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1.
Molecules ; 27(19)2022 Sep 26.
Artigo em Inglês | MEDLINE | ID: mdl-36234897

RESUMO

Cydonia oblonga is a medicinal plant that is used to treat a number of health complications in traditional medication systems. The objective of this study was to evaluate the phytochemical composition, and antibacterial, antioxidant, and ant-diabetic potentials of methanolic extracts of Cydonia oblonga bark. The Cydonia oblonga bark extraction was fractionated through HPLC and seven purified fractions labeled as F1, F2, F3, F4, F5, F6, and F7 were obtained. The HPLC-UV analysis of methanolic extract showed the presence of a number of possible compounds. The GC-MS and HPLC analysis confirmed the presence of the following bioactive compounds in the crude extract and purified fractions: malic acid, mandelic acid, quercetin, caffeic acid, catechin hydrate, as morin (HPLC analysis), BIS-(2-ethylhexyl)phthalate and diisooctyl phthalate (F1), carbamide (F2, used as fertilizer), octasiloxane and dimethylsiloxanecyclictrimer (F3), silicic acid and cyclotrisiloxane (F4), 6-AH-cAMP, 4H-cyclopropa[5',6']benz[1',2',7,8]azule, and 4-(4-chlorophenyl)-3-morpholinepyrol-2-yl)-butenedioic acid (F5), isopropyamine (F6), and 1-propylhydrazine (F7). The extract and purified fractions were then tested for biological activities. All the purified fractions and methanolic extract showed effective antibacterial activity; however, the highest activity was recorded for methanolic extract against Staphylococcus aureus and Streptococcus pneumonia. Antioxidant evaluation of methanolic extract and purified fractions against DPPH showed strong % inhibition of the synthetic free radical. The methanolic extract exhibited 87.41 ± 0.54% inhibition whereas fractions showed: F1, 85.45 ± 0.85; F2, 65.78 ± 0.68; F3, 58.61 ± 0.58; F4, 80.76 ± 0.59; F5, 571.29 ± 0.49; F6, 85.28 ± 0.94; and F7, 48.45 ± 0.62% inhibition. Ascorbic acid (standard) was used as a control with 94.88 ± 0.56% inhibition at a maximum concentration of 1000 µg/mL. The α-glucosidase inhibition assay of methanolic extract and purified fractions at a maximum concentration of 1000 µg/mL showed activities as: methanolic extract, 78.21 ± 0.67; F1, 55.01 ± 0.29; F2, 56.10 ± 0.24; F3, 62.44 ± 1.03; F4, 70.52 ± 0.15; F5, 62.18 ± 0.92; F6, 72.68 ± 0.2; and F7, 57.33 ± 0.05% inhibition. α-Amylase % inhibition of methanolic extract and purified fractions were noted as: methanolic extract, 77.98 ± 0.57; F1, 79.72 ± 0.02; F2, 79.72 ± 0.02; F3, 82.16 ± 0.48; F4, 77.37 ± 0.28; F5, 72.14 ± 0.30; F6, 74.24 ± 0.29; and F7, 56.58 ± 0.10 at the highest concentration of 1000 µg/mL. Acarbose (standard) showed 87.65 ± 0.71% inhibition of α-glucosidase and 85.99 ± 0.44% inhibition of α-amylase at the highest concentration of 1000 µg/mL. It was found that all biological activities of methanolic extract and purified fractions might be attributed to the fact that they are rich sources of phenolic and flavonoids along with other bioactive compounds. The total phenolic and flavonoid contents of methanolic extract were recorded higher as compared to purified fractions (TPC = 70% and TFC = 69%). Amongst the purified fractions, fraction 6 exhibited the highest TPC value (64%), and purified fraction 1 exhibited the highest value of TFC (58%). Recent research demonstrated that Cydonia oblonga may be considered an antibacterial medicinal plant. The result of the present study revealed that it might be utilized for the isolation of bioactive phytochemicals that can lead to new opportunities in the discovery of new antibiotics.


Assuntos
Catequina , Rosaceae , Acarbose/análise , Antibacterianos/análise , Antibacterianos/farmacologia , Antioxidantes/química , Ácido Ascórbico/análise , Catequina/análise , Fertilizantes/análise , Flavonoides/farmacologia , Radicais Livres/análise , Hipoglicemiantes/análise , Hipoglicemiantes/farmacologia , Fenóis/análise , Compostos Fitoquímicos/química , Casca de Planta/química , Extratos Vegetais/química , Quercetina/análise , Quercetina/farmacologia , Ácido Silícico , Ureia/análise , alfa-Amilases , alfa-Glucosidases
2.
Molecules ; 27(16)2022 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-36014445

RESUMO

Schiff bases are a class of organic compounds with azomethine moiety, exhibiting a wide range of biological potentials. In this research, six chiral Schiff bases, three 'S' series (H1−H3) and three 'R' series (H4−H6), were synthesized. The reaction was neat, which means without a solvent, and occurred at room temperature with a high product yield. The synthesized compounds were evaluated for analgesic potential in vivo at doses of 12.5 and 25 mg/kg using acetic-acid-induced writhing assay, formalin test, tail immersion and hot plate models, followed by investigating the possible involvement of opioid receptors. The compounds H2 and H3 significantly (*** p < 0.001) reduced the writhing frequency, and H3 and H5 significantly (*** p < 0.001) reduced pain in both phases of the formalin test. The compounds H2 and H5 significantly (*** p < 0.001) increased latency at 90 min in tail immersion, while H2 significantly (*** p < 0.001) increased latency at 90 min in the hot plate test. The 'S' series Schiff bases, H1−H3, were found more potent than the 'R' series compounds, H4−H6. The possible involvement of opioid receptors was also surveyed utilizing naloxone in tail immersion and hot plate models, investigating the involvement of opioid receptors. The synthesized compounds could be used as alternative analgesic agents subjected to further evaluation in other animal models to confirm the observed biological potential.


Assuntos
Extratos Vegetais , Bases de Schiff , Analgésicos/uso terapêutico , Animais , Dor/tratamento farmacológico , Extratos Vegetais/farmacologia , Receptores Opioides , Bases de Schiff/farmacologia
3.
Front Pharmacol ; 13: 874914, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35924049

RESUMO

Polycystic ovary syndrome (PCOS) is a very common, complex, and heterogeneous endocrine disorder of women that involves a combination of environmental and genetic factors. PCOS affects women of growing age particularly at the early to late reproductive stage (15-35 years). Currently, PCOS affects 1 in every 10 women worldwide. It is characterized majorly by a raised level of androgens such as testosterone and a large number of ovarian cysts (more than 10) that cause anovulation, infertility, and irregular menstrual cycle. PCOS is also related to other endocrine and metabolic abnormalities, such as obesity, hirsutism, acne, diabetes, insulin resistance, and glucose impairment. PCOS can be treated with allopathic, ayurvedic, and natural or herbal medications along with lifestyle modifications. Herbal medicines remained in demand for numerous reasons such as high cost and side effects associated with the use of allopathic medicine and our traditional norms, which have helped humans to use more herbal products for their health benefits. Estrogenic and nonestrogenic phytochemicals present in various plant species such as Glycyrrhiza glabra L. [Fabaceae], Aloe vera (L.) Burm. f. [Asphodelaceae], Silybum marianum (L.). Gaertn. [Asteraceae], Serenoa repens (W.Bartram) Small [Arecaceae], Actaea racemosa L. [Ranunculaceae], and Angelica sinensis (Oliv.) Diels [Apiaceae] are effective and harmless. Herbal medicines are found to be cost-effective, efficacious, and a highly esteemed source of management/treatment for PCOS than allopathic medicines. In this literature review, diagnosis, signs, and symptoms of PCOS; causes of hormonal imbalance; and risk factors associated with PCOS and their management are discussed briefly, and the focus was to find out the role of herbal remedies in PCOS management.

4.
Brain Sci ; 12(7)2022 Jul 07.
Artigo em Inglês | MEDLINE | ID: mdl-35884701

RESUMO

Salvia moorcroftiana is medicinally used in various parts of the world to treat a number of diseases. In the literature, the antiamnesic activity of this plant has not yet been reported. Therefore, the current study was aimed at evaluating the in vivo antiamnesic (scopolamine-induced) potential of Salvia moorcroftiana. The major phytochemical groups such as total phenolic (TPC), total tannin (TTC), and total flavonoid content (TFC) in methanolic extract (SlMo-Crd) and subsequent fractions of Salvia moorcroftiana were quantified using standard methods. The in vitro anticholinesterase (against butyryl cholinesterase; BChE and acetylcholinesterase; AChE) and antioxidant (against 2,2-diphenyl-1-picrylhydrazyl; DPPH and 2,2'-Azino-bis (3-ethylbenzothiazoline-6-sulfonic acid); ABTS free radicals) potentials of crude (SIMO-Crd) extract and fractions (hexane; SlMo-Hex, chloroform; SlMo-Chl, ethyl acetate; SlMo-Et) were also determined. The SlMo-Crd at doses of 100 and 200 mg/kg body weight compared to fractions of 75 and 150 mg/kg body weight (which were 1/10th of the highest dose tested in acute toxicity tests) were evaluated for their memory enhancement and learning behavior in normal and scopolamine-induced mental dysfunction in mice using behavioral memory tests such as the Y-maze test and novel object recognition test (NORT). Moreover, the samples were further evaluated for acetylcholine contents and biochemical markers such as MDA (malondialdehyde), SOD (superoxide dismutase), CAT (catalase), and GSH (glutathione peroxidase) levels. The maximum TPC with a value of 114.81 ± 1.15 mg GAE/g, TTC with a value of 106.79 ± 1.07 mg GAE/g, and TFC with a value of 194.29 ± 0.83 mg RE/g were recorded for the SlMo-Chl fraction. Against the DPPH free radical, the methanolic extract exhibited an IC50 value of 95.29 ± 1.06 µg/mL whereas, among the fractions, the best activity was observed for the SlMo-Chl fraction with an IC50 of 75.02 ± 0.91 µg/mL, followed by SlMoS-Et with an IC50 value of 88.71 ± 0.87 µg/mL. Among the extracts, the SlMo-Chl and SlMo-Et fractions inverted the amnesic effects of scopolamine in mice effectively. Additionally, the SlMo-Chl and SIMO-Et fractions considerably enhanced the percent spontaneous alteration performance in the Y-maze test with values of 65.18 ± 2.61/69.51 ± 2.71 and 54.92 ± 2.49/60.41 ± 2.69, respectively, for the tested doses. The discrimination index (DI) in experimental mice was considerably enhanced by the SlMo-Chl in the NORT with values of 59.81 ± 1.21/61.22 ± 1.31% DI correspondingly for the tested doses, as mentioned above, followed by the SlMo-Et extract. The selected plant in the form of extracts ameliorated the effects of amnesia in mice and could, therefore, be used as a therapy for amnesia; however, this is subject to further exploration in other animal models and the isolation of the responsible compounds.

5.
Molecules ; 27(11)2022 May 30.
Artigo em Inglês | MEDLINE | ID: mdl-35684463

RESUMO

Biologically synthesized silver nanoparticles are emerging as attractive alternatives to chemical pesticides due to the ease of their synthesis, safety and antimicrobial activities in lower possible concentrations. In the present study, we have synthesized silver nanoparticles (AgNPs) using the aqueous extract of the medicinal plant Euphorbia wallichii and tested them against the plant pathogenic bacterium Xanthomonas axonopodis, the causative agent of citrus canker, via an in vitro experiment. The synthesized silver nanoparticles were characterized by techniques such as UV-Vis spectroscopy, Fourier transform infrared spectroscopy, energy-dispersive X-ray spectroscopy, X-ray diffraction analysis and transmission electron microscopy. Moreover, the plant species were investigated for phenolics, flavonoids and antioxidant activity. The antioxidant potential of the extract was determined against a DPPH radical. The extract was also evaluated for phenolic compounds using the HPLC technique. The results confirmed the synthesis of centered cubic, spherical-shaped and crystalline nanoparticles by employing standard characterization techniques. A qualitative and quantitative phytochemical analysis revealed the presence of phenolics (41.52 mg GAE/g), flavonoids (14.2 mg QE/g) and other metabolites of medicinal importance. Different concentrations (1000 µg/mL to 15.62 µg/mL-2 fold dilutions) of AgNPs and plant extract (PE) alone, and both in combination (AgNPs-PE), exhibited a differential inhibition of X. axanopodis in a high throughput antibacterial assay. Overall, AgNPs-PE was superior in terms of displaying significant antibacterial activity, followed by AgNPs alone. An appreciable antioxidant potential was recorded as well. The observed antibacterial and antioxidant potential may be attributed to eight phenolic compounds identified in the extract. The Euphorbia wallichii leaf-extract-induced synthesized AgNPs exhibited strong antibacterial activity against X. axanopodis, which could be exploited as effective alternative preparations against citrus canker in planta in a controlled environment. In addition, as a good source of phenolic compounds, the plant could be further exploited for potent antioxidants.


Assuntos
Citrus , Euphorbia , Nanopartículas Metálicas , Antibacterianos/química , Antibacterianos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Flavonoides , Nanopartículas Metálicas/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Prata/química , Espectroscopia de Infravermelho com Transformada de Fourier , Difração de Raios X
6.
Molecules ; 27(11)2022 May 30.
Artigo em Inglês | MEDLINE | ID: mdl-35684464

RESUMO

Anabasis articulata is medicinally used to treat various diseases. In this study, A. articulata was initially subjected to extraction, and the resultant extracts were then evaluated for their antimicrobial, antioxidant, and antidiabetic potentials. After obtaining the methanolic extract, it was subjected to a silica gel column for separation, and fractions were collected at equal intervals. Out of the obtained fractions (most rich in bioactive compounds confirmed through HPLC), designated as A, B, C, and D as well hexane fraction, were subjected to GC-MS analysis, and a number of valuable bioactive compounds were identified from the chromatograms. The preliminary phytochemical tests were positive for the extracts where fraction A exhibited the highest total phenolic and flavonoid contents. The hexane fraction as antimicrobial agent was the most potent, followed by the crude extract, fraction A, and fraction D. DPPH and ABTS assays were used to estimate the free radical scavenging potential of the extracts. Fraction C was found to contain potent inhibitors of both the tested radicals, followed by fraction D. The potential antidiabetic extracts were determined using α-glucosidase and amylase as probe enzymes. The former was inhibited by crude extract, hexane, and A, B, C and D fractions to the extent of 85.32 ± 0.20, 61.14 ± 0.49, 62.15 ± 0.84, 78.51 ± 0.45, 72.57 ± 0.92 and 70.61 ± 0.91%, respectively, at the highest tested concentration of 1000 µg/mL with their IC50 values 32, 180, 200, 60, 120 and 140 µg/mL correspondingly, whereas α-amylase was inhibited to the extent of 83.98 ± 0.21, 58.14 ± 0.75, 59.34 ± 0.89, 81.32 ± 0.09, 74.52 ± 0.13 and 72.51 ± 0.02% (IC50 values; 34, 220, 240, 58, 180, and 200 µg/mL, respectively). The observed biological potentials might be due to high phenolic and flavonoid content as detected in the extracts. The A. articulata might thus be considered an efficient therapeutic candidate and could further be investigated for other biological potentials along with the isolation of pure responsible ingredients.


Assuntos
Antioxidantes , Chenopodiaceae , Antibacterianos/farmacologia , Antioxidantes/química , Flavonoides/química , Hexanos , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Fenóis/análise , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química
7.
Molecules ; 27(8)2022 Apr 08.
Artigo em Inglês | MEDLINE | ID: mdl-35458597

RESUMO

Different species of Artemisia have been reported to have therapeutic potential in treating various health disorders, including diabetes and memory dysfunction. The present study was planned to evaluate the effects of Artemisia macrocephala Jacquem crude extract and its subfractions as antiamnesic agents in streptozotocin-induced (STZ) diabetic mice. The in vivo behavioral studies were performed using the Y Maze test and novel object recognition test (NORT) test at doses of 100 and 200 mg/kg of crude extract and 75 and 150 mg/kg of fractions. The in vitro and ex vivo anticholinesterase activities, along with biochemical parameters (superoxide dismutase, catalase, glutathione and lipid peroxidation) in the brain, were evaluated. Blood glucose levels were monitored with a glucometer; crude extract and fractions reduced the glucose level considerably, with some differences in the extent of their efficacies. The crude extract and fractions demonstrated significant inhibitory activity against cholinesterases (AChE and BuChE) in vitro. Crude, chloroform and ethyl acetate extract were found to be more potent than the other fractions, with IC50 of Crd-Am = 116.36 ± 1.48 and 240.52 ± 1.35 µg/mL, Chl-Am = 52.68 ± 1.09 and 57.45 ± 1.39 µg/mL and Et-Am = 75.19 ± 1.02 and 116.58 ± 1.09 µg/mL, respectively. Oxidative stress biomarkers like superoxide dismutase, catalase and glutathione levels were elevated, whereas MDA levels were reduced by crude extract and all fractions with little difference in their respective values. The Y-maze test and novel object recognition test demonstrated declines in memory impairment in groups (n = 6) treated with crude extract and fractions as compared to STZ diabetic (amnesic) group. The most active fraction, Chl-Am, was also subjected to isolation of bioactive compounds; three compounds were obtained in pure state and designated as AB-I, AB-II and AB-III. Overall, the results of the study showed that Artemisia macrocephala Jacquem enhanced the memory impairment associated with diabetes, elevated acetylcholine levels and ameliorated oxidative stress. Further studies are needed to explore the beneficial role of the secondary metabolites isolated in the present study as memory enhancers. Toxicological aspects of the extracts are also important and need to be evaluated in other animal models.


Assuntos
Artemisia , Diabetes Mellitus Experimental , Transtornos da Memória , Estresse Oxidativo , Animais , Antioxidantes/farmacologia , Artemisia/química , Encéfalo/metabolismo , Catalase/metabolismo , Diabetes Mellitus Experimental/metabolismo , Glutationa/metabolismo , Transtornos da Memória/induzido quimicamente , Camundongos , Extratos Vegetais/uso terapêutico , Estreptozocina/farmacologia , Superóxido Dismutase/metabolismo
8.
Pharmaceuticals (Basel) ; 15(2)2022 Feb 11.
Artigo em Inglês | MEDLINE | ID: mdl-35215329

RESUMO

The application of plant extracts or plant-derived compounds in the green synthesis of metal nanoparticles (NPs) was researched. Determining the exact metabolite implicated in the formation of NPs would necessitate comprehensive investigations. Copper nanoparticles (CuNPs) are gaining a lot of attention because of their unique properties and effectiveness against a wide range of bacteria and fungi, as well as their potential for usage in catalytic, optical, electrical, and microelectronics applications. In the course of this study, we aimed to formulate CuNPs utilizing pure tamarixinin A (TA) ellagitannin isolated from Tamarix aphylla galls. The main particle size of the formed CuNPs was 44 ± 1.7 nm with zeta potential equal to -23.7 mV, which emphasize the stability of the CuNPs. The X-ray diffraction spectroscopy showed a typical centered cubic crystalline structure phase of copper. Scanning electron microscopy images were found to be relatively spherical and homogeneous in shape. The antimicrobial properties of TA, as well as its mediated CuNPs, have been evaluated through well diffusion assays against four bacterial, Bacillus subtilis NCTC 10400, Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, and Pseudomonas aeruginosa ATCC 27853, and two fungal, Candida albicans and Aspergillus flavus, strains. The distinctive antimicrobial activities were noted against the fungal strains and the Gram-negative bacterial strains P. aeruginosa ATCC 27853, and E. coli ATCC 25922. In conclusion, CuNPs mediated by TA can be applied for combating a wide range of bacterial and fungal species especially C. albicans, Asp. flavus, and P. aeruginosa in a variety of fields.

9.
Nanomaterials (Basel) ; 12(1)2022 01 04.
Artigo em Inglês | MEDLINE | ID: mdl-35010119

RESUMO

Colorectal cancer (CRC) is a serious disease that affects millions of people throughout the world, despite considerable advances in therapy. The formation of colorectal adenomas and invasive adenocarcinomas is the consequence of a succession of genetic and epigenetic changes in the normal colonic epithelium. Genetic and epigenetic processes associated with the onset, development, and metastasis of sporadic CRC have been studied in depth, resulting in identifying biomarkers that might be used to predict behaviour and prognosis beyond staging and influence therapeutic options. A novel biomarker, or a group of biomarkers, must be discovered in order to build an accurate and clinically useful test that may be used as an alternative to conventional methods for the early detection of CRC and to identify prospective new therapeutic intervention targets. To minimise the mortality burden of colorectal cancer, new screening methods with higher accuracy and nano-based diagnostic precision are needed. Cytotoxic medication has negative side effects and is restricted by medication resistance. One of the most promising cancer treatment techniques is the use of nano-based carrier system as a medication delivery mechanism. To deliver cytotoxic medicines, targeted nanoparticles might take advantage of differently expressed molecules on the surface of cancer cells. The use of different compounds as ligands on the surface of nanoparticles to interact with cancer cells, enabling the efficient delivery of antitumor medicines. Formulations based on nanoparticles might aid in early cancer diagnosis and help to overcome the limitations of traditional treatments, including low water solubility, nonspecific biodistribution, and restricted bioavailability. This article addresses about the molecular pathogenesis of CRC and highlights about biomarkers. It also provides conceptual knowledge of nanotechnology-based diagnostic techniques and therapeutic approaches for malignant colorectal cancer.

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