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Zinc oxide nanoparticles (ZnO-NPs) have provided promising potential in the biomedical field, including the ability to overcome various health problems. Diosgenin is used to treat multiple health disorders but has very low solubility in water. Using ZnO-NPs as a diosgenin delivery vehicle was expected to increase the solubility of diosgenin, which would affect its bioavailability. This study demonstrates phytofabrication and characterization of ZnO-NPs, loading of diosgenin onto the ZnO-NPs, characterization of the product (ZnO-NPs/diosgenin), and evaluations of diosgenin release. Phytofabrication of the ZnO-NPs was carried out with zinc precursors and Hibiscus tiliaceus leaf extract (HLE) obtained with various extraction solvents. To explore the potential of using the ZnO-NPs as a diosgenin delivery vehicle, diosgenin release from the ZnO-NPs/diosgenin was studied. Based on the X-ray fluorescence (XRF) and X-ray diffraction (XRD) results, ZnO-NPs with high purity have been successfully fabricated. Nano-sized particles were detected using scanning electron microscopy (SEM) and confirmed by transmission electron microscopy (TEM), revealing the smallest particle size of 45.924 ± 27.910 nm obtained from the methanol extract with the zinc acetate precursor. The ZnO-NPs had hexagonal wurtzite and rod-like structures. Diosgenin was successfully added to the ZnO-NPs with loadings of 79.972% for ZnO-HLMEA-D500 (ZnO-NPs/diosgenin produced by doping with a 500 µg mL-1 of diosgenin solution) and 39.775% for ZnO-HLMEA-D1000 (ZnO-NPs/diosgenin produced by doping with a 1000 µg mL-1 of diosgenin solution). The solubilities of diosgenin from ZnO-HLMEA-D500 and ZnO-HLMEA-D1000 were higher than that of free diosgenin, confirming that ZnO-NPs have potential as delivery vehicles for diosgenin and conceivably other water-insoluble drugs.
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Gaharu bouya oil obtained from distillation of the woods from Gonystylus genus has attracted essential oil industry interest. However, the information about gaharu bouya essential oil profile is limited. The presence of Gonystylus species is also critically endangered on the IUCN Red List. Therefore, exploring the -omics profiles of Gonystylus bancanus, a native plant from Borneo Island, is important for Indonesia to conserve the population. This research investigated the metabolite profiling of G. bancanus oil, especially the volatile components of its essential oils. Distillations were performed in two technical ways: hydrodistillation on a laboratory scale and steam distillation on an industrial scale. According to LC-MS and GC-MS profiles, both essential oils displayed similar chemical compositions. This article also discusses the similarity of the chemical contents of gaharu bouya oil and agarwood oil from the gaharu superior type (Aquilaria) to support the value of the oil. This research also investigated the cytotoxicity of gaharu bouya oil against three cell lines: HeLa, MCF-7, and HT-29.
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Óleos Voláteis , Madeira , Humanos , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Bornéu , Madeira/química , Thymelaeaceae/química , Cromatografia Gasosa-Espectrometria de Massas , Óleos de Plantas/química , Óleos de Plantas/farmacologia , Células HeLa , Linhagem Celular Tumoral , Indonésia , Antineoplásicos Fitogênicos/farmacologia , Antineoplásicos Fitogênicos/química , Sobrevivência Celular/efeitos dos fármacosRESUMO
Gonystylus bancanus wood or ramin wood has been generally known as a source of agarwood (gaharu) bouya, a kind of agarwood inferior type, or under the exported trading name of aetoxylon oil. The massive exploitation of ramin wood is causing this plant's extinction and putting it on Appendix II CITES and IUCN Red List of Threatened Species. To date, no scientific publication concerns the chemical exploration of G. bancanus wood and preserving this germplasm through its metabolite profiling. Therefore, research focused on chemical components profiling of G. bancanus is promised. This research is aimed to explore metabolomics and analyze the influence of solvent polarities on the partitioning of metabolites in G. bancanus wood. A range of solvents in different polarities was applied to provide comprehensive extraction of metabolites in G. bancanus wood. Moreover, a hydrodistillation was also carried out to extract the volatile compounds despite the non-volatile ones. LCMS and GCMS analyses were performed to identify volatile and non-volatile components in the extracts and essential oil. Multivariate data analysis was processed using Principal Component Analysis (PCA) and agglomerative hierarchical clustering. 142 metabolites were identified by LCMS analysis, while 89 metabolites were identified by GCMS analysis. Terpenoids, flavonoids, phenyl propanoids, and saccharides are some major compound classes available from LCMS data. Oxygenated sesquiterpenes, especially 10-epi-γ-eudesmol, and ß-eudesmol, are the major volatile components identified from GCMS analysis. PCA of LCMS analysis demonstrated that PC1 discriminated two clusters: essential oil, dichloromethane, and n-hexane extracts were in the positive quadrant, while methanol and ethyl acetate extracts were in the negative quadrant. Three-dimensional analysis of GCMS data revealed that n-hexane extract was in the superior quadrant, and its composition can be significantly distinguished from other extracts and essential oil. G. bancanus wood comprises valuable metabolites, i.e., terpenoids, which benefit the essential oil industry. Comprehensive extraction by performing solvents in different polarities on G. bancanus wood could allow exploration of fully extracted metabolites, supported by the exhibition of identified metabolites from LCMS and GCMS analysis.
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Óleos Voláteis , Terpenos , Solventes , BornéuRESUMO
A simple and concise three-component synthesis of a key pyrrole framework was developed from the reaction between α-hydroxyketones, oxoacetonitriles, and anilines. The synthesis was used to obtain several pyrrole-based drug candidates, including COX-2 selective NSAID, antituberculosis lead candidates BM212, BM521, and BM533, as well as several analogues. This route has potential to obtain diverse libraries of these pyrrole candidates in a concise manner to develop optimum lead compounds.
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Compostos de Anilina , Pirróis , Pirróis/farmacologiaRESUMO
Mesoporous heterojunction MOF-derived α-Fe2O3/ZnO composites were prepared by a simple calcination of α-Fe2O3/ZIF-8 as a sacrificial template. The optical properties confirm that coupling of both the modified pore and the n-n heterojunction effectively reduces the possibility of photoinduced charge carrier recombination under irradiation. The mesoporous Fe(25)ZnO with 25% loading of α-Fe2O3 exhibited the best performance in MB degradation, up to â¼100% after 150 minutes irradiation, higher than that of pristine ZnO and α-Fe2O3. Furthermore, after three cycles reusability, mesoporous Fe(25)ZnO still showed an excellent stability performance of up to 95.42% for degradation of MB. The proposed photocatalytic mechanism of mesoporous Fe(25)ZnO for the degradation of MB corresponds to the n-n heterojunction system. This study provides a valuable reference for preparing mesoporous MOF-derived metal oxides with an n-n heterojunction system to enhance MB photodegradation.
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In this study, chitosan (CS) doped sulphosuccinic acid (SSA)-glycerol (Gly) and modified montmorillonite clay (MMT) were successfully fabricated. The membranes were prepared using the solution casting method. Analysis of morphology and topography using scanning electron microscopy (SEM) and atomic force microscopy (AFM) revealed that the composite membrane with 3 wt% MMT filler, namely CS/MMT-1, possessed the most adequate surface roughness compared to the other fabricated membranes. Furthermore, mechanical characterization of the CS/MMT-1 composite membrane showed that the membrane achieved satisfactory mechanical strength with a value of 39.23 MPa. Proton conductivity of the composite membranes increased as the temperature was increased. The proton conductivity of the CS/MMT-1 composite membrane increased from 1.75 × 10-2 S cm-1 at 25 °C up to 3.57 × 10-2 S cm-1 at 80 °C. The CS/MMT-1 composite membrane also exhibited a methanol permeability value that was significantly lower than that of pristine CS, namely 1.22 × 10-7 cm2 s-1 and 12.49 × 10-7 cm2 s-1, respectively. The results of this study show that the fabricated composite membrane can be used as an alternative polymer electrolyte membrane (PEM) for DMFC applications.
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Nanocellulose (NC) composite membranes containing novel ternary materials including NC, imidazole (Im), and mesoporous phosphotungstic acid (m-PTA) were successfully fabricated by a phase inversion method. The single-particle size of NC was 88.79 nm with a spherical form. A m-PTA filler with a mesopore size of 4.89 nm was also successfully synthesized by a self-assembly method. Moreover, the fabricated membrane NC/Im/m-PTA-5 exhibited the best performances towards its proton conductivity and methanol permeability at 31.88 mS cm-1 and 1.74 × 10-6 cm2 s-1, respectively. The membrane selectivity was 1.83 × 104 S cm-3.
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The synthesized 3,3-di(indolyl)indolin-2-ones 1a-p showed desired higher α-glucosidase inhibitory activities and lower α-amylase inhibitory activities than standard drug acarbose. Particularly, compound 1i showed favorable higher α-glucosidase % inhibition of 67 ± 13 and lower α-amylase % inhibition of 51 ± 4 in comparison to acarbose with % inhibition activities of 19 ± 5 and 90 ± 2, respectively. Docking studies of selected 3,3-di(indolyl)indolin-2-ones revealed key interactions with the active sites of both α-glucosidase and α-amylase, further supporting the observed % inhibitory activities. Furthermore, the binding energies are consistent with the % inhibition values. The results suggest that 3,3-di(indolyl)indolin-2-ones may be developed as suitable Alpha Glucosidase Inhibitors (AGIs) and the lower α-amylase activities should be advantageous to reduce the side effects exhibited by commercial AGIs.
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Heterocyclic nitrogen compounds are privileged structures with many applications in the pharmaceutical and nutraceutical industries since they possess wide bioactivities. Trisindolines are heterocyclic nitrogen compounds consisting of an isatin core bearing two indole moieties. Trisindolines have been synthesized by reacting isatins with indoles using various routes and the yield greatly depends on the catalyst used, reaction conditions, and the substituents on both the isatin and indole moieties. Amongst the synthetic routes, acid-catalyzed condensation reaction between isatins and indoles are the most useful due to high yield, wide scope and short reaction times. Trisindolines are biologically active compounds and show anticancer, antimicrobial, antitubercular, antifungal, anticonvulsant, spermicidal, and antioxidant activities, among others. Trisindolines have not previously been reviewed. Therefore, this review aims to provide a comprehensive account of trisindolines including their natural occurrence, routes of synthesis, and biological activities. It aims to inspire the discovery of lead trisindoline drug candidates for further development.
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Over the past few decades, complementary medicine therapy using medicinal plants have been developed in healthcare. Phytochemical studies about medicinal plants have been conducted to verify their potency as medicinal remedies in modern therapeutics. Dipterocarpus littoralis commonly known as Meranti Jawa in Indonesia is traditionally used to treat diseases such as diarrhea, diabetic and malaria. This study aimed to isolate bioactive compounds from D. littoralis using bioguided fractionation method. The bioactivity measured were antioxidant, antidiabetic, and antiplasmodial activity. Alpha-glucosidase and alpha-amylase assays were applied to estimate the in vitro antidiabetic activity of D. littoralis. The antioxidant activities were determined by using the free radical scavenging assays 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2-2â³-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS). Analysis of total flavonoid and phenolic contents were expressed as Quercetin Equivalent (QE) and Gallic Acid Equivalent (GAE), respectively. The in vitro antiplasmodial activity test of methanol extract of D. littoralis was also conducted against Plasmodium falciparum strain 3D7. Purification of the ethyl acetate fraction of the methanol extract of D. littoralis resulted in an oligostilbenes namely α-viniferin (1). The structure of the α-viniferin was characterized by comprehensive spectral analysis including IR, 1D and 2D NMR, and in comparison with the literature data. Compound 1 showed an alpha-glucosidase and alpha-amylase inhibitory activity with IC50 values of 256.17 and 212.79 µg/mL, respectively. The in vitro antiplasmodial activity test against Plasmodium falciparum strain 3D7 at a concentration of 100 µg/mL revealed a strong antiplasmodial inhibitory activity with IC50 value of 2.76 µg/mL. Our findings indicated that α-viniferin (1) which is isolated from D. littoralis extract could be regarded as potential antidiabetic and antiplasmodial resources in the future.
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A simple trimethylsilyl trifluoromethanesulfonate (TMSOTf)-promoted intermolecular cascade reaction of aromatic diazo ketones with olefins has been developed. This method directly gave 3-phenylethylideneoxindoles from 3-diazooxindoles and styrenes with exclusive regioselectivity, chemoselectivity, and E-stereoselectivity. The key to the success of the reaction and higher yields is the elegant use of TMSOTf, which gradually released the active triflic acid promoter in situ. The reaction tolerates a wide substrate scope of 3-diazooxindoles and styrenes with electron-donating and electron-withdrawing groups and works well on the gram scale.
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Patchouli is used as an incense material and essential oil. The characteristic odor of patchouli leaves results from the drying process used in their production; however, there have to date been no reports on the changes in the odor of patchouli leaves during the drying process. We investigated the aroma profile of dried patchouli leaves using the hexane extracts of fresh and dried patchouli leaves. We focused on the presence or absence of the constituents of the fresh and dried extracts, and the differences in the content of the common constituents. Fourteen constituents were identified as characteristic of dried patchouli extract odor by gas chromatography-olfactometry analysis. The structures of seven of the 14 constituents were determined by gas chromatography-mass spectrometry (α-patchoulene, seychellene, humulene, α-bulnesene, isoaromadendrene epoxide, caryophyllene oxide, and patchouli alcohol). The aroma profile of the essential oil obtained from the dried patchouli leaves was clearly different from that of dried patchouli. The aroma profile of the essential oil was investigated by a similar method. We identified 12 compounds as important odor constituents. The structures of nine of the 12 constituents were determined by gas chromatography-mass spectrometry (cis-thujopsene, caryophyllene, α-guaiene, α-patchoulene, seychellene, α-bulnesene, isoaromadendrene epoxide, patchouli alcohol, and corymbolone). Comparing the odors and constituents demonstrated that the aroma profile of patchouli depends on the manufacturing process.
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Azulenos/isolamento & purificação , Odorantes/análise , Óleos Voláteis/química , Óleos Voláteis/isolamento & purificação , Extratos Vegetais/química , Óleos de Plantas/química , Óleos de Plantas/isolamento & purificação , Pogostemon/química , Sesquiterpenos de Guaiano/isolamento & purificação , Sesquiterpenos/isolamento & purificação , Azulenos/química , Cromatografia Gasosa , Cromatografia Gasosa-Espectrometria de Massas , Hexanos , Extração Líquido-Líquido/métodos , Olfatometria , Folhas de Planta/química , Sesquiterpenos Policíclicos , Sesquiterpenos/química , Sesquiterpenos de Guaiano/química , Terpenos/química , Terpenos/isolamento & purificaçãoRESUMO
AIM: To determine the prevalence of diabetic foot according to severity of disease, causing microorganism, resistance pattern of microorganism, and blood glucose level of diabetes mellitus (DM) patients at Koja Regional General Hospital, to provide additional information to improve patient follow-up. METHODS: This study is designed as a descriptive cross-sectional study. The population in this study consists of patients with diabetes mellitus patients admitted and treated at the internal medicine outpatient clinic of Koja Regional General Hospital from January 1999 to December 2004. RESULTS: We obtained a prevalence of diabetic foot according to the causal microorganisms as follows: Pseudomonas (40.9%), followed by Staphylococcus (29.5%). The prevalence of diabetic foot according to the blood glucose groups were: 9.5% having random blood glucose concentration of 150-200 mg/dl, 9.3% 201-250 mg/dl, 30% 251-300 mg/dl, and 30% >300 mg/dl. According to Wagner classification, most cases were classified as 0 degree, highly effective antibiotics treatment followed by fifth degree at 13.5%. In addition, the Pseudomonas were Cefotaxim 53.8% and Ceftriaxon 41.5%. CONCLUSION: According to the results of this study, the most common cause of diabetic foot is Pseudomonas, and the effective antibiotics treatment is Ceftriaxone and Cefotaxim. The prevalence of diabetic foot has increased along with increased blood glucose level, and according to Wagner classification, 0 degree was the most common, but fifth degree was also higher than 2nd to 4th degree.