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1.
Saudi Pharm J ; 32(2): 101928, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38261905

RESUMO

The lost dopaminergic neurons in the brain prevent mobility in Parkinson's disease (PD). It is impossible to stop the disease's progress by means of symptoms management. Research focuses on oxidative stress, mitochondrial dysfunction, and neuronal degeneration. Exploration of potential neuroprotective drugs against prosurvival B-cell lymphoma 2 (Bcl-2) protein is ongoing. An investigable cause behind PD, as well as preventive measures, could be discovered considering the association between such behavioural manifestations (cataleptic behaviours) and PD. The compound Afzelin, known to guard the nervous system, was chosen for this study. The study was done on rats divided into six different groups. First, there was a control group. The other group was treated with Reserpine (RES) (1 mg/kg). The third group received RES (1 mg/kg) and levodopa (30 mg/kg). The remaining three groups were given RES (1 mg/kg) in conjunction with Afzelin at the following doses: 5 mg/kg, 10 mg/kg, and 20 mg/kg. Cataleptic behavior and mobility in rats was assessed using the rotarod, open field, and modified forced-swim tests. thiobarbituric acid reactive substances (TBARS), nitric oxide (NO), biogenic amines, and Bcl-2 level in rat tissue homogenates were considered. According to the study's findings, the rats treated through co-administration of RES and Afzelin improved significantly in their cataleptic behaviours and locomotor activity. In addition, administering Afzelin itself caused Bcl-2 expression, which could have some neuroprotection properties. This study provides meaningful information on the effectiveness of Afzelin in handling catalepsy and other degenerative neurologic disorders. As a result, other studies need to be conducted to establish the reasons behind the reactions and determine the long-term effects of Afzelin on these conditions.

2.
Artigo em Inglês | MEDLINE | ID: mdl-37123083

RESUMO

Background: Quercetin hastraditionally been used in various oxidative and urinary tract dysfunctions. Thecurrent project is consequently set to evaluate the defensive efficacy ofQuercetin against potassium bromate (KBrO3) induced testiculartissue oxidative dysfunctions through biochemical, hormonal, and genotoxicmarkers. Methods: To observe theprotective efficacy of Quercetin against urinogenital oxidative dysfunction inrats, thirty six albino male rats were divided into six groups. Protectiveefficacies of Quercetin were checked on reproductive hormonal levels,antioxidant enzyme activities, lipids peroxidation (LP), and DNA damages. Results: Potassium bromate exposure in experimentalanimals caused a reduction in the activities of antioxidant enzymes and disturbedhormonal secretions while enhancing the peroxidation of lipids andfragmentations of DNA. Cotreatment of Quercetin considerably (P<0.01)reversed these abnormalities with admiration to levels of hormones, antioxidantenzymes activities, and peroxidations of lipids secure to those seen inuntreated rats. (P < 0.01). Conclusion: The findings of the current project revealedthat various doses of Quercetin are able to keep the testicular organ fromabnormal free radical dysfunctions. These improvements might be due to theantioxidant ability of polyphenolic bioactive constituent, i.e., Quercetin.

3.
Biomedicines ; 11(4)2023 04 18.
Artigo em Inglês | MEDLINE | ID: mdl-37189822

RESUMO

Diabetic polyneuropathy is characterized by structural abnormalities, oxidative stress, and neuroinflammation. The current study aimed to determine the antinociceptive effects of isoeugenol and eugenol and their combinations in neuropathic pain resulting from streptozotocin (STZ)-induced diabetes and neuroinflammation. Female SD rats were categorized into normal control, diabetic control, and treatment groups. On the 28th day and 45th day, behavioral studies (allodynia and hyperalgesia) were performed to analyze the development and protection of diabetic polyneuropathy. The levels of inflammatory and oxidative mediators, such as superoxide dismutase (SOD), tumor necrosis factor-α (TNF-α), catalase, reduced glutathione, and thiobarbituric acid reactive substances (TBARS), were estimated. In addition, the level of nerve growth factor (NGF) was estimated at the end of the study in different groups. The anti-NGF treatment decreased its upregulation in the dorsal root ganglion significantly. The results showed that isoeugenol, eugenol, and their combination have therapeutic potential against neuronal and oxidative damage induced by diabetes. In particular, both compounds significantly affected behavioral function in treated rats and showed neuroprotection against diabetic neuropathy, and their combination had synergistic effects.

