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Aim To investigate the effect of p-hydroxybenzaldehyde ( HD) on intestinal fibrosis in mice based on mouse intestinal fibrosis model and in vitro EMT model,and to explore the underlying mechanism Methods HE staining, Masson staining, immunohisto-chemistry ,qPCR, Western blot and other experimental methods were used to verify the effect of HD on intestinal fibrosis in mice and the potential mechanism. Results In vivo experiments showed that compared with the normal group, the DSS-induced intestinal fibrosis model group had shortened colon, increased colon his-topathological score, increased collagen volume fraction, and significantly increased collagen I expression. After treatment with 4, 10, and 25 mg • kg
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Abstract Beagles are less susceptible to Rhipicephalus sanguineus sensu lato tick due to the production of the allomones benzaldehyde and 2-hexanone. Our previous published work showed that these compounds can reduce tick burden on susceptible dogs. Here we tested the hypothesis that an increase in repellent dose and release rate could increase repellent efficacy and persistence. Slow-release formulations of these compounds, with higher doses and release rates, were tested on artificially-infested dogs. Ten dogs were randomly assigned to two groups with five dogs each. The treated group received collars with slow-release formulations of the compounds attached, while the control group received collars with clean formulations attached. Five environmental infestations were performed, with the number of ticks (at all stages) on the dogs being counted once a day for 40 days. No significant increase in repellent efficacy was observed with the higher doses and release rates, whereas a greater persistence in repellent activity was observed. Treatment with the formulations resulted in a two-to-three-fold reduction in the number of immature stage ticks for up to three weeks. However, the number of adults was similar in both groups. Loss of repellent activity after the third week of testing coincided with a marked change in the relative release rates for the two compounds. It is hypothesized that relative amounts, rather than absolute amounts, of repellent release from slow-release formulations are important for repellent activity. We also hypothesize that the avoidance of less-preferred hosts by ticks relies on olfactory-mediated perception of specific blends of volatile cues from less preferred hosts.
Resumo Beagles são menos suscetíveis ao carrapato Rhipicephalus sanguineus sensu lato devido à produção de benzaldeído e 2-hexanona. Nosso trabalho anterior já publicado mostrou que esses compostos podem reduzir a carga de carrapatos em cães suscetíveis. Aqui testamos a hipótese de que um aumento na dose destes repelentes e na taxa de liberação poderia aumentar a eficácia e a persistência do efeito repelente. As formulações de liberação lenta destes compostos, com doses e taxas de liberação mais elevadas foram testadas em cães infestados artificialmente. Dez cães foram distribuídos aleatoriamente em dois grupos com cinco cães cada. O grupo tratado recebeu colares contendo formulações de liberação lenta dos compostos, enquanto o grupo controle recebeu colares com formulações limpas. Cinco infestações ambientais foram realizadas, com o número de carrapatos (em todas as fases) nos cães sendo contados, uma vez ao dia, por 40 dias. Não se observou aumento significativo na eficácia do repelente com doses e taxas de liberação mais elevadas e, enquanto observou-se maior persistência na atividade repelente. O tratamento com as formulações resultou em uma redução de duas a três vezes no número de carrapatos dos estágios imaturos, por até três semanas. No entanto, o número de adultos foi semelhante em ambos os grupos. A perda de atividade repelente após a terceira semana de teste coincidiu com uma mudança nas taxas de liberação relativa para os dois compostos. A hipótese é que as quantidades relativas, ao invés das quantidades absolutas de liberação lenta, são importantes para a atividade repelente. Então, a hipótese é de que a repelência apresentada por hospedeiros menos susceptíveis aos carrapatos depende da percepção pelos carrapatos de misturas específicas de voláteis liberados por estes hospedeiros.
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Animals , Male , Female , Dogs , Tick Infestations/veterinary , Benzaldehydes/administration & dosage , Rhipicephalus sanguineus/drug effects , Dog Diseases/prevention & control , Insect Repellents/administration & dosage , Methyl n-Butyl Ketone/administration & dosage , Tick Infestations/prevention & control , Time Factors , Case-Control Studies , Treatment OutcomeABSTRACT
Objective To investigate the chemical constituents from Disporum cantoniense. Methods Compounds were isolated and purified by macroporus resin, ods, Sephadex LH-20, MCI-gel CHP20 resin column chromatography and preparative HPLC. The structures were identified by spectral analysis. Results Twenty compounds were isolated and identified as 2-hydroxybenzyl alcohol (1), p-hydroxybenzaldehyde (2), 4-hydroxyacetophenone (3), 3,5-dimethoxy-4-hydroxy-benzaldehyde (4), 4-(4-hydroxyphenyl)-2- butanone (5), neoliquiritin (6), 2,3,5,4’-tetrahydroxy stilbene-2-Ο-β-D-glucoside (7), (E)-1-(4’-hydroxyphenyl)-but-1-en-3-one (8), isoquercitrin (9), 3-hydroxy-1-(4-hydroxy-3,5-dimethoxy-phenyl)-1-propanone (10), icariol A2 (11), ecdysterone (12), glansreginic acid (13), hesperidin (14), ononin (15), quercetin (16), isorhamnetin-3-O-β-D-glucoside (17), (E)-4-(4-hydroxy-3-methoxyphenyl) but-3-en-2-one (18), (-)-secoisolariciresinol (19), and luteolin (20). Conclusion Compounds 1, 3-8, 10-15, and 17-19 are isolated from the genus of Disporum for the first time.
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ABSTRACT This work describes the isolation, by high-speed counter-current chromatography, of the diterpenes manool, jhanol and steviol and the benzaldehyde p-oxy-2-ethylhexyl benzaldehyde from the stilt roots hexane extract of the mangrove plant Rhizophora mangle L., Rhizophoraceae. For this, a non-aqueous biphasic solvent system composed of hexane–acetonitrile–methanol 1:1:0.5 (v/v/v) was applied. As far as we know, only steviol was previously isolated in Rhizophoraceae and this is the first time that p-oxy-2-ethylhexyl benzaldehyde is reported.
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Objective To investigate the chemical constituents of Ajuga ovalifolia var. calantha. Methods The 95% ethanol extract from the whole herb of A. ovalifolia var. calantha was separated and purified by column chromatography over silica gel, Sephadex LH-20, ODS, and RP-HPLC. Their chemical structures were identified on the basis of physicochemical characteristics and spectral analyses. Results Thirteen compounds were isolated and identified as (16S)-12,16-epoxy-11,14-dihydroxy-17 (15→16)-abeo-abieta- 8,11,13-trien-7-one (1), ajuforrestin B (2), ajudecumin A (3), 14,15-dihydroajugapitin (4), cyasterone (5), β-sitosterol (6), acacetin (7), apigenin (8), luteolin (9), scopoletin (10), isoscopoletin (11), 4-hydroxy-3-methoxy-benzaldehyde (12), and acetovanillon (13). Conclusion Compounds 1 and 10-13 are reported from the genus Ajuga Linn., and compounds 2-5 and 7 are isolated from this plant for the first time. Single crystal X-ray diffraction experiment is carried out for compound 1, and the crystal structure data of single crystal X-ray diffraction of compound 1 is obtained for the first time.
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Objective:To establish a quality control method for Jingdu Niancian Milian Chuanbei Pipagao by quantitative analysis of multi-components by single marker ( QAMS) . Methods:GC was used with benzaldehyde as the internal standard,and the relative calibration factor of benzaldehyde and menthol was establish by GC and used for the content calculation of menthol by QAMS. Mean-while,the results of QAMS and those of the external standard method were compared. The effects of different instruments and chromato-graphic columns were studied to evaluate the accuracy and scientificity of QAMS applied in compound preparations. Results:No signif-icant differences in the quantitative results of benzaldehyde and menthol were found between the external standard method and QAMS. Conclusion:It is feasible and suitable to evaluate the quality of benzaldehyde and menthol in Jingdu Niancian Milian Chuanbei Pipagao by QAMS.
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Objective:To establish a quality control method for Jingdu Niancian Milian Chuanbei Pipagao by quantitative analysis of multi-components by single marker ( QAMS) . Methods:GC was used with benzaldehyde as the internal standard,and the relative calibration factor of benzaldehyde and menthol was establish by GC and used for the content calculation of menthol by QAMS. Mean-while,the results of QAMS and those of the external standard method were compared. The effects of different instruments and chromato-graphic columns were studied to evaluate the accuracy and scientificity of QAMS applied in compound preparations. Results:No signif-icant differences in the quantitative results of benzaldehyde and menthol were found between the external standard method and QAMS. Conclusion:It is feasible and suitable to evaluate the quality of benzaldehyde and menthol in Jingdu Niancian Milian Chuanbei Pipagao by QAMS.
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Objective:To determine the related substances in benzalkonium chloride used as a pharmaceutical adjuvant, and com-pare the quality at home and abroad. Methods:An HPLC method was used with an ODS-HYPERSIL C18 column(250 mm × 4. 6 mm, 5 μm). The detection wavelength was 210 nm and 257 nm. The flow rate was 1. 0 ml· min-1 and the column temperature was 30℃. The injection volume was 20 ml. The mobile phase was A ( dissolving 1. 09 g sodium1-hexanesulfonate and 6. 9 g sodium dihydrogen phosphate in water, adjusting pH to 3. 5 with phosphoric acid and diluting to 1 000. 0 ml) and B ( methanol) with gradient elution. Results:The content of benzaldehyde in the samples at home and abroad was low. The content of benzyl alcohol in the samples from a-broad was qualified, which was significantly higher than that in the domestic samples. The content of benzyl chloride in the domestic samples was higher than that in the samples from abroad. Conclusion:The method is simple and fast, which is suitable for comparing the related substances of domastic and imported samples. At the same time, the study provides basis for enterprises to choose benzalko-nium chloride rationally.
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Objective: To stuey the the chemical constituents from the residue left over the rectification of star anise oil (essential oil from Anisi Stellati Fructus). Methods: Two compounds were isolated from the residue left over the rectification of star anise oil by various chromatographic techniques, such as silica gel, and Sephadex LH-20 column chromatography. Results: Their structures were elucidated on the basis of chemical and spectral data. A new compound was identified to be 4-hydroxy-3-(3-methylbut-3-en-2-yl) benzaldehyde (2), along with a known compound (E)-1,4-bis (4-methoxyphenyl) but-3-en-2-one (1). Conclusion: NMR data of compound 1 are first reported and compound 2 is new one.
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Objective: To investigate the chemical constituents in the flower buds of Lonicera confusa. Methods: The chemical constituents were isolated by repeated silica gel chromatography, Sephadex LH-20, medium pressure column chromatography, and semi-preparative HPLC, and their structures were elucidated by spectroscopic analyses and comparison of NMR data with those reported in literature. Results: Ten compounds were isolated and identified to be chlorogenic acid (1), quercetin (2), luteolin (3), luteolin-3'-O-α-L-rhamnopyranoside (4), apigenin-7-O-α-L-rhamnopyranoside (5), trans-cinnamic acid (6), p-hydroxy benzaldehyde (7), gentisic acid-5-O-β-D-glucopyranoside (8), benzyl-β-D-glucoside (9), and abscisic acid (10). Conclusion: Compounds 4-10 are obtained from this plant for the first time.
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Objective: To study the chemical constituents in the whole herb of Coreopsis lanceolata and to investigate the antibacterial activity. Methods: The compounds in the whole herb of C. lanceolata were isolated and purified by column chromatography and identified based on spectral analyses (MS, NMR). The antibacterial activities of compounds 1-8 were screened. Results: Fifteen compounds including eight sesquiterpenes were isolated from the chloroform fraction in the whole herb of C. lanceolata and were identified as 1β, 5α-diangeloyloxy-eudesm-(15)-ene (1), 1β, 6α-dihydroxyeudesm-4(15)-ene (2), 10α-hydroxyoplopan-4-one (3), (7R*)-opposit-4(15)-ene-1β, 7-diol (4), (7R*)-opposit-4(15)-ene-1β, 8-diol (5), (7R*)-opposit-4(15)-ene-1β, 11-diol (6), (7R*)-opposit-4(15)-ene-1β, 7α-diol (7), 4(15)-eudesmene-1β, 7α-diol (8), p-hydroxy cinamic acid (9), 3-methoxy4-hydroxy-benzoic acid (10), methyl-p-hydroxybenzoate (11), 3, 4-dihydroxy-benzaldehyde (12), β-sitosterol (13), friedeline (14), and friedelinol (15). Conclusion: Compounds 1-15 are obtained from the whole herb of C. lanceolata for the first time. The bioassays show that the compounds 3 and 4 have the stronger inhibition against Staphylococcus aureus.
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Objective: To study the secondary metabolites of Eurotium cristatum from Fu Brick Tea and their biological activities. Methods: The compounds were isolated by various column chromatographies on normal phase silica gel, reversed silica gel, Sephadex LH-20, preparative TLC, and recrystallization. The structures were identified by the extensive analysis on their spectroscopic data. The inhibitory effects of compounds 1-9 against SF-268, MCF-7, and NCI-H460 cell lines were tested in vitro by SRB method. The inhibitory effects of compounds 2-9 on Staphyloccocus aureus, Escherichia coli, Salmonella enterica subsp. enterica, Shigella dysenteriae, and Proteus vulgaris were tested by MTT method. Results: Nine compounds were isolated from the extract of liquid fermentation broth of E. cristatum in Fu Brick Tea and identified as physcion (1), 1, 5-dihydroxy-3-methoxy-7-methyl-anthracene-9,10-dione (2), flavoglaucin (3), 2-(2', 3-epoxy-1', 3'-heptadienyl)-6-hydroxy-5-(3-methyl-2-butenyl) benzaldehyde (4), 2-(2', 3-epoxy-1', 3', 5'-heptatrienyl)-6-hydroxy-5-(3-methyl-2-butenyl) benzaldehyde (5), isodihydroauroglaucin (6), tyrosol (7), p-hydroxybenzoic acid (8), and orcinol (9). The results of the bioactivity test showed that compounds 3-6 displayed the good cytotoxic acitivities against the three tumor cell lines, and all the compounds exhibited the strong inhibitory activities against P. vulgaris except compounds 1 and 6. Besides, compound 9 also showed the significant inhibitory effects against S. aureus and E. coli. Conclusion: The benzaldehyde compounds are considered as the main metabolites of E. cristatum, compounds 7 and 9 are reported from the species of genus Eurotium Link: Fr. for the first time and compounds 2, 3, 5, 6, and 8 are firstly isolated from the fungus.
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Chalcone is an aromatic ketone that forms the central core for the variety of important biological compounds, which are collectively known as chalcones. The name chalcones was given by Kostanecki and Tambor. The chalcones, two aromatic rings are linked by an aliphatic three carbon chain which bears a very good synthon so that variety of novel heterocyclics with good pharmaceutical profile can be designed. Chalcones have been considered as a magic moiety possessing myriad spectrum of medicinal activities. Diversity of biological response profile has attracted considerable interest of several researchers across the globe to explore this skeleton for its assorted therapeutic significance. By using different synthetic methods new chalcone derivatives were synthesized and characterized by physicochemical analysis. Chalcone is a lead nucleus for future developments to get effective compounds.
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The benzaldehyde di-n-butylacetal has been synthesized and its reactions with acid chlorides, viz., acetylchloride, benzoylchloride, benzylchloride, perchloricacid, sodiumperchlorate, zirconiumoxychloride and calciumoxychloride have been studied at -20oC. The acetal generates esters with acetylchloride, benzoylchloride and perchloricacid while produced ether with benzylchloride, but only aldehyde with sodiumperchlorate. Interestingly, acetal yields substituted aldehyde alone with zirconiumoxychloride and calciumoxychloride. Acid chlorides are synthetically very useful reagents and vary widely in their acceptor synthon character and reactivity; hence their application in the present work on the action of acid chlorides on benzaldehyde di-n-butylacetal is a new venture.
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OBJECTIVE: To synthesize a kind of novel cytotoxin with multi-drug-resistance reverting properties and study their cytotoxicity. METHODS: The target compounds were obtained from N-benzyl-4-piperidones and benzaldehyde derivatives on the condition of 20°C, 7-8 h, taking dry hydrogen chloride as catalyst, using aldol condensation reaction, inspected by TLC and purified through recrystallization. RESULTS: Five N-benzyl-3, 5-bis(arylmethylene)-4-piperidone derivatives were synthesized. The yield was over 49%. Their structures were characterized by 1H-NMR, ESI-MS with melting points. The data of cytotoxicity was obtained. CONCLUSION: The synthetic route is convenient and efficient; The compounds had good inhibiting activity for a few kinds of tumor cells. Copyright 2012 by the Chinese Pharmaceutical Association.
