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1.
Chem Biodivers ; : e202401209, 2024 Jun 12.
Artigo em Inglês | MEDLINE | ID: mdl-38865194

RESUMO

This research aimed to evaluate the antidiabetic, dermatoprotective, and antibacterial activities of Mentha viridis L. essential oil (MVEO) collected in the province of Ouezzane (Northwest Morocco). Gas chromatography-mass spectrometry (GC-MS) analysis revealed that the main constituents of MVEO were carvone (37.26%), 1,8-cineole (11.82%), limonene (5.27%), α-terpineol (4.16%), and ß-caryophyllene (4.04%). MVEO showed strong inhibitory effects on α-amylase and α-glucosidase activities, exceeding those of acarbose, but weak anti-elastase activity. The main compounds, ß-caryophyllene (IC50 = 79.91 ± 2.24 and 62.08 ± 2.78 µg/mL) and limonene (IC50 = 90.73 ± 3.47 and 68.98 ± 1, 60 µg/mL), demonstrated the strongest inhibitory effects on both digestive enzymes (α-glucosidase and α-amylase, respectively). In silico investigations, using molecular docking, also showed the inhibitory potential of these bioactive compounds against the enzymes tested. In conclusion, MVEO, due to its main components such as limonene, 1,8-cineole, ß-caryophyllene, carvone, and α-terpineol, shows promising prospects for drug discovery and natural therapeutic applications.

2.
Heliyon ; 10(9): e30453, 2024 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-38720726

RESUMO

Climate change results in continuous warming of the planet, threatening sustainable crop production around the world. Amaranth is an abiotic stress-tolerant, climate-resilient, C4 leafy orphan vegetable that has grown rapidly with great divergence and potential usage. The C4 photosynthesis allows amaranth to be grown as a sustainable future food crop across the world. Most amaranth species grow as weeds in many parts of the world, however, a few amaranth species can be also found in cultivated form. Weed species can be used as a folk medicine to relieve pain or reduce fever thanks to their antipyretic and analgesic properties. In this study, nutritional value, bioactive pigments, bioactive compounds content, and radical scavenging potential (RSP) of four weedy and cultivated (WC) amaranth species were evaluated. The highest dry matter, carbohydrate content, ash, content of iron, copper, sodium, boron, molybdenum, zinc, ß-carotene and carotenoids, vitamin C, total polyphenols (TP), RSP (DPPH), and RSP (ABTS+) was determined in Amaranthus viridis (AV). On the other hand, A. spinosus (AS) was found to have the highest content of protein, fat, dietary fiber, manganese, molybdenum, and total flavonoids (TF). In A. tricolor (AT) species the highest total chlorophyll, chlorophyll a and b, betaxanthin, betacyanin, and betalain content was determined. A. lividus (AL) was evaluated as the highest source of energy. AV and AT accessions are underutilized but promising vegetables due to their bioactive phytochemicals and antioxidants.

3.
Food Chem X ; 22: 101453, 2024 Jun 30.
Artigo em Inglês | MEDLINE | ID: mdl-38803670

RESUMO

This study aimed to explore the possibility of enriching cold-pressed Virginia (VIO) and Valencia (VAO) peanut oils with omega-3 fatty acids (FAs) from walnut oil (WO) to produce blended oils with improved nutritional value. The oxidative stability of pure and blended oils was examined under accelerated conditions (60 °C) for 28 days. The FA and tocopherol profiles, as well as nutritional quality indices, were determined. As the proportion of WO increased in the blends, the levels of linoleic and α-linolenic essential FAs increased, while oleic acid content decreased. Furthermore, γ- and δ-tocopherol levels rose, whereas α-tocopherol declined. Among the studied blends, VIO:WO blends, especially at a (70:30) ratio, were nutritionally favorable with a balanced FA profile. During storage, notable changes were observed in tocopherol levels, along with subtle alterations in the FA profile of the blended oils. Hence, the oxidative stability of pure VIO and VAO decreased with WO incorporation.

