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Objective: To characterize the antifungal activity of methanolic leaf extract of Calotropis gigantea alone or in combination with amphotericin B against invasive pulmonary aspergillosis in mice. Methods: GC/MS was used for analysis of active constituents of Calotropis gigantea extract. Spore germination assay and broth micro-dilution method were used to determine antifungal potential of Calotropis gigantea/amphotericin B against Aspergillus fumigatus. Neutropenic mice were randomly assigned into 5 groups: group 1 was neutropenic (control); group 2 was infected with Aspergillus fumigatus; group 3 was infected with Aspergillus fumigatus, and treated with Calotropis gigantea extract; group 4 was infected with Aspergillus fumigatus and treated with amphotericin B; group 5 was infected with Aspergillus fumigatus and treated with both Calotropis gigantea extract and amphotericin B. Fresh lung tissues were histopathologically examined. Fungal burden and gliotoxin concentration were evaluated in lung tissues. Catalase, superoxide dismutase, and malondialdehyde content were determined in lung tissues. Myeloperoxidase, tumor necrosis factor-alpha, interleukin-1, and interleukin-17 were also estimated by the sandwich enzyme-linked immuno-sorbent assay. Results: Calotropis gigantea/amphotericin B had a minimum inhibitory concentration and minimum fungicidal concentration of 80 and 160 μg/mL, respectively, for Aspergillus fumigatus. Additionally, Calotropis gigantea/amphotericin B significantly reduced lung fungal burden by 72.95% and inhibited production of gliotoxin in lung tissues from 6 320 to 1 350 μg/g lung. Calotropis gigantea/amphotericin B reduced the oxidative stress of the lung via elevating the activity of antioxidant enzymes and decreasing the levels of lipid peroxidation. Myeloperoxidase activity and the production of pro-inflammatory cytokines were also significantly reduced. Scanning electron microscopy revealed deteriorations in the hyphae ultrastructure in Calotropis gigantea/amphotericin B treated Aspergillus fumigatus and leak of cellular components after damage of the cell wall. In vivo study revealed the suppression of lung tissue damage in mice of invasive pulmonary aspergillosis, which was improved with Calotropis gigantea/amphotericin B compared to the control group. Conclusions: Calotropis gigantea/amphotericin B is a promising treatment to reduce lung fungal burden and to improve the drugs' therapeutic effect against invasive pulmonary aspergillosis.
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OBJECTIVE: To study the anti-cancer components of Calotropis gigantean L. METHODS: The powdered whole plants of C. gigantea were extracted with 95% alcohol. After removal of the solvent, the residue was extracted with petroleum ether and chloroform, and the compounds in the chloroform extract were isolated and purified by different column chromatograghies carried out on silica gel, RP-18, MCI, and Sephadex LH - 20 and their structures were elucidated by spectral data. RESULTS: Thirteen compounds were isolated and their structures were characterized as gofruside(1), uzarigenin(2), arjunolic acid(3), 3ξ-(1ξ-hydroxyethyl) -7-hydroxy-1-isobenzofuranone(4), daucosterol(5), syringaresinol(6), 12-O-benzoyl-deacylmetaplexigenin(7), 3-hydroxy-4-methoxybenzoic acid(8), oleanolic acid(9), β-sitosterol(10), methyl 1-naphthaleneacetate(11), butylparaben(12), α-D-oleandropyranoside(13), and compounds 2 - 4, 6- 9, and 11 - 13 were isolated from this plant for the first time. Compounds 1 and 2 showed cytotoxicity against HLE, K562, RPMI8226, MCF7, MDA, and WM9 cell lines, with K562 and RPMI8226 being the most sensitive cells. CONCLUSION: Compounds 1 and 2 are premilinarily judged as the anti-cancer components in C. gigantean.
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The present study aimed to develop pharmacognostical and phytochemical descriptors (HPTLC) of Calotropis procera and Calotropis gigantea. β-sitosterol which is one of the common terpene content and a potent antioxidant, purgative, antispasmodic and expectorant, has also been studied through a simple and high-precision method using high performance thin layer chromatography (HPTLC). This may be utilized by pharmaceutical industries for quality evaluation, ensuring successful commercial exploitation of this drug. From the present study it has been observed that both Calotropis procera and C. gigantea have similar microscopic characteristics, physico-chemical parameters showed a little variation as total ash components and extractive values are little less in C. gigantea. HPTLC studies also showed similar qualitative profile with some quantitative variations in total β-sitosterol, which was higher in C. gigantea (2.79%).
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Objective: To evaluate possible anxiogenic activity, sedative property and anxiolytic potential of crude ethanolic extract of Calotropis gigantea leaves.Methods:evaluated using standard animal behavioral models, such as hole cross and open field; sedative property and anxiolytic potential were evaluated by conducting thiopental sodium induced sleeping time tests and elevated plus-maze test. The anxiogenic activity of crude ethanolic extract of Calotropis gigantea leaves was Results: The crude ethanolic extract exhibited a significant (P<0.05, P<0.001) decrease of motor activity and exploratory behavior in hole cross and open field tests. The extract also markedly increased both the number of visits to and time spent in the corners of the open field. The extract treated rats spent more time in the open arm of elevated plus-maze, showing its antianxiety activity. There was a decrease in the locomotor activity.Conclusions:The obtained results provide support for the use of this species in traditional medicine and warrant further investigation to isolate the specific components that are responsible for the sedative and anxiolytic effects. Components from this plant may have a great potential value as medicinal agents, as leads or model compounds for synthetic or semi synthetic structure modifications and optimization, and as neuropharmacological probes.
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A phytochemical study on the flowe r of Calotropis gigantea (Linn.) using silica gel column chromatography and preparative thin layer chromatography, led to the first time isolation of Di-(2-ethylhexyl) phthalate (compound 1) and anhydrosophoradiol-3-acetate (compound 2). The structures of these compounds were confirmed by spectroscopic analyses (IR, HRTOFMS and NMR). The antibacterial and antifungal activities of ethyl acetate extract, compound 1 and compound 2 were measured using the disc diffusion method. Ethyl acetate extract and compound 1 presented better results than compound 2. The minimum inhibitory concentrations (MICs) of the extract and compounds were found to be in the range of 16~128 microg/ml. The cytotoxicity (LC50) against brine shrimp nauplii (Artemia salina) were also evaluated and found to be 14.61 microg/ml for ethyl acetate, 9.19 microg/ml for compound 1 and 15.55 microg/ml for compound 2.