ABSTRACT
Three new secoiridoid glycosides, named lonijapoglycol A (1), aldosecolohanin C (2) and aldosecolohanin B (3), together with three known ones (4-6), have been isolated from the flower the buds of Lonicera japonica. All the structures were identified by spectroscopic analyses. Lonijapoglycol A (1) expressed significant anti-inflammatory activity to inhibit the release of β-glu-curonidase induced by platelet-activating factor in rat polymorphonuclear leukocytes with an IC value of 3.76 μmol·L.
ABSTRACT
Emblic medicine is a popular natural source in the world due to its outstanding healthcare and therapeutic functions. Our preliminary results indicated that the quality of emblic medicines might have an apparent regional variation. A rapid and effective geographical traceability system has not been designed yet. To trace the geographical origins so that their quality can be controlled, an integrated spectroscopic strategy including spectral pretreatment, outlier diagnosis, feature selection, data fusion, and machine learning algorithm was proposed. A featured data matrix (245 × 220) was successfully generated, and a carefully adjusted RF machine learning algorithm was utilized to develop the geographical traceability model. The results demonstrate that the proposed strategy is effective and can be generalized. Sensitivity (SEN), specificity (SPE) and accuracy (ACC) of 97.65％, 99.85％ and 97.63％ for the calibrated set, as well as 100.00％ predictive efficiency, were obtained using this spectroscopic analysis strategy. Our study has created an integrated analysis process for multiple spectral data, which can achieve a rapid, nondestructive and green quality detection for emblic medicines originating from seventeen geographical origins.
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Abstract Achillinoside was isolated from methanol extract of Achillea alpina L., Asteraceae. The structure of the compound was characterized based on various spectrum data, including IR, HR-ESI-MS, 1D and 2D NMR. The cardiovascular protective effect of achillinoside was tested on H2O2-induced H9c2 cells. In our research, achillinoside could increase the cell viability dose-dependently in H2O2-induced H9c2 cells. In addition, the levels of caspase-3/9 cells were significantly decreased in H2O2 and achillinoside incubated H9c2 cells.
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A new polyketide:3R, 5R-(-)-talaroflavone (2), along with 15 known compounds were isolated from a EtOAc extract of a sponge-derived fungus Alternaria sp. F49. Compounds 1-2 and 3-4 were separated as two pairs of enantiomers by chiral HPLC from Ⅰ and Ⅱ. The structures of compounds 1-16 were elucidated by means of NMR and MS. Furthermore, the absolute configurations of compounds 1-2 were determined by single crystal X-ray diffraction experiment and CD analyses. Compounds 6, 8-10 were isolated from this genus (Alternaria sp.) for the first time. Compound 16 showed moderate COX-2 enzyme inhibitory activity with IC50of 7.3 μmol·L-1.
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Magnesium gluconate is a classical organometallic pharmaceutical compound used for the prevention and treatment of hypomagnesemia as a source of magnesium ion. The present research described the in-depth study on solid state properties viz. physicochemical and thermal properties of magnesium gluconate using sophisticated analytical techniques like Powder X-ray diffraction (PXRD), particle size analysis ( PSA), Fourier transform infrared (FT-IR) spectrometry, ultraviolet–visible (UV–Vis) spectroscopy, thermogravimetric analysis (TGA)/differential thermogravimetric analysis (DTG), and differential scanning calorimetry (DSC). Magnesium gluconate was found to be crystalline in nature along with the crystallite size ranging from 14.10 to 47.35 nm. The particle size distribution was at d(0.1)=6.552 μm, d(0.5)=38.299 μm, d(0.9)=173.712 μm and D(4,3)=67.122 μm along with the specific surface area of 0.372 m2/g. The wavelength for the maximum absorbance was at 198.0 nm. Magnesium gluconate exhibited 88.51% weight loss with three stages of thermal degradation process up to 895.18 ℃ from room temperature. The TGA/DTG thermograms of the analyte indicated that magnesium gluconate was thermally stable up to around 165 ℃. Consequently, the melting temperature of magnesium gluconate was found to be 169.90 ℃ along with the enthalpy of fusion of 308.7 J/g. Thus, the authors conclude that the achieved results from this study are very useful in pharmaceutical and nutraceutical industries for the identification, characterization and qualitative analysis of magnesium gluconate for preformulation studies and also for developing magnesium gluconate based novel formulation.