4.
Sci Rep ; 14(1): 12368, 2024 05 29.
Artigo em Inglês | MEDLINE | ID: mdl-38811671

RESUMO

Iron, a crucial micronutrient, is an integral element of biotic vitality. The scarcity of iron in the soil creates agronomic challenges and has a detrimental impact on crop vigour and chlorophyll formation. Utilizing iron oxide nanoparticles (IONPs) via nanopriming emerges as an innovative method to enhance agricultural efficiency and crop health. The objective of this study was to synthesize biogenic IONPs from Glycyrrhiza glabra (G. glabra) plant extract using green chemistry and to evaluate their nanopriming effects on rice seed iron levels and growth. The synthesized IONPs were analyzed using UV-Vis spectroscopy, Fourier-transform infrared spectroscopy (FTIR), Scanning electron microscope (SEM), Transmission electron microscopy (TEM), and Energy-dispersive X-ray (EDX) techniques. The UV-Vis peak at 280 nm revealed the formation of IONPs. SEM and TEM showed that the nanoparticles were spherical and had an average diameter of 23.8 nm. Nanopriming resulted in a substantial enhancement in growth, as seen by a 9.25% and 22.8% increase in shoot lengths for the 50 ppm and 100 ppm treatments, respectively. The yield metrics showed a positive correlation with the concentrations of IONPs. The 1000-grain weight and spike length observed a maximum increase of 193.75% and 97.73%, respectively, at the highest concentration of IONPs. The study indicates that G. glabra synthesized IONPs as a nanopriming agent significantly increased rice seeds' growth and iron content. This suggests that there is a relationship between the dosage of IONPs and their potential for improving agricultural biofortification.


Assuntos
Biofortificação , Glycyrrhiza , Oryza , Sementes , Oryza/crescimento & desenvolvimento , Oryza/metabolismo , Sementes/crescimento & desenvolvimento , Sementes/metabolismo , Sementes/química , Glycyrrhiza/química , Glycyrrhiza/crescimento & desenvolvimento , Glycyrrhiza/metabolismo , Extratos Vegetais/química , Nanopartículas Magnéticas de Óxido de Ferro/química , Química Verde/métodos , Ferro/metabolismo , Ferro/química , Compostos Férricos/química , Espectroscopia de Infravermelho com Transformada de Fourier
5.
Sci Rep ; 14(1): 7875, 2024 04 03.
Artigo em Inglês | MEDLINE | ID: mdl-38570564

RESUMO

This study examines the manufacturing, characterization, and biological evaluation of platinum nanoparticles, which were synthesized by Enterobacter cloacae and coated with Bovine Serum Albumin (BSA) and Resveratrol (RSV). The formation of PtNPs was confirmed with the change of color from dark yellow to black, which was due to the bioreduction of platinum chloride by E. cloacae. BSA and RSV functionalization enhanced these nanoparticles' biocompatibility and therapeutic potential. TGA, SEM, XRD, and FTIR were employed for characterization, where PtNPs and drug conjugation-related functional groups were studied by FTIR. XRD confirmed the crystalline nature of PtNPs and Pt-BSA-RSV NPs, while TGA and SEM showed thermal stability and post-drug coating morphological changes. Designed composite was also found to be biocompatible in nature in hemolytic testing, indicating their potential in Biomedical applications. After confirmation of PtNPs based nanocaompsite synthesis, they were examined for anti-bacterial, anti-oxidant, anti-inflammatory, and anti-cancer properties. Pt-BSA-RSV NPs showed higher concentration-dependent DPPH scavenging activity, which measured antioxidant capability. Enzyme inhibition tests demonstrated considerable anti-inflammatory activity against COX-2 and 15-LOX enzymes. In in vitro anticancer studies, Pt-BSA-RSV NPs effectively killed human ovarian cancer cells. This phenomenon was demonstrated to be facilitated by the acidic environment of cancer, as the drug release assay confirmed the release of RSV from the NP formulation in the acidic environment. Finally, Molecular docking also demonstrated that RSV has strong potential as an anti-oxidant, antibacterial, anti-inflammatory, and anticancer agent. Overall, in silico and in vitro investigations in the current study showed good medicinal applications for designed nanocomposites, however, further in-vivo experiments must be conducted to validate our findings.


Assuntos
Nanopartículas Metálicas , Nanopartículas , Humanos , Soroalbumina Bovina/química , Nanopartículas Metálicas/química , Resveratrol/farmacologia , Platina/farmacologia , Platina/química , Antioxidantes/farmacologia , Simulação de Acoplamento Molecular , Nanopartículas/química , Anti-Inflamatórios
6.
BMC Complement Med Ther ; 24(1): 157, 2024 Apr 12.
Artigo em Inglês | MEDLINE | ID: mdl-38609946

RESUMO

BACKGROUND: Oral bacterial infections are difficult to treat due to emergence of resistance against antibiotic therapy. Essential oils are considered emerging alternate therapy against bacterial infections and biofilms. We investigated Citrus bergemia flower essential oil against oral pathogens. METHODS: The essential oil was analsyed using Gas Chromatography(GC-MS), in silico investigations, antioxidant, antimicrobial, antibiofilm and antiquorum sensing assays. RESULTS: Gas Chromatography analysis confirmed presence of 17 compounds including 1,6-Octadien-3-ol,3,7-dimethyl, 48.17%), l-limonene (22.03%) and p-menth-1-ol, 8-ol (7.31%) as major components. In silico analysis showed compliance of all tested major components with Lipinski's rule, Bioavailability and antimicrobial activity using PASS (prediction of activity spectrum of substances). Molecular docking with transcriptional regulators 3QP5, 5OE3, 4B2O and 3Q3D revealed strong interaction of all tested compounds except 1,6-Octadien-3-ol,3,7-dimethyl. All tested compounds presented significant inhibition of DPPH (2,2-diphenyl-1-picrylhydrazyl) (IC50 0.65 mg/mL), H2O2 (hydrogen peroxide) (63.5%) and high FRAP (ferrous reducing antioxidant power) value (239.01 µg). In antimicrobial screening a significant activity (MIC 0.125 mg/mL) against Bacillus paramycoides and Bacillus chungangensis was observed. Likewise a strong antibiofilm (52.1 - 69.5%) and anti-QS (quorum sensing) (4-16 mm) activity was recorded in a dose dependent manner. CONCLUSION: It was therefore concluded that C. bergemia essential oil posess strong antioxidant, antimicrobial and antibiofilm activities against tested oral pathogens.


Assuntos
Anti-Infecciosos , Infecções Bacterianas , Citrus , Óleos Voláteis , Antioxidantes/farmacologia , Peróxido de Hidrogênio , Simulação de Acoplamento Molecular , Óleos Voláteis/farmacologia , Anti-Infecciosos/farmacologia , Flores
7.
Chem Biodivers ; 21(5): e202301399, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38393939

RESUMO

Imidazoles and phenylthiazoles are an important class of heterocycles that demonstrate a wide range of biological activities against various types of cancers, diabetes mellitus and pathogenic microorganisms. The heterocyclic structure having oxothiazolidine moiety is an important scaffold present in various drugs, with potential for enzyme inhibition. In an effort to discover new heterocyclic compounds, we synthesized 26 new 4,5-diphenyl-1H-imidazole, phenylthiazole, and oxothiazolidine heterocyclic analogues that demonstrated potent α-glucosidase inhibition and anticancer activities. Majority of the compounds noncompetitively inhibited α-glucosidase except for two that exhibited competitive inhibition of the enzyme. Docking results suggested that the noncompetitive inhibitors bind to an apparent allosteric site on the enzyme located in the vicinity of the active site. Additionally, the analogues also exhibited significant activity against various types of cancers including non-small lung cancer. Since tubulin protein plays an important role in the pathogenesis of non-small lung cancer, molecular docking with one of the target compounds provided important clues to its binding mode. The current work on imidazoles and phenylthiazole derivatives bears importance for designing of new antidiabetic and anticancer drugs.


Assuntos
Antineoplásicos , Inibidores de Glicosídeo Hidrolases , Simulação de Acoplamento Molecular , alfa-Glucosidases , Antineoplásicos/farmacologia , Antineoplásicos/química , Antineoplásicos/síntese química , Humanos , Inibidores de Glicosídeo Hidrolases/síntese química , Inibidores de Glicosídeo Hidrolases/farmacologia , Inibidores de Glicosídeo Hidrolases/química , alfa-Glucosidases/metabolismo , Relação Estrutura-Atividade , Ensaios de Seleção de Medicamentos Antitumorais , Estrutura Molecular , Tiazóis/química , Tiazóis/farmacologia , Tiazóis/síntese química , Linhagem Celular Tumoral , Imidazóis/química , Imidazóis/farmacologia , Imidazóis/síntese química , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga
8.
Heliyon ; 10(4): e25814, 2024 Feb 29.
Artigo em Inglês | MEDLINE | ID: mdl-38375246

RESUMO

Salvia (Lamiaceae family) is used as a brain tonic to improve cognitive function. The species including S. plebeia and S. moorcroftiana are locally used to cure hepatitis, cough, tumours, hemorrhoids, diarrhoea, common cold, flu, and asthma. To the best of authors' knowledge, no previous study has been conducted on synthesis of S. plebeia and S. moorcroftiana silver nanoparticles (SPAgNPs and SMAgNPs). The study was aimed to synthesize AgNPs from the subject species aqueous and ethanol extracts, and assess catalytic potential in degradation of standard and extracted (from yums, candies, and snacks) dyes, nitrophenols, and antibiotics. The study also aimed at AgNPs as probe in sensing metalloids and heavy metal ions including Pb2+, Cu2+, Fe3+, Ni2+, and Zn2+. From the results, it was found that Salvia aqueous extract afforded stable AgNPs in 1:9 and 1:15 (quantity of aqueous extract and silver nitrate solution concentration) whereas ethanol extract yielded AgNPs in 1:10 (quantity of ethanol extract and silver nitrate solution concentration) reacted in sunlight. The size of SPAgNPs and SMAgNPs determined by scanning electron microscopy (SEM) and transmission electron microscopy (TEM) were 21.7 nm and 19.9 nm, with spherical, cylindrical, and deep hollow morphology. The synthesized AgNPs demonstrated significant potential as catalyst in dyes; Congo red (85 %), methylene blue (75 %), Rhodamine B (<50 %), nitrophenols; ortho-nitrophenol (95-98 %) and para-nitrophenol (95-98 %), dyes extracted from food samples including yums, candies, and snacks. The antibiotics (amoxicillin, doxycycline, levofloxacin) degraded up to 80 %-95 % degradation. Furthermore, the synthesized AgNPs as probe in sensing of Pb2+, Cu2+, and Fe3+ in Kabul river water, due to agglomeration, caused a significant decrease and bathochromic shift of SPR band (430 nm) when analyzed after 30 min. The Pb2+ ions was comparatively more agglomerated and chelated. Thus, the practical applicability of AgNPs in Pb2+ sensing was significant. Based on the results of this research study, the synthesized AgNPs could provide promising efficiency in wastewater treatment containing organic dyes, antibiotics, and heavy metals.

9.
J Biomol Struct Dyn ; 42(4): 1826-1845, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-37114651

RESUMO

Three triorganotin(IV) compounds, R3Sn(L), with R = CH3 (1), n-C4H9 (2) and C6H5 (3), and LH = 4-[(2-chloro-4-methylphenyl)carbamoyl]butanoic acid, were prepared and confirmed by various techniques. A five-coordinate, distorted trigonal-bipyramidal geometry was elucidated for tin(IV) centres both in solution and solid states. An intercalation mode was confirmed for the compound SS-DNA interaction by UV-visible, viscometric techniques and molecular docking. MD simulation revealed stable binding of LH with SS-DNA. Anti-bacterial investigation revealed 2 to be generally the most potent, especially against Sa and Ab, i.e. having the lowest MIC values (≤0.25 µg/mL) compared to the standard anti-biotics vancomycin-HCl (MIC = 1 µg/mL) and colistin-sulphate (MIC = 0.25 µg/mL). Similarly, the anti-fungal profile shows 2 exhibits 100% inhibition against Ca and Cn fungal strains and has MIC values (≤0.25 µg/mL) comparatively lower than standard drug fluconazole (0.125 and 8 µg/mL for Ca and Cn, respectively). Compound 2 has the greatest activity with CC50 ≤ 25 µg/mL and HC50 > 32 µg/mL performed against HEC239 and RBC cell lines. The anti-cancer potential was assessed against the MG-U87 cell line, using cisplatin as the standard (133 µM), indicates 2 displays the greatest activity (IC50: 5.521 µM) at a 5 µM dose. The greatest anti-leishmanial potential was observed for 2 (87.75 at 1000 µg/mL) in comparison to amphotericin B (90.67). The biological assay correlates with the observed maximum of 89% scavenging activity exhibited by 2. The Swiss-ADME data publicised the screened compounds generally follow the rule of 5 of drug-likeness and have good bioavailability potential.


Assuntos
DNA , Simulação de Acoplamento Molecular , Ácido Butírico , Linhagem Celular , DNA/química , Simulação por Computador , Testes de Sensibilidade Microbiana
10.
J Enzyme Inhib Med Chem ; 39(1): 2288548, 2024 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-38073431

RESUMO

Isatin, known as 1H-indole-2,3-dione, was originally recognised as a synthetic molecule until its discovery in the fruits of the cannonball tree, Couroupita guianensis. It is naturally occurring in plants of the genus Isatis and serves as a metabolic derivative of adrenaline in humans. Isatin possesses significant pharmacological importance, and its synthetic versatility has prompted extensive interest in its derivative compounds due to their diverse biological and pharmacological properties. These derivatives represent a valuable class of heterocyclic compounds with potential applications as precursors for synthesizing numerous valuable drugs. In the pursuit of advancing our research on isatin hybrids, we investigate the utilisation of readily available hydrazonoindolin-2-one and isatin as starting materials for the synthesis of a wide range of analogues. Characterisation of the synthesized compounds was carried out through various analytical techniques. Furthermore, the obtained compounds were subjected to extensive testing to evaluate their anticancer and antimicrobial activities. Specifically, their efficacy against key proteins, namely Staphylococcus aureus protein (PDB ID: 1JIJ), Escherichia coli protein (PDB ID: 1T9U), Pseudomonas aeruginosa protein (PDB ID: 2UV0), and Acinetobacter baumannii protein (PDB ID: 4HKG), was examined through molecular docking calculations. Several molecules, such as 3, 4, 6, 16, and 19, displayed remarkable activity against the renal cancer cell line UO-31. Additionally, the results of antimicrobial activity testing revealed that compound 16 exhibited significant cytotoxicity against Candida albicans and Cryptococcus neoformans. Subsequently, ADME/T calculations were performed to gain insights into the potential effects and reactions of these molecules within human metabolism. This comprehensive study provides valuable insights into the potential pharmacological applications of isatin derivatives and underscores their significance in drug development.


Assuntos
Anti-Infecciosos , Antineoplásicos , Isatina , Humanos , Simulação de Acoplamento Molecular , Isatina/farmacologia , Antineoplásicos/farmacologia , Anti-Infecciosos/farmacologia , Linhagem Celular , Estrutura Molecular , Relação Estrutura-Atividade , Antibacterianos/farmacologia
11.
Front Cell Dev Biol ; 10: 972111, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36299484

RESUMO

Due to poor diagnosis breast cancer in women has emerged as the most common cause of death disease in developing countries. Medicinal plants have been used for thousands of years and can be useful in healthcare, especially in developing countries. Ethanol extracts of leaves of fire bush or arta (Calligonum comosum; EECC), exhibited significant anticancer potencies against two breast cancer cell lines, MCF-7 and MDA 231. These in vitro effects of EECC indicated potential anticancer activities that were determined to be specific since minimal toxicity was recorded against MCF-12, a non-cancerous breast cell line used as a reference. EECC also induced cell cycle arrest in MCF-7 and MDA 231 as revealed by the increased proportions of sub-G1 cells. Fluorescence-activated cell sorter analysis (FACS), utilizing double staining by annexin V-FITC/propidium iodide, revealed that the observed cytotoxic effects were mediated via apoptosis and necrosis. FACS measurement of thegreater in fluorescence intensity, linked with oxidation of DCFH to DCF, revealed that apoptosis was attributable to production of free radicals. EECC-mediated apoptosis was further validated by observation of up-regulation in the "executioner" enzyme, caspase 3. The current findings reveal that EECC exhibits significant, selective cytotoxicity to breast cancer cells, that proceeds via the generation of ROS, which culminates in apoptosis. The anti-proliferative effects of EECC weres further verified by use of a structure-based, virtual screening between its major bioactive polyphenolic constituents and the apoptosis executioner marker enzyme, caspase-3. Based on their glide score values against the active site of caspase 3, some phyto-constituents present in EECC, such as DL-alpha-tocopherol and campesterol, exhibited distinctive, drug-like potential with no predicted toxicity to non-target cells. Taken together, the usefulness of natural phenolic and flavonoid compounds contained in Calligonum comosum were suggested to be potent anticancer agents.

12.
Antioxidants (Basel) ; 11(8)2022 Aug 03.
Artigo em Inglês | MEDLINE | ID: mdl-36009233

RESUMO

Centaurea calcitrapa has been intensively utilized in ethnomedicinal practices as a natural therapeutic recipe to cure various ailments. The current study aimed to chemically characterize ethanolic extract of C. calcitrapa (EECC) aerial parts (leaves and shoots) by use of gas chromatography-mass spectrometry analyses (GC-MS) and investigate its antioxidant and in vitro anticancer activities, elucidating the underlying molecular mechanism by use of flow cytometry-based fluorescence-activated cell sorting (FACS) and conducting in silico assessment of binding inhibitory activities of EECC major compounds docked to caspase-3. CG-MS profiling of EECC identified a total of 26 major flavonoids and polyphenolic compounds. DPPH and ABTS assays revealed that EECC exhibits potent antioxidant activity comparable to standard reducing agents. Results of the proliferation assay revealed that EECC exhibit potent, dose-dependent cytotoxic activities against triple-positive (MCF-7) and triple-negative (MDA-MB-231) breast cancer cell models, with IC50 values of 1.3 × 102 and 8.7 × 101 µg/mL, respectively. The observed cytotoxic effect was specific to studied cancer cells since EECC exhibited minimal (~<10%) cytotoxicity against MCF-12, a normal breast cell line. FACS analysis employing annexin V-FITC/propidium iodide double labeling demonstrated that the observed anti-proliferative activity against MCF-7 and MDA-MB-231 was mediated via apoptotic as well as necrotic signaling transduction processes. The increase in fluorescence intensity associated with DCFH oxidation to DCF, as reported by FACS, indicated that apoptosis is caused by generation of ROS. The use of caspase-3-specific fluorogenic substrate revealed a dose-dependent elevation in caspase-3 substrate-cleavage activity, which further supports EECC-mediated apoptosis in MCF-7 cells. The major EECC compounds were examined for their inhibitory activity against caspase-3 receptor (1HD2) using molecular docking. Three compounds exhibited the highest glide score energy of −5.156, −4.691 and −4.551 kcal/mol, respectively. Phenol, 2,6-dimethoxy established strong binding in caspase-3 receptor of hydrogenic type, with residue ARG 207 and of PI-PI stacking type with residue HIS 121. By contract, hexadecenoic acid showed 3 H-bond with the following residues: ASN 615, ASN 616a and THR 646. Taken together, the current findings reveal that EECC exhibits significant and specific cytotoxicity against breast cancer cells mediated by the generation of ROS and culminating into necrosis and apoptosis. Further investigations of the phytoconstituents-rich C. calcitrapa are therefore warranted against breast as well as other human cancer cell models.

14.
Microsc Res Tech ; 85(3): 900-916, 2022 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-34664754

RESUMO

Investigation of alternative energy sources is need of current time due to growing power crisis and associated environmental issues. Biodiesel is considered as sustainable power source and promising alternative to fossil fuels. Therefore, our current investigation aimed to identify micromorphological characters of 10 novel nonedible oil-yielding seeds through scanning electron microscopy. It was revealed from light microscopic study that there is variation in seed size from 3 to 15 mm in length and 2 to 11 mm in width. Likewise, a huge variation in color was observed such as light green, greenish yellow, blackish brown, and various shades of brown. Presence and absence of Hilum was observed, and compression of seeds varied from depressed, lateral, and dorsoventral. Seed's shape differs from ovate, clavate, triangular ovate, cuneiform, ovoid, and elliptical shape. Seed oil content fall in range of 18-58% (wt/wt). Free fatty acid content of the seeds varies from 0.3 to 3.1 mg KOH/g. Ultrastructure of seeds exhibited huge variation in shape, size, periclinal wall, anticlinal wall, and surface ornamentation. Nonedible seeds varied in wall structure from angular, wavy, dentate entire, irregular, puzzled, elongated, even, and polygonal. The periclinal wall arrangements show alteration from flat, looped, raised, depressed, lofty, even, pentagonal, polygonal, and undulate seed margins. Outcomes of this investigation recommended that scanning electron microscopy could act as a helpful tool in disclosing the hidden micromorphological characters among nonedible oil-yielding seeds and subsequently helping in correct, authentic seed identification and classification as potential feedstock for biodiesel.


Assuntos
Biocombustíveis , Óleos de Plantas , Microscopia Eletrônica de Varredura
15.
Pharmaceutics ; 13(8)2021 Aug 21.
Artigo em Inglês | MEDLINE | ID: mdl-34452271

RESUMO

The current study is aimed to fabricate doxorubicin (Dox) loaded mild temperature responsive liposomes (MTLs) by thin film hydration technique for enhanced in vitro and in vivo anticancer efficacy against hepatocellular carcinoma. The aforementioned Dox loaded MTLs were developed and optimized with extrusion and drug loading techniques. The optimized MTLs were in optimum size range (118.20 ± 2.81-187.13 ± 4.15 nm), colloidal stability (-13.27 ± 0.04 to -32.34 ± 0.15 mV), and enhanced entrapment of Dox (28.71 ± 2.01-79.24 ± 2.16). Furthermore, the optimized formulation (MTL1-E(AL)) embodied improved physicochemical stability deducted by Fourier transform infra-red (FTIR) spectroscopy and mild hyperthermia-based phase transition demonstrated from differential scanning calorimetry (DSC). An in vitro drug release study revealed mild hyperthermia assisted rapid in vitro Dox release from MTLs-E(AL) (T100% ≈ 1 h) by Korsmeyer-Peppas model based Fickian diffusion (n < 0.45). Likewise, an in vitro cytotoxicity study and lower IC50 values also symbolized mild hyperthermia (40.2 °C) based quick and improved cytotoxicity of MTL1-E(AL) in HepG2 and MCF-7 cells than Dox. The fluorescence microscopy also represented enhanced cellular internalization of MTL1-E(AL) at mild hyperthermia compared to the normothermia (37.2 °C). In addition, an in vivo animal study portrayed the safety, improved anticancer efficacy and healing of hepatocellular carcinoma (HCC) through MTL1-E(AL). In brief, the Dox loaded MTLs could be utilized as safe and effective therapeutic strategy against HCC.

16.
Pharmaceutics ; 13(3)2021 Mar 17.
Artigo em Inglês | MEDLINE | ID: mdl-34156396

RESUMO

Bioassays guided phytochemical investigations on the ethyl acetate-soluble fraction of the root material of Ballota pseudodictamnus (L.) Benth. led to the isolation of two new compounds, ballodiolic acid A (1) and ballodiolic acid B (2), along with three known compounds ballodiolic acid (3), ballotenic acid (4), and ß-amyrin (5), which were also isolated for the first time from this species by using multiple chromatographic techniques. The structures of the compounds (1-5) were determined by modern spectroscopic analysis including 1D and 2D NMR techniques and chemical studies. In three separate experiments, the isolated compounds (1-5) demonstrated potent antioxidant scavenging activity, with IC50 values ranging from 07.22-34.10 µM in the hydroxyl radical (•OH) inhibitory activity test, 58.10-148.55 µM in the total ROS (reactive oxygen species) inhibitory activity test, and 6.23-69.01 µM in the peroxynitrite (ONOO-) scavenging activity test. With IC50 values of (07.22 ± 0.03, 58.10 ± 0.07, 6.23 ± 0.04 µM) for •OH, total ROS, and scavenge ONOO-, respectively, ballodiolic acid B (2) showed the highest scavenging ability. Antibacterial and antifungal behaviors were also exposed to the pure compounds 1-5. In contrast to compounds 4 and 5, compounds 1-3 were active against all bacterial strains studied, with a good zone of inhibition proving these as a potent antibacterial agent. Similarly, compared to compounds 3-5, compounds 1 and 2 with a 47 percent and 45 percent respective inhibition zone were found to be more active against tested fungal strains.

17.
Molecules ; 26(5)2021 Feb 26.
Artigo em Inglês | MEDLINE | ID: mdl-33652639

RESUMO

Hepatitis C is affecting millions of people around the globe annually, which leads to death in very high numbers. After many years of research, hepatitis C virus (HCV) remains a serious threat to the human population and needs proper management. The in silico approach in the drug discovery process is an efficient method in identifying inhibitors for various diseases. In our study, the interaction between Epigallocatechin-3-gallate, a component of green tea, and envelope glycoprotein E2 of HCV is evaluated. Epigallocatechin-3-gallate is the most promising polyphenol approved through cell culture analysis that can inhibit the entry of HCV. Therefore, various in silico techniques have been employed to find out other potential inhibitors that can behave as EGCG. Thus, the homology modelling of E2 protein was performed. The potential lead molecules were predicted using ligand-based as well as structure-based virtual screening methods. The compounds obtained were then screened through PyRx. The drugs obtained were ranked based on their binding affinities. Furthermore, the docking of the topmost drugs was performed by AutoDock Vina, while its 2D interactions were plotted in LigPlot+. The lead compound mms02387687 (2-[[5-[(4-ethylphenoxy) methyl]-4-prop-2-enyl-1,2,4-triazol-3-yl] sulfanyl]-N-[3(trifluoromethyl) phenyl] acetamide) was ranked on top, and we believe it can serve as a drug against HCV in the future, owing to experimental validation.


Assuntos
Catequina/análogos & derivados , Hepacivirus/efeitos dos fármacos , Hepatite C/tratamento farmacológico , Proteínas do Envelope Viral/genética , Antivirais/química , Antivirais/farmacologia , Catequina/química , Catequina/farmacologia , Hepacivirus/genética , Hepacivirus/patogenicidade , Hepatite C/virologia , Humanos , Ligantes , Simulação de Acoplamento Molecular , Polifenóis/química , Polifenóis/farmacologia , Chá/química , Envelope Viral/química , Proteínas do Envelope Viral/antagonistas & inibidores , Internalização do Vírus/efeitos dos fármacos
18.
Molecules ; 26(3)2021 Jan 26.
Artigo em Inglês | MEDLINE | ID: mdl-33530597

RESUMO

Caralluma europaea (Guss.) N.E.Br.: (C. europaea) is a wild medicinal plant belonging to the family Apocynaceae. It is commonly used in traditional medicines for treating several diseases. The present work aims to evaluate the anti-inflammatory, antibacterial, and antifungal potentials of C. europaea fractions including hydro ethanol (ET CE), n-butanol (But CE), and polyphenol (Poly CE). The chemical composition of hydroethanol, n-butanol, and polyphenol-rich fractions from C. europaea were determined using GC-MS after silylation. The anti-inflammatory effect of hydroethanol, n-butanol, and polyphenol-rich fractions was studied by carrageenan-induced paw edema. Antibacterial and antifungal activities of hydroethanol, n-butanol, and polyphenol-rich fractions against Gram-positive bacteria, Gram-negative bacteria, and yeasts were assessed using the disc diffusion and micro-dilution assays. The findings of the chemical characterization affirmed the presence of interesting bioactive compounds in C. europaea fractions. The polyphenol-rich fraction was the best inhibitor of edema by75.68% after 6 h of treatment. The hydroethanol fraction was the most active against both bacteria and yeasts. This study contributes to society as it provides potential bioactive compounds in C. europaea extract, which may help in fighting nosocomial antibiotic-resistant microbes.


Assuntos
Anti-Infecciosos/administração & dosagem , Anti-Inflamatórios/administração & dosagem , Apocynaceae/química , Infecção Hospitalar/microbiologia , Inflamação/tratamento farmacológico , Compostos Fitoquímicos/administração & dosagem , 1-Butanol/administração & dosagem , 1-Butanol/isolamento & purificação , 1-Butanol/farmacologia , Animais , Antibacterianos/administração & dosagem , Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Anti-Infecciosos/isolamento & purificação , Anti-Infecciosos/farmacologia , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Antifúngicos/administração & dosagem , Antifúngicos/isolamento & purificação , Antifúngicos/farmacologia , Candida albicans/efeitos dos fármacos , Carragenina/efeitos adversos , Infecção Hospitalar/tratamento farmacológico , Farmacorresistência Bacteriana/efeitos dos fármacos , Farmacorresistência Fúngica/efeitos dos fármacos , Feminino , Cromatografia Gasosa-Espectrometria de Massas , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Humanos , Inflamação/induzido quimicamente , Masculino , Testes de Sensibilidade Microbiana , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Polifenóis/administração & dosagem , Polifenóis/isolamento & purificação , Polifenóis/farmacologia , Ratos , Saccharomyces cerevisiae/efeitos dos fármacos
19.
Drug Deliv ; 27(1): 1271-1282, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-32885688

RESUMO

Antibiotic resistance amongst microbial pathogens is a mounting serious issue in researchers and physicians. Various alternatives to overcome the multidrug-resistant bacterial infections are under search, and biofilm growth inhibition is one of them. In this investigation, a polymeric drug delivery system loaded with multi-serratial drugs to improve the delivery of drugs against urinary tract infection causative Serratia marcescens. The chitosan grafted pyromellitic dianhydride - cysteine (CS-g-PMDA-CYS) was conjugated with AuNPs by using the -SH group of CYS and RF (rifampicin) and INH (isoniazid) were loaded in AuNPs-fused CS-g-PMDA-CYS system. Several physicochemical techniques characterized this fabricated AuNPs/RF/INH/CS-g-PMDA-CYS system. The successful encapsulation of RF and INH in AuNPs-fused CS-g-PMDA-CYS polymer had confirmed, and it observed the loading capacity for RF and INH was 9.02% and 13.12%, respectively. The in vitro drug discharge pattern was perceived high in pH 5.5 compared with pH 7.4. The AuNPs/RF/INH/CS-g-PMDA-CYS escalates 74% of Caenorhabditis elegans survival during Serratia marcescens infection by aiming biofilm development and virulence in S. marcescens. Author postulate that the fabricated system is a promising drug carrier and delivery system for inhibition of multidrug-resistant bacterias like S. marcescens.


Assuntos
Antibacterianos/administração & dosagem , Sistemas de Liberação de Medicamentos/métodos , Farmacorresistência Bacteriana Múltipla/efeitos dos fármacos , Compostos de Ouro/administração & dosagem , Nanopartículas Metálicas/administração & dosagem , Serratia marcescens/efeitos dos fármacos , Animais , Antibacterianos/química , Benzoatos/administração & dosagem , Benzoatos/síntese química , Caenorhabditis elegans/efeitos dos fármacos , Caenorhabditis elegans/microbiologia , Caenorhabditis elegans/fisiologia , Quitosana/administração & dosagem , Quitosana/síntese química , Cisteína/administração & dosagem , Cisteína/síntese química , Farmacorresistência Bacteriana Múltipla/fisiologia , Compostos de Ouro/síntese química , Nanopartículas Metálicas/química , Testes de Sensibilidade Microbiana/métodos , Infecções por Serratia/tratamento farmacológico , Serratia marcescens/fisiologia , Infecções Urinárias/tratamento farmacológico , Difração de Raios X/métodos
20.
Artigo em Inglês | MEDLINE | ID: mdl-32256660

RESUMO

BACKGROUND: Caralluma europaea (C. europaea) is a medicinal plant used in Moroccan popular medicine. Objective of the Study. The present work was aimed at identifying the chemical composition and the antioxidant and antiproliferative activities of hydroethanolic and bioactive compound classes of C. europaea) is a medicinal plant used in Moroccan popular medicine. Materials and Methods. The chemical composition was analyzed using HPLC. The antioxidant power was determined using both DPPH and FRAP assays. The antiproliferative activity was effectuated against cancerous cells using WST-1. RESULTS: The chemical analysis showed the presence of bioactive constituents such as quercetin, myricetin, and hesperetin. The polyphenol and flavonoid contents were estimated at 51.42 mg GA/g and 20.06 mg EQ/g, respectively. The EC50 values of FRAP assay of hydroethanolic, flavonoid, saponin, and mucilage extracts were 5.196 mg/ml, 4.537 mg/ml, 3.05 mg/ml, and 6.02 mg/ml, respectively. The obtained IC50 values with the DPPH test were 1.628 mg/ml, 1.05 mg/ml, 1.94 mg/ml, and 9.674 mg/ml, respectively. Regarding MDA-MB-231, saponins were highly effective even with the lowest concentration (15.62 µg/ml). The flavonoids decreased the cell viability with IC50 values of 43.62 ± 0.06 µg/ml). The flavonoids decreased the cell viability with IC50 values of 43.62 ± 0.06 µg/ml). The flavonoids decreased the cell viability with IC50 values of 43.62 ± 0.06 . CONCLUSION: The present results suggest that C. europaea) is a medicinal plant used in Moroccan popular medicine.

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