Chemical constituents from stems and leaves of Cratoxylum cochinchinense and their inhibitory effects on proliferation of synoviocytes in vitro / 中国中药杂志

The chemical constituents from the stems and leaves of Cratoxylum cochinchinense were isolated and purified using silica gel, ODS gel, and Sephadex LH-20 gel column chromatography, as well as preparative HPLC. The chemical structures of all isolated compounds were identified on the basis of their physicochemical properties, spectroscopic analyses, and the comparison of their physicochemical and spectroscopic data with the reported data in literature. As a result, 21 compounds were isolated from the 90% ethanol extract of the stems and leaves of C. cochinchinense, which were identified as cratocochine(1), 1-hydroxy-3,7-dimethoxyxanthone(2), 1-hydroxy-5,6,7-trimethoxyxanthone(3), ferrxanthone(4), 3,6-dihydroxy-1,5-dimethoxyxanthone(5), 3,6-dihydroxy-1,7-dimethoxyxanthone(6), 1,2,5-trihydroxy-6,8-dimethoxyxanthone(7), securixanthone G(8), gentisein(9), 3,7-dihydroxy-1-methoxyxanthone(10), pancixanthone B(11), garcimangosxanthone A(12), pruniflorone L(13), 9-hydroxy alabaxanthone(14), cochinchinone A(15), luteolin(16), 3,5'-dimethoxy-4',7-epoxy-8,3'-neolignane-5,9,9'-triol(17), N-benzyl-9-oxo-10E,12E-octadecadienamide(18), 15-hydroxy-7,13E-labdadiene(19), stigmasta-4,22-dien-3-one(20), and stigmast-5-en-3β-ol(21). Among these isolates, compound 1 was a new xanthone, compounds 2-5, 7, 8, 12, and 16-21 were isolated from the Cratoxylum plant for the first time, and compounds 11 and 13 were obtained from C. cochinchinense for the first time. Furthermore, all isolated compounds 1-21 were appraised for their anti-rheumatoid arthritis activities by MTS method through measuring their anti-proliferative effect on synoviocytes in vitro. As a result, xanthones 1-15 displayed notable anti-rheumatoid arthritis activities, which showed inhibitory effects on the proliferation of MH7A synoviocytes with the IC_(50) values ranging from(8.98±0.12) to(228.68±0.32) μmol·L~(-1).

Chemical composition and antioxidant studies of underutilized part of mangosteen (Garcinia mangostana L.) fruit

Mangosteen (Garcinia mangostana L) is one of Indonesian fruit with export commodity due to its sweet-sour andpleasant taste. The pulp of this fruit is frequently consumed freshly, while the seed and peel are removed and become awaste. The chemical components contained in mangosteen’s seed and peel, especially xanthones, have been reported asantioxidants either in vitro or in vivo. Several traditional medicine products used the extracts of mangosteen as one ofits components; therefore, the characterization of mangosteen extracts through identification of its active componentsis very important. This review article highlighted the updates on the characterization and antioxidant activities ofmangosteen’s seed and peel to prove that the wastes of mangosteen fruit could be advantageous to be developed asfunctional food as antioxidants. Several databases have been used during performing this review, including PubMed,Scopus, Biological abstracts, chemical abstracts, and Google Scholar.

Chemical composition by HPLC-ESI-QTOF-MS/MS: Estrogenic and antioxidant effects of Mangifera indica L. cv. "Kent" leave extracts on ovariectomized rats / Composición química por HPLC-ESI-QTOF-MS/MS: efectos estrogénicos y antioxidantes de extractos de Mangifera indica L. cv. "Kent" en ratas ovariectomizadas

The chemical composition of Mangifera indica L. cv. "Kent" leaves was determined by HPLC-ESI-QTOF-MS/MS. Polyphenolic compounds characterized as benzophenone derivatives were the main components found in extracts (1, maclurin 3-C-(2-O-galloyl)-D- glucoside isomer; 2, maclurin 3-C---D-glucoside; 3, iriflophenone 3-C---D-glucoside; 5, maclurin 3-C-(2,3-di-O-galloyl)---D-glucoside; 6, iriflophenone 3-C-(2-O-galloyl)---D-glucoside; 7, methyl-iriflophenone 3-C-(2,6-di-O-galloyl)---D-glucoside) and xanthones (4, mangiferin and 8, 6-O-galloyl-mangiferin). The estrogenic and antioxidant effects of aqueous extracts from Mangifera indica L. cv. "Kent" leaves on ovariectomized rats were determined by uterotrophic assay and malondialdehyde (MDA) levels in erythrocytes, bone, liver, and stomach. We conclude that the polyphenolic compounds from extracts act as exogenous antioxidant agents against oxidative damage in ovariectomized rats.