ABSTRACT
Magnesium gluconate is a classical organometallic pharmaceutical compound used for the prevention and treatment of hypomagnesemia as a source of magnesium ion. The present research described the in-depth study on solid state properties viz. physicochemical and thermal properties of magnesium gluconate using sophisticated analytical techniques like Powder X-ray diffraction (PXRD), particle size analysis ( PSA), Fourier transform infrared (FT-IR) spectrometry, ultraviolet–visible (UV–Vis) spectroscopy, thermogravimetric analysis (TGA)/differential thermogravimetric analysis (DTG), and differential scanning calorimetry (DSC). Magnesium gluconate was found to be crystalline in nature along with the crystallite size ranging from 14.10 to 47.35 nm. The particle size distribution was at d(0.1)=6.552 μm, d(0.5)=38.299 μm, d(0.9)=173.712 μm and D(4,3)=67.122 μm along with the specific surface area of 0.372 m2/g. The wavelength for the maximum absorbance was at 198.0 nm. Magnesium gluconate exhibited 88.51% weight loss with three stages of thermal degradation process up to 895.18 ℃ from room temperature. The TGA/DTG thermograms of the analyte indicated that magnesium gluconate was thermally stable up to around 165 ℃. Consequently, the melting temperature of magnesium gluconate was found to be 169.90 ℃ along with the enthalpy of fusion of 308.7 J/g. Thus, the authors conclude that the achieved results from this study are very useful in pharmaceutical and nutraceutical industries for the identification, characterization and qualitative analysis of magnesium gluconate for preformulation studies and also for developing magnesium gluconate based novel formulation.
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Objective: To confirm the structure and preferential conformation of the Schiff base of gossypol with 1, 3, 4, 6-tetra-O-acetyl-β-D-glucosamine and explore its anti-HIV-1 activity.Methods: The Schiff base of gossypol with 11, 3, 4, 6-tetra-O-acetyl-β-D-glucosamine was synthesized and identified by FT-IR, NMR spectroscopy and the PM6 semi-classical calculation.The inhibitory activity of the novel compound against the laboratory-adapted HIV-1IIIB strain was examined using the HIV-1IIIB/TZM-bl indicator cell culture system.Results: The 1H and 13C-NMR signals of the new Schiff base were assigned.The PM6 semi-classical calculation indicated that enamine-enamine tautomeric form of the new Schiff base was more stable,which was stabilized by the intramolecular hydrogen bonds.The anti-HIV-1 test showed that the compound could block the entry of HIV-1IIIB into the target cells.Conclusion: The Schiff base of gossypol with 1, 3, 4, 6-tetra-O-acetyl-β-D-glucosamine exhibits enamine-enamine tautomeric form in solution, which shows potential anti-HIV-1 activity.
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Objective: To optimize the preparation of Saussureae Involucratae Herba extract (SIHE)-composite phospholipid liposome (CPL) by the central composite design-response surface methodology (CCD-RSM) and to investigate the in vitro release of drugs. Methods: The method of ammonium sulfate transmembrane gradients was adopted to prepare SIHE-CPL. The single factor experiments were used for the key experimental factors and their test ranges. Based on the single factor experiments, with the size of SIHE-CPL, polymey disperse index (PDI), encapsulation efficiency (EE), and Zeta potential as dependent variables, central composite design was adopted to optimize the preparation technology by taking the content of phospholipid and the content of cholesterol as independent variables, test results were fitted by multiple linear and binomial nonlinear equations, and optimum formulation was selected by RSM, then the in vitro release behavior of the drug was studied by method of dynamic dialysis. Infrared (IR) spectroscopy and X-ray diffraction (XRD) pattern were used to analyze the spectroscopic properties of SIHE-CPL. Results: The second-order polynomial equation was superior to the linear one, the observed values agreed well with model predicted values. The optimal process conditions were as follows: Size of SIHE-CPL was (102.7 ± 5.1) nm, PDI was 0.154 ± 0.017, EE of chologenic acid and rutin was (87.68 ± 2.57)% and (84.18 ± 2.97)%, Zeta potential was (-28.4 ± 2.2) mV, SIHE-CPL and solution of SIHE were both accorded with the first order model, and IR analysis and XRD proved the formation of SIHE-CPL. Conclusion: The size and PDI of SIHE-CPL are low, the EE and Zeta potential of SIHE-CPL are high. CCD-RSM could be successfully used to optimize the prescription of SIHE-CPL.
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Objective: To isolate and characterize the bioactive secondary metabolites from aerial parts of widespread Chenopodiaceae taxa growing in Saudi Arabia: Salsola villosa Delile. ex Schul. Methods: Antibacterial activities of chloroformic extract, fractions and isolate compounds was evaluated against five bacterial strains (Escherichia coli, Pseudomonas aeruginosa, Salmonella typhimurium, Staphylococcus aureus and Staphylococcus epidermidis), using a paper disc diffusion method. The purification of compound(s) of chloroform extract was done by chromatographic column of silica gel. The structure elucidation was determined by extensive spectroscopic analysis (1H and 13C nuclear magnetic resonance, correlation spectroscopy, heteronuclear multiple bond correlation, heteronuclear multiple quantum coherence and nuclear overhauser enhancement spectroscopy) and high resolution electrospray ionization mass spectroscopy analysis. Results: Bioactivity guided fractionation of the chloroformic extract led to the isolation of two bioactive compounds: 4-(4'-hydroxy-2'-methylcyclopent-2'-enyloxy)- 4-methylcyclopent-2-enol (1) named salsolanol and 4'-[3-(hydroxymethyl)oxiran-2-yl]-3- [(E)-3-hydroxyprop-1-en-1-yl]-6, 2'-dimethoxy [1, 1'-biphenyl]-2-ol (2) named biphenylsalsinol. The antibacterial effects of the chloroform extracts, fractions and isolated compounds 1 and 2 were also evaluated in this work. Results showed that the compounds 1 and 2 exhibited antibacterial activities against four strains: Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli and Pseudomonas aeruginosa with diameter of zone of inhibition ranging between (9.33 ± 0.94) to (26.33 ± 0.94) mm. Conclusions: Based on data presented here, two new natural compounds secondary cyclic alcohol 1 and biphenylpropanoid 2 isolated from bioactive chloroformic extract from aerial parts of Salsola villosa can be responsible for its antibacterial activities.
ABSTRACT
Objective: To optimize the preparation of Saussureae Involucratae Herba extract (SIHE) phospholipid complex (PC) by the central composite design-response surface method, and to increase the bioavailability of SIHE. Methods: Five main factors including reaction solvent, reaction time, SIHE concentration, reaction temperature, and ratio of reactants on this reaction were investigated. On the basis of single factor test, central composite design was further adopted to arrange experiments in search of a curve fitting model between factors and effects. The optimal formulation was predicted by response surface method and was verified as well. The structure of SIHE-PC was analyzed by infrared spectroscopic (IR) analysis and X-ray diffraction (XRD). Results: The correlation coefficient of second-order quadratic model was high. The optimal process conditions were as follows: The ratio of SIHE and soybean lecithin was 1∶2.5, reaction concentration was 10 mg/mL, reaction time was 2 h, chologenic acid complex molar ratio was 96%, and rutin complex molar ratio was 93%. IR analysis and XRD proved the formation of SIHE-PC. Conclusion: Central composite design-response surface method is successfully used for the optimization on preparation of SIHE-PC, with good predictability and stability.