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New, simple, accurate, sensitive, economical, and reproducible UV-spectrophotometric method was developed and validated for the estimation of Lacidipine in bulk and tablet dosage form. Lacidipine shows maximum absorbance at 615.7 nm and linearity (Beer’s Lamberts law) was found to be in the range of 10-70 μg/ml. The apparent molar absorptivity and Sandell’s sensitivity coefficient were found to be 2.84 x 103 L mol-1 cm-1 and 0.16043 indicating the high sensitivity of the proposed methods. The slope, intercept and correlation coefficient were also calculated. Interference of common excipients with the proposed method was also studied and found there was no interference of common excipients with the proposed method. The method was validated by determining its sensitivity, accuracy and precision which proves the suitability of the developed method for the routine estimation of Lacidipine in pharmaceutical formulations.
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Objective: To investigate the chemical constituents in the root bark of Torricellia angulata var. intermedia. Methods: The compounds were isolated by means of column chromatography on silica gel, macroporous resin, Sephadex LH-20, and ODS, and their structures were elucidated by physicochemical properties and spectra. Results: Ten compounds were obtained and identified as syringaresinol (1), stigmasterol (2), 3,4,5,7-tetrahydroxy benzeneacetic acid (3), stigmasta-5,11-dien-3β-ol (4), 22,23-dihydrostigmasterol (5), β-daucosterol (6), 26,27-dinor-4,4-dimethyl-cholesta-8,14-dien-3-ol (7), octadecanoic acid (8), palmitic acid (9), and 4-hydroxy-3,5-dimethoxyl benzaldehyde (10). Conclusion: Compound 3 is isolated from natural plant for the first time and compounds 1, 2, 4, 5,7, and 10 are isolated from this plant for the first time.
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Toxoplasma, which infects all eukaryotic cells, is considered to be a good system for the study of drug action and of the behavior of infected host cells. In the present study, we asked if thiosemicarbazone derivatives can be effective against tachyzoites and which morphological and ultrastructural features of host cells and parasites are associated with the destruction of Toxoplasma. The compounds were tested in infected Vero cell culture using concentration screens (0.1 to 20 mM). The final concentration of 1 mM was chosen for biological assay. The following results were obtained: 1) These new derivatives decreased T. gondii infection with an in vitro parasite IC50 percent of 0.2-0.7 mM, without a significant effect on host cells and the more efficient compounds were 2, 3 (thiosemicarbazone derivatives) and 4 (thiazolidinone derivative); 2) The main feature observed during parasite elimination was continuous morphological disorganization of the tachyzoite secretory system, progressive organelle vesiculation, and then complete disruption; 3) Ultrastructural assays also revealed that progressive vesiculation in the cytoplasm of treated parasites did not occur in the host cell; 4) Vesiculation inside the parasite resulted in death, but this feature occurred asynchronously in different intracellular tachyzoites; 5) The death and elimination of T. gondii was associated with features such as apoptosis-like stage, acidification and digestion of parasites into parasitophorous vacuoles. Our results suggest that these new chemical compounds are promising for the elimination of intracellular parasites by mainly affecting tachyzoite development at 1 mM concentration for 24 h of treatment.
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Animals , Antiprotozoal Agents/pharmacology , Thiazoles/pharmacology , Thiosemicarbazones/pharmacology , Toxoplasma/drug effects , Antiprotozoal Agents/chemistry , Chlorocebus aethiops , Host-Parasite Interactions , Microscopy, Electron, Transmission , Parasitic Sensitivity Tests , Thiazoles/chemistry , Thiosemicarbazones/chemistry , Toxoplasma/ultrastructure , Vero Cells/parasitologyABSTRACT
Object To develop and utilize a folk-medicine of Yunnan Province, Lethariella cladonioides (Nyl.) Krog. Methods The constituents were extracted with 80% ethanol and isolated with silica gel column chromatography. The structures were identified by physicochemical properties and spectral analysis. Results Two unknown constituents were elucidated from the extract as 3-aldehyde-6-methyl-2, 4-dihydroxy-ethyl-benzoate (Ⅰ), and 4-methyl-2, 6-dihydroxy-benzaldehyde (Ⅱ). Conclusion They are both new constituents obtained firstly.