4.
Molecules ; 28(10)2023 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-37241830

RESUMO

Myocardial infarction (MI) continues to be an important issue in healthcare systems worldwide, leading to high rates of morbidity and mortality. Despite ongoing efforts towards the development of preventive measures and treatments, addressing the challenges posed by MI remains difficult both in developed and developing countries. However, researchers recently investigated the potential cardioprotective effects of taraxerol utilizing an isoproterenol (ISO)-induced cardiotoxicity model among Sprague Dawley rats. Specifically, subcutaneous tissue injections consisting of 5.25 mg/kg or 8.5 mg/kg ISO were administered over two consecutive days as stimuli to induce cardiac injury. To investigate the possibility of preventing damage caused by ISO-induced cardiotoxicity by taraxerol treatment, five groups were formed: a normal control group (1% Tween 80), an ISO control group, an amlodipine group administered 5 mg/kg/day, and various doses of taraxerol. The study results showed that treatment significantly reduced cardiac marker enzymes. Additionally, pretreatment with taraxerol increased myocardial activity in SOD and GPx, leading to significant reductions in serum CK-MB levels along with MDA, TNF-α, and IL-6. Further histopathological analysis supported these observations, as treated animals had less cellular infiltration compared to untreated ones. These multifaceted findings suggest that oral administration of taraxerol could potentially protect hearts from ISO-caused damage by increasing endogenous antioxidant concentrations while decreasing pro-inflammatory cytokines.


Assuntos
Cardiotoxicidade , Infarto do Miocárdio , Ratos , Animais , Isoproterenol/toxicidade , Isoproterenol/metabolismo , Cardiotoxicidade/tratamento farmacológico , Cardiotoxicidade/etiologia , Cardiotoxicidade/metabolismo , Mediadores da Inflamação/metabolismo , Ratos Sprague-Dawley , Miocárdio/metabolismo , Infarto do Miocárdio/tratamento farmacológico , Antioxidantes/metabolismo , Modelos Animais de Doenças , Estresse Oxidativo
5.
Gels ; 9(3)2023 Feb 24.
Artigo em Inglês | MEDLINE | ID: mdl-36975627

RESUMO

Mangiferin is a herbal drug that has proven anticancer potential. Owing to its lower aqueous solubility and poor oral bioavailability, the full pharmacological potential of this bioactive drug has not fully been explored. In the present study, phospholipid-based microemulsion systems were developed to bypass oral delivery. The globule size of the developed nanocarriers was less than 150 nm and the drug entrapment was >75% with a drug loading ~25%. The developed system offered a controlled release pattern following the Fickian drug release. This enhanced mangiferin's in vitro anticancer activity by four-fold, the cellular uptake was observed to be improved by three-fold on the MCF-7 cells. Ex vivo dermatokinetic studies showed substantial topical bioavailability with a prolonged residence time. The findings provide a simple technique to administer mangiferin via a topical route promising a safer, topically bioavailable and effective treatment option for breast cancer. Such scalable carriers with immense topical delivery potential may provide a better option for present-day topical products of a conventional nature.

6.
Molecules ; 28(3)2023 Jan 17.
Artigo em Inglês | MEDLINE | ID: mdl-36770602

RESUMO

The study was conducted to determine whether corosolic acid could protect the myocardium of diabetic rats from damage caused by isoproterenol (ISO) and, if so, how peroxisome proliferator-activated receptor gamma (PPAR-γ) activation might contribute into this protection. Diabetes in the rats was induced by streptozotocin (STZ), and it was divided into four groups: the diabetic control group, diabetic rats treated with corosolic acid, diabetic rats treated with GW9662, and diabetic rats treated with corosolic acid plus GW9662. The study was carried out for 28 days. