7-diol (5), 5,8-epidioxy-22,24-ergosta-6,22-dien-3-ol (6), stigmast-4-ene-3,6-dione (7), 6,9-epoxy-ergosta-7,22-dien-3-ol (8), stigmast-22-en-3,6, 9-triol (9), 3,4,5-trimethoxyphenol (10), 2,6-dimethoxy-1,4-quinone (11), sinapaldehyde (12), hydroxycinnamic acid (13), β-sitostenone (14), α-asarone (15), 4-dodecylbenzaldehyde (16), β-sitosterol (17), α-spinasterol (18), p-hydroxybenzaldehyde (19), ursolic acid (20), N-acetyltryptamine (21), daucosterol (22), and (-)-syringaresinol (23). Conclusion: Compouds 1-16 and 18-23 are isolated from the plant in genus Arundo L. for the first time.
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OBJECTIVE: To investigate the antibacterial agents in the marine fungus Penicillium sp. F00120 from the deep sea sediments in the South China Sea. METHODS: The compounds were purified by a combination of chromatographic methods, and their structures were identified by MS, 1H-NMR, and 13C-NMR spectroscopic analysis. The antimicrobial activities of the isolates were evaluated by the agar plate diffusion method. RESULTS: Eight compounds were isolated from the culture and were characterized as ergosta-4, 6, 8(14), 22-tetraen -3-one(1), 25-hydroxyergosta4, 6, 8(14), 22-tetraen-3-one(2), ergosta-7, 22-dien-3β, 5α, 6β-triol (3), ergosta-5, 7, 22-trien-3β-ol(4), 5α, 8α-epidioxyergosta-6, 22-dien-3β-ol(5), 5α, 6α-epoxyergost-8(14), 22-dien-3β, 7α-diol(6), cholesterol(7), and 4-hydroxyacetophenone(8), respectively. CONCLUSION: Compounds 1-3 and 6-8 are isolated from this fungus for the first time. Compounds 3, 4, and 8 shows moderate antibacterial activities against P. aeruginosa, S. aureus, and E. coll.
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Objective: This study focused on the secondary metabolites of endophytic fungus Fusarium chlamydosporum in Dioscorea opposite. Methods: Compounds were isolated from the MeOH extract by chromatography technology and their structures were elucidated on the basis of comprehensive spectroscopic analysis. Results: Eight compounds were isolated and their structures were identified as: ergosterol-5α, 8α-peroside (1), ergosta-4, 22-dien-3-one (2), di-n-butyl phthalate (3), di-isobutyl phthalate (4), 3-pyridinecarboxylic acid (5), amber acid (6), pentanedioic acid (7), and Nb-acetyltrytamine (8). Conclusion: All these compounds are isolated from F. chlamydosporum for the first time.
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Objective: To study the triterpenoids from the fruiting body of Inonotus obliquus. Methods: The compounds were isolated and purified by silica gel, MCI gel, Sephadex LH-20 column chromatographies, and their structures were mainly elucidated on the basis of physicochemical characteristics and spectral analysis. Results: Fifteen compounds were isolated from 95% EtOH extract of I. obliquus, and were identified as 3-oxo-lanosta-8, 24-diene-21-al (1), lanosterol (2), 3β-hydroxy-lanosta-8, 24-diene-21-al (3), betulin (4), inotodiol (5), trametenolic acid (6), 3β, 21-dihydroxy-lanosta-8, 24-diene (7), oleanic acid (8), ursolic acid (9), betulinic acid (10), inonotusane A (11), inoterpene D (12), 3-O-acetyl-11α, 12α-epoxy-oleanan-28, 13β-olide (13), ergosterol (14), and ergosta-4, 6, 8, 22-tetraene-3-one (15), respectively. Conclusion: Compound 1 is a new triterpenoid named as inonotusane D, while compounds 9, 13, and 15 are isolated from I. obliquus for the first time.
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Objective: To study the chemical constituents of Russula foetens. Methods: The chemical constituents were isolated by repeated silica gel and Sephadex LH-20 column chromatography, and their structures were elucidated by 1H-NMR, 13C-NMR, 2D-NMR (1H-1H COSY, HMQC, HMBC, NOESY), HR-MS, CD, and IR. Results: Eleven compounds were isolated from the fruiting bodies of R. foetens. Of which, six marasmane sesquiterpenes: 8β, 13-dihydroxy-marasm-5β-methoxy γ-acetal (1), 13-hydroxy-marasm-7(8)-en-5-methoxy γ-acetal (2), 8β, 13-dihydroxy-marasm-5-oic acid γ-lactone (3), 8β, 13, 14-trihydroxy- marasm-5-oic acid γ-lactone (4), 7, 8, 13-trihydroxy-marasm-5-oic acid γ-lactone (5), and lactapiperanol A (6); three steroids: (22E, 24R)-ergosta-7, 22-dien-3, 5, 6-triol (7), ergosta-5, 7, 22-trien-3-ol (8), 3-hydroxy-5, 8-epidioxy-ergosta-6, 22-dien (9); and uridine (10), D-allitol (11) were identified. Conclusion: Compounds 1-4, named as russacetal, russacetalen, russunone, and russunoneol respectively, are new compounds isolated from R. foetens. Compounds 7, 8, 10, and 11 in this fungus are first reported.
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OBJECTIVE: To study the chemical constituents of whole plant of Physalis angulata L. METHODS: The constituents were isolated and purified by chromatographic methods and their structures were elucidated by spectroscopic methods and physio-chemical analysis. RESULTS: Thirteen known compounds was isolated and identified as physalin A (1), physalin B (2), physalin E (3), physalin P(4), stigmast-5-en-3β-ol (5), ergost-5, 24 (28) -diene-3β-ol (6), brassicaaterol (7), stigmasta-22-en-3, 6-dione (8), pregn-5-en-3-ol-20-carboxylic acid (9), ergost-5, 24 (28)-diene-3β, 23S-diol (10), ergosta-5, 25 (26)-diene-3, 24ξ-diol(11), n-hexade-canoic acid (12), and n-heptadecanoic acid (13). CONCLUSION: All of the compounds except 2 and 3 are isolated from this plant for the first time, and compounds 5-10 and 12-13 are isolated from Physalis for the first time.
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OBJECTIVE: To prepare folate-conjugated ergosta-4,6,8,22-tetraen-3-one liposomes(FLE). Then to study the release feature of FLE in vitro and the eytotoxieity and targeting ability of it via folate receptor-mediated endocytosis on tumor cells in vitro. Pharmacokinetic characterization was also studied in rats. METHODS The characteristics were measured by transmission electron microscope(TEM), laser light scattering granularity equipment and HPLC. Dialytic method was used to determine ergone release rate of FLE in vitro. The cytotoxicity and targeting ability of FLE on HeLa in vitro was measured by MTT assay. The concentrations of ergone in plasma of rats and their pharmacokinetic behaviors after oral administration were studied by HPLC. The pharmacokinetic parameters were computed by software DAS2.0. RESULTS: The prepared FLE was round and uniform, and the mean particle size was 112 nm. The encapsulating efficiency of it reached 73%. The experiment of drug release in vitro follows Higuchi releasing process and showed significant sustained-release feature. The IC50 of ergone, LE and FLE was 10, 14, 5 μg · mL-1, respectively. Compared with ergone solution, AUC in FLE had increased significantly. And the residence time of ergone was prolonged. CONCLUSION: The FLE were characterized by sustained-release performance, target recognition, and low toxic and side effect and did improve the bioavailability of ergone significantly. It can also be expected to be used for tumor by targeting therapy.
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Objective: To study the constituents of the stem in Dendrobium crystallinum. Methods: Compounds were isolated and purified by silica gel, Sephadex LH-20, ODS, and MCI column chromatography. Their structures were identified by physicochemical properties and spectral analyses. Results: Ten compounds were obtained and identified as 4′-hydroxy-3,3′,5- trimethoxybibenzyl (1), 5′-hydroxy-3,3′,4-trimethoxybibenzyl (2), 3,3′-dihydroxy-5-methoxybibenzyl (batatasin III) (3), 3,4′- dihydroxy-5-methoxybibenzyl (4), kaempferol (5), 6″-0-(3‴-hydroxy- 3‴-methylglutaroyl) vitexin (6), ursone (7), ergosta-7,22-diene-3β, 5α,6β-triol (8), uridine (9), and (+)-syringaresinol (10). Conclusion: All these compounds are isolated from this plant for the first time, compounds 6 and 9 are obtained from the plants of Orchidaceae for the first time, and compounds 2 and 8 are obtained from the plants of Dendrobium Sw. for the first time.
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Gymnopilus spectabilis, a hallucinogenic mushroom belonging to the family Cortinariaceae, is found growing in dense clusters on stumps and logs of hardwoods and conifers. It contains the hallucinogenic alkaloid psilocybin and its strongly bitter taste makes it undesirable as an edible. In an effort to identify chemical constituents of Korean native wild mushrooms, 4,6-decadiyne-1,3,8-triol (1), ergosta-4,6,8(14), 22-tetraen-3-one (2), bisnoryangonin (3), and hispidin (4) were isolated from the methanolic extract of the fruiting bodies of G. spectabilis. Their structures were assigned on the basis of various spectroscopic studies. Compounds 3 and 4 displayed significant scavenging activity against the ABTS radical cation, DPPH radical, and superoxide radical anion, while 1 and 2 exhibited no antioxidant activity.
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Humans , Agaricales , Benzothiazoles , Tracheophyta , Fruit , Methanol , Pyrones , Sulfonic Acids , SuperoxidesABSTRACT
s:The chemical constituents of gliocladium roseum(called Y)accelerating the growth of famous medicin al plant Anoectochilus roxburghiiwas studied.Five comp ounds were separated by silica gel column chromatograph from this fungal mycelia and their structures were elu cidated by the data of IR,NMR,UV and MS.Compound I was 6,22-diene-3-hydroxy- 5,8-epidioxy ergosta,compound 2 is ergosterol,compound 3 is D-arabitol and com pound 4 is mannitol.