La composición química de las hojas de Mangifera indica L. cv. "Kent" se determinó por HPLC-ESI-QTOF-MS/MS. Compuestos polifenólicos caracterizados como derivados de benzofenona fueron los componentes principales encontrados en los extractos (1, isómero de la maclurina 3-C-(2-O-galoyil)-D-glucósido; 2, maclurina 3-C-ß-D-glucósido; 3, iriflofenona 3-C-ß-D-glucósido; 5, maclurina 3-C-(2,3-di-O-galloíl)-ß-D-glucósido; 6, iriflofenona 3-C-(2-O-galloil)-ß-D-glucósido; 7, metil-iriflofenona 3-C-(2,6-di-O- galloyl)-ß-D-glucósido) y xantonas (4, mangiferina y 8, 6-O-galoyil-mangiferina). Los efectos estrogénicos y antioxidantes de los extractos acuosos de hojas de Mangifera indica L. cv. "Kent" en ratas ovariectomizadas se determinaron mediante ensayo uterotrófico y la medición de los niveles de malondialdehído (MDA) en eritrocitos, huesos, hígado y estómago. Concluimos que los compuestos polifenólicos de los extractos actúan como agentes antioxidantes exógenos contra el daño oxidativo en ratas ovariectomizadas.

Mangostanaxanthone VIIII, a new xanthone from Garcinia mangostana pericarps, α-amylase inhibitory activity, and molecular docking studies

ABSTRACT A new xanthone: mangostanaxanthone VIIII [1,3,5,6,7-pentahydroxy-2-(3-methylbut-2-enyl)-8-(3-hydroxy-3-methylbut-1-enyl) xanthone] (5) and four known xanthones: mangostanaxanthones I (1) and II (2), γ-mangostin (3), and mangostanaxanthone VII (4) were separated and characterized from the acetone fraction of Garcinia mangostana L., Clusiaceae (mangosteen) pericarps. Their structures were established based on various spectroscopic analyses in addition to HRMS and comparison with the literature. The α-amylase inhibitory potential of the isolated metabolites was evaluated. Compounds 1, 2, and 5 had the highest activity with % inhibition 72.5, 86.5, and 81.8, respectively compared to acarbose (97.1%, reference α-amylase inhibitor). The molecular docking study of the tested metabolites was estimated to shade up the rational explanation of the α-amylase inhibitory activity results. Moreover, the pharmacokinetic parameters were assessed using Swiss ADME. It is noteworthy that 1, 2, and 5 had similar binding poses as the X-ray crystal structure of acarbose, whereas the other metabolites possessed different binding mode that decreased their inhibitory capacity. Thus, these data reinforced the health benefit of mangosteen as an alternative medicine to help lowering the postprandial glucose absorption. Therefore, it could have a good potential for the treatment of diabetes.

Chemical constituents from ethyl acetate fraction of Swertia davidii / 中草药

Objective: To study the chemical constituents from Swertia davidii. Methods: The chemical constituents of the ethyl acetate fraction from the whole plants of S. davidii (Gentianaceae) were investigated by various chromatographic methods including silica gel, ODS, semi-preparative HPLC and so on. Their structures were identified on the basis of NMR spectral data analysis and comparisons with the data reported in literatures. Results: Seventeen known compounds were separated and purified from the ethyl acetate fraction of this plant, which were identified as gentiocrucine (1), gentiocrucine A (2), gentiocrucine B (3), junipediol A (4), 1-hydroxy-3,4,7,8-tetramethoxyxanthone (5), 1,7,8-trihydroxy-3-methoxyxanthone (6), 1,8-dihydroxy-3,4,7-trimethoxyxanthone (7), 1,5,8-trihydroxy-3-methoxyxanthone (8), swertianolin (9), deacetylcentapicrin (10), amarogentin (11), amaroswerin (12), swertiamarin (13), gentiopicroside (14), oleanolic acid (15), daucosterol (16), and β-sitosterol (17). Conclusion: Compounds 1-6, 10, 12, 16, and 17 are isolated from S. davidii for the first time.

Nitric oxide inhibitory and anti-Bacillus activity of phenolic compounds and plant extracts from Mesua species

ABSTRACT Species from the genus Mesua, Calophyllaceae, are rich source for phenolic compounds such as coumarin xanthone, and benzophenone derivatives. An investigation on the potential biologically active phenolic compounds 1-5 and crude extracts from the stem bark of Mesua hexapetala (Hook. f.) P.S. Ashton and Mesua beccariana (Baill.) Kosterm. for nitric oxide inhibitory activity on RAW 264.7 macrophage as well as anti-Bacillus activity on selected Bacillus were carried out. Hexapetarin (1), which we reported as a new compound isolated from M. hexapetala showed very good nitric oxide inhibitory activity with an IC50 value of 30.79 ± 2.68 µM. This compound also gave very significant activities towards Bacillus subtilis ATCC 6633, Bacillus cereus ATCC 33019, Bacillus megaterium ATCC 14581 and Bacillus pumilus ATCC 14884 in disc diffusion and minimum inhibitory concentrations assay. Moreover, 1,3,7-trihydroxy-2,4-di (3-methyl-2-butenyl)xanthone (2) isolated from M. hexapetala showed very significant nitric oxide inhibitory activity with an IC50 value of 12.41 ± 0.89 µM and does not exhibit anti-Bacillus activity on four types of Bacillus. Meanwhile, compounds 3-5 were inactive in the nitric oxide activity test and anti-Bacillus assay.

Bioactive xanthones from whole plants of Gentianella acuta / 中草药·英文版

Objective: To study the constituents from the whole plants of Gentianella acuta and their biological activities. Methods: The compounds were isolated by multiple chromatographic methods and the structures of mentioned isolates were determined by routine NMR experiments and chemical methods. Results: A phytochemical investigation to obtain intestine motility inhibitor resulted in the isolation of one new xanthone glycoside, gentixanthonoside A (1), along with nine tetrahydroxanthones, 1,3,5R,8S-tetrahydroxy-5,6,7,8-tetrahydroxanthone (2), 1,3,5S,8S-tetrahydroxy-5,6,7,8-tetrahydroxanthone (3), amarellin E (4), amarellin F (5), swertiachoside B (6), amarellin D (7), amarellin C (8), amarellin A (9), and amarellin B (10) from the whole plants of G. acuta. Conclusion: Compounds 2–10 showed significant reduce effects on contraction tension at 40 µM.

Antioxidant xanthones and anthraquinones isolated from a marine-derived fungus Aspergillus versicolor / 中国天然药物

Chemical examination of an EtOAc extract of cultured Aspergillus versicolor fungus from deep-sea sediments resulted in the isolation of four xanthones, eight anthraquinones and five alkaloids, including a new xanthone, oxisterigmatocystin D (1) and a new alkaloid, aspergillusine A (13). High resolution electron impact mass spectrometry (HR-EI-MS), FT-IR spectroscopy, and NMR techniques were used to elucidate the structures of these compounds, and the absolute configuration of compound 1 was established by its NMR features and coupling constant. Furthermore, the biosynthesis pathway of these xanthones and anthraquinones were deduced, and their antioxidant activity and cytotoxicity in human cancer cell lines (HTC-8, Bel-7420, BGC-823, A549, and A2780) were evaluated. The trolox equivalent antioxidant capacity (TEAC) assay indicated most of the xanthones and anthraquinones possessing moderate antioxidant activities. The Nrf2-dependent luciferase reporter gene assay revealed that compounds 6, 7, 9, and 12 potentially activated the expression of Nrf2-regulated gene. In addition, compounds 5 and 11 showed weak cytotoxicity on A with the IC values of 25.97 and 25.60 μmol·L, respectively.

Chemical constituents from roots of Veratrilla baillonii / 中草药

Objective To study the chemical constituents from the roots of Veratrilla baillonii. Methods Compounds were purified by normal and reversed column chromatographic techniques, and isolated by high performance liquid chromatography. Their structures were identified on the basis of spectral data including MS and NMR. Results Twenty-four compounds (including 10 xanthone glycosides, 8 xanthones, and 6 iridoids) were isolated from the ethyl acetate extracts of the roots of V. baillonii. They were identified as 1-hydroxy-2,3,4-trimethoxyxanthone-7-O-β-D-glucopyranoside (1), tripteroside (2), 1-hydroxy-2,7-dimethoxyxanthone-3-O-β-D- glucopyranoside (3), 1-hydroxy-3,4-dimethoxyxanthone-7-O-β-D-glucopyranoside (4), secamonoide B (5), tetrasweroside A (6), veratriloside B (7), 2,3,4,5-tetramethoxyxanthone-1-O-β-D-glucopyranoxyl-(1→6)-β-D-glucopyranoside (8), 2,3,4,7-tetra- methoxyxanthone-1-O-β-D-xylopyranoxyl-(1→6)-β-D-glucopyranoside (9), 2,3,5-trimethoxy-xanthone-1-O-β-D-xylopyranoxyl- (1→6)-β-D-glucopyranoside (10), 1,3-dihydroxy-4,7-dimethoxyxanthone (11), 1,7-dihydroxy-2,3,4-trimethoxyxanthone (12), 1,7- dihydroxy-3,4-dimethoxyxanthone (13), 1,7-dihydroxy-3-methoxyxanthone (14), 1-hydroxy-2,3,4,5-tetramethoxyxanthone (15), 1-hydroxy-2,3,4,7-tetramethoxyxanthone (16), 1-hydroxy-2,3,5-trimethoxyxanthone (17), 1-hydroxy-2,3,7-trimethoxyxanthone (18), sweroside (19), gentiopicrin (20), swertiamarin (21), deacetylcentapicrin (22), amaronitidin (23), and amarogentin (24). Conclusion Compound 1 is a new compound named 2-methoveratriloside, and compounds 2, 3, 5, 6, 8, 10-12, 14, and 22-24 are isolated from the Veratrilla genus for the first time.

Research advance on chemical constituents and pharmacological effects of Gentianella acuta / 中草药

Gentianella acuta is a commonly used Mongolian medicine and its mainly active constituents are xanthone, terpenoids, and phenylpropanoids. It has the effects of clearing heat and draining dampness, anti-tumor, liver protection, anti-depression, and anti-inflammation. This review summarizes the chemical components and pharmacology of G. acuta from the literatures in recent 30 years in order to provide basis for the development of this plant.

Antioxidant xanthones and anthraquinones isolated from a marine-derived fungus Aspergillus versicolor / 中国天然药物

Chemical examination of an EtOAc extract of cultured Aspergillus versicolor fungus from deep-sea sediments resulted in the isolation of four xanthones, eight anthraquinones and five alkaloids, including a new xanthone, oxisterigmatocystin D (1) and a new alkaloid, aspergillusine A (13). High resolution electron impact mass spectrometry (HR-EI-MS), FT-IR spectroscopy, and NMR techniques were used to elucidate the structures of these compounds, and the absolute configuration of compound 1 was established by its NMR features and coupling constant. Furthermore, the biosynthesis pathway of these xanthones and anthraquinones were deduced, and their antioxidant activity and cytotoxicity in human cancer cell lines (HTC-8, Bel-7420, BGC-823, A549, and A2780) were evaluated. The trolox equivalent antioxidant capacity (TEAC) assay indicated most of the xanthones and anthraquinones possessing moderate antioxidant activities. The Nrf2-dependent luciferase reporter gene assay revealed that compounds 6, 7, 9, and 12 potentially activated the expression of Nrf2-regulated gene. In addition, compounds 5 and 11 showed weak cytotoxicity on A with the IC values of 25.97 and 25.60 μmol·L, respectively.

Metabolic profile and β-glucuronidase inhibitory property of three species of Swertia

ABSTRACT β-Glucuronidase inhibitors are suggested as potential hepatoprotective agents. Swertia chirayita (Roxb.) Buch.-Ham. ex C.B. Clarke, Gentianaceae, is known for its hepatoprotective and anti-hepatotoxic activity in Ayurvedic system of medicine for ages. This plant is substituted by other species like S. decussata Nimmo ex C.B. Clarke and S. bimaculata (Siebold & Zucc.) Hook. f. & Thomson ex C.B. Clarke. The aim of the study was to compare metabolite profile and β-glucuronidase inhibitory activity of these three important species of Swertia and to identify the active constituents. S. chirayita (IC50 210.97 µg/ml) and S. decussata (IC50 269.7 µg/ml) showed β-glucuronidase inhibitory activity significantly higher than that of silymarin, the known inhibitor of the enzyme. The activity of S. bimaculata was low. The metabolites present in the three species were analyzed by HPLC and GC-MS based metabolomics approach. Five amino acids, twenty one organic acids, one inorganic acid, eight fatty acids, twenty one phenols including xanthones, eight sugars, seven sugar alcohols, five terpenoids and amarogentin were identified. Activities of the xanthones mangiferin (IC50 16.06 µg/ml), swerchirin (IC50 162.84 µg/ml), decussatin (IC50 195.11 µg/ml), 1-hydroxy-3,5,8-trimethoxy xanthone (IC50 245.97 µg/ml), bellidifolin (IC50 390.26 µg/ml) were significantly higher than that of silymarin (IC50 794.62 µg/ml). Quinic acid (IC50 2.91 mg/ml), O-acetylsalicylic acid (IC50 48.4 mg/ml), citric acid (IC50 1.77 mg/ml), D-malic acid (IC50 14.82 mg/ml) and succinic acid (IC50 38.86 mg/ml) also inhibited the enzyme β-glucuronidase. The findings suggest that constituents, in addition to the xanthones, probably also contribute to the bioactivity of different Swertia species by synergistic effect. Further in vivo study is required to support the claim.

Chemical constituents from Tibetan medicine Swertia chirayita / 中草药

Objective: To investigate the chemical constituents of Swertia chirayita. Methods: Column chromatography, such as silica gel, MCI, Sephadex LH-20 were used to isolate and purify the compounds. Physicochemical properties and spectroscopic methods were used to elucidate their structures. Results: Twelve compounds, including 2 xanthones, 4 triterpenoids, 3 secoiridoids, and 3 other compounds, the chemical constituents were isolated from the ethyl acetate fraction from 85% ethanol extract of S. chirayita, and identified as bellidifolin (1), norbellidifolin (2), oleanolic acid (3), 4-epi-hederagenin (4), 2-epi-corosolic acid (5), ursolic acid (6), amarogentin (7), swerimilegenin I (8), erythrocentaurin (9), pyrocatechol (10), syringic acid (11), and 4-hydroxy-3-methoxybenzoic acid (12). Conclusion: Compounds 4, 5, and 11 are isolated from genus Swertia for the first time, compounds 8 and 9 are found from S. chirayita for the first time.

Isolation and identification of xanthones from Gentianella acuta / 中国中药杂志

Twelve xanthones compounds were isolated from the ethanol extract of Gentianella acuta by means of reversed-phase preparative HPLC and various kinds of column chromatography including silica gel and ODS . Their structures were fully elucidated on the basis of MS, 1D and 2D-NMR data. The structures of xanthones were identified as 1, 7-dihydroxy-3-methoxyxanthone-7-O-β-D-glucopyranoside (1), swertiapuniside (2), 1, 3, 8- trihydroxy -4, 5-dimethoxyxanthone-1-O-β-D-glucopyranosyl(6→1)-O-β-D-glucopyranoside (3), 1, 2, 8-trihydroxy-5, 6-dimethoxyxanthone-2-O-β-D-glucopyranoside (4), 1, 3, 7, 8-tetrahydroxyxanthone-1-O-β-D-glucopyranoside (5), 1, 3, 5, 8-tetrahydroxy-5, 6, 7, 8-tetrahydroxanthone (6), 1, 3, 5-thihydroxyxanthone (7),1, 3, 5, 8-tetrahydroxyxanthone (8), 1, 2, 8-trihydroxy-5, 6-dimethoxyxanthone (9), bellidifolin (10), mangiferin (11), swertianolin (12). Compounds 1-9 were isolated from Gentianella genus for the first time.

Study on Chemical Components of Swertia nervosa / 中国药房

OBJECTIVE:To study the chemical components of Swertia nervosa. METHODS:Silica gel column chromatogra-phy was used for purification and analysis of compounds’structure based on physicochemical properties and spectral data. RE-SULTS:Five compounds were isolated and identified in petroleum ether portion of S. nervosa,involving 1-hydroxy-3,7,8-trime-thoxyxanthone (1),1,8-dihydroxy-3,7-dimethoxyxanthone (2),1,8-dihydroxy-3,5-dimethoxyxanthone(3),1-hydroxy-3,5-dime-thoxyxanthone(4)and β-sitosterol(5). CONCLUSIONS:Compound 1,3 and 4 are isolated from S. nervosa for the first time,and the study has laid a foundation for the quality evaluation of S. nervosa.

Chemical constituents of Swertia bimaculataa / 中草药

Objective: To investigate the chemical constituents from the dried whole plants of Swertia bimaculata. Methods: The compounds were isolated and purified by various column chromatography, and their structures were elucidated on the basis of chemical and spectroscopic analyses. Results: Thirty compounds were isolated from the n-BuOH fraction of S. bimaculata EtOH extract and identified as 1,3,6-trihydroxy-4,7-dimethoxyxanthone (1), 1,8-dihydroxy-2,3,4,5-tetramethoxyxanthone (2), 1,3,5-trihydroxy-4- methoxyxanthone (3), 1,3-dihydroxy-5-methoxyxanthone (4), 1,3,5-trihydroxyxanthone (5), 1,3,7-trihydroxy-4-methoxyxanthone (6), 2-(3'-O-β-D-glucopyranosyl) benzoyloxygentisic acid (7), veratrilogenin (8), demethylbellidifolin (9), isobellidifolin (10), 1,3,8-trihydroxy-4,5-dimethoxyxanthone (11), 1,3-dihydroxy-4,5-dimethoxyxanthone (12), methylbellidifolin (13), 1-hydroxy-2,3,4,7-tetramethoxyxanthone (14), mangiferin (15), astragalin (16), isoquercitrin (17), nicotiflorin (18), rutin (19), isoorientin-7,3'-dimethylether (20), swertisin (21), swertiajaponin (22), isoorientin (23), isoscutellarein-8-methyl ether (24), 8-chrysoeriol (25), kaempferol (26), luteolin (27), quercetin (28), β-sitosterol (29), and oleanolic acid (30). Conclusion: Compound 1 is a new compound. named bimaculatone A. Compounds 2-7, 16-20, and 24-26 are firstly obtained from the plants of Swertia L., and compounds 2-11 and 16-28 are obtained from S. bimaculata for the first time.

Research progress on Polygalae Radix / 中草药

Polygalae Radix used as Chinese materia medica has a long history. The main chemical constituents include triterpenoid saponins, xanthones, oligosaccharide esters, and so on. The study shows that Polygalae Radix has a wide range of pharmacological activities, such as sedative hypnotic, anticonvulsant, antiaging, antidementia, brain protection, cough expectorant, antidepressant, antibacterial, and anticancer. In this paper, through referring to the domestic and foreign relevant literatures on Polygalae Radix systematically, we summarize the chemical composition, pharmacological activity, and structure activity relationship of Polygalae Radix, which could provide the reference for the further investigation and development of this plant.

Identification and characterization of two new xanthones from Cudrania fruticosa / 中国天然药物

The present study was designed to investigate the chemical constituents of the roots of Cudrania fruticosa Wight. Compounds were isolated by various column chromatographic methods including silica gel, polyamide, sephadex LH-20, and semi-preparative HPLC. Their structures were elucidated by a combination of 1D and 2D NMR techniques, mass spectrometry, and chemical methods. Two new xanthones, Cudraxanthone T and U (1-2), along with four known compounds (3-6) were isolated from the roots of Cudrania fruticosa Wight.

Efeitos da fração acetato de etila de Tabernaemontana catharinensis sobre respostas glicêmicas e estresse oxidativo de Rattus norvegicus diabéticos / Effects of tabernaemontana catharinensis ethyl acetate fraction on glycemic responses and oxidative stress

OBJECTIVE: To evaluate the Tabernaemontana catharinensis ethyl acetate fraction hypoglycemic and antioxidant activity through the peripheral glycemic dosage and enzymatic tests. Methods: Male rats were divided into 6 groups: control, diabetic control, control extract 50, diabetic extract 50, control extract 80, diabetic extract 80. In diabetic group animals alloxan (150mg/Kg) was administered to induce Diabetes Mellitus. The animals were beheaded following 15 days of treatment with extract or distilled water and the blood was collected in order to perform oxidative stress tests. Results: The diabetic control group showed high levels of glucose, increased levels of thiobarbituric acid and superoxide dismutase activity, and decreased activity of catalase and glutathione peroxidase enzymes. The diabetic animals that received 50mg/Kg and 80mg/Kg of extract showed a decrease in thiobarbituric acid levels and an increase of glutathione peroxidase activity when compared to the diabetic control group. It was observed that only animals treated with 80mg/Kg of extract had positive results regarding superoxide dismutase. Conclusions: The Tabernaemontana catharinensis ethyl acetate fraction when orally administered for 14 consecutive days at doses of 50mg/Kg and 80mg/Kg reduces the oxidative stress induced by alloxan administration

OBJETIVO: Avaliar a ação hipoglicemiante e antioxidante da fração acetato de etila do extrato de Tabernaemontana catharinensis através da dosagem glicêmica periférica e testes enzimáticos. MÉTODOS: Ratos machos foram divididos em seis grupos: controle, controle diabético, controle extrato 50, diabético extrato 50, controle extrato 80, diabético extrato 80. Nos animais dos grupos diabéticos foi induzida Diabetes Mellitus pela administração de 150mg/Kg de aloxana. Após 15 dias de tratamento com a fração acetato de etila de Tabernaemontana catharinensis ou água destilada, os animais foram decapitados e o sangue foi coletado para realização dos testes de estresse oxidativo. RESULTADOS: O grupo controle diabético apresentou níveis elevados de glicose, aumento dos níveis de ácido tiobarbitúrico e atividade da superóxido dismutase, e diminuição da atividade das enzimas catalase e glutationa peroxidase. Os animais dos grupos diabéticos tratados com 50 e 80mg/Kg do extrato apresentaram redução nos níveis de ácido tiobarbitúrico e aumento da atividade de glutationa peroxidase quando comparado ao grupo controle diabético. Apenas os animais que receberam o extrato na dose de 80mg/Kg obtiveram resultados positivos em relação ao superóxido dismutase. CONCLUSÕES: A fração acetato de etila de Tabernaemontana catharinensis, quando administrada por 14 dias consecutivos, via oral, nas doses de 50 e 80mg/Kg, promove redução nos níveis de estresse oxidativo gerado pela administração de aloxana

Chemical constituents from leaves of Swertia atroviolacea / 中草药

Objective: To study the chemical constituents from the leaves of Swertia atroviolacea and five compounds were obtained. In addition, the cytotoxic activity of compound 1 was tested. Methods: Compounds 1-5 were isolated and purified by silica gel column chromatography, Zorbax PrepHT GF (250 mm×21.2 mm) reversed phase and Sephadex LH-20 gel column chromatography, and other modern separation technology. Their structures were elucidated by physicochemical properties and spectroscopic methods. Compound 1 was evaluated for its in vitro cytotoxicity against human tumor NB4, A549, SHSY5Y, PC3, and MCF-7 cell line, using the MTT method. Results: Five compounds were obtained from the 95% ethanol extract from the leaves of S. atroviolacea, and identified as 3-(3-methyl-2-oxobut-3-enyl)-6-acetyl-1, 5-dimethoxy-xanthone (1), 1, 2, 3, 4-tetrahydro-1, 4, 6, 8-tetrahydroxyxanthone (2), 1, 3-dimethoxy-8-hydroxy-xanthone (3), 1, 2, 6, 8-tetrahydroxy-xanthone (4), and ursolic acid (5). The IC50 values of compound 1 on NB4, A549, SHSY5Y, PC3, and MCF-7 were all below 10 μmol/L. Compound 1 had higher cytotoxic activity on A549 and MCF-7, and the IC50 values were 5.2 and 3.8 μmol/L. Conclusion: Compound 1, named atroviolacone A, is a new compound, and exhibits significant cytotoxic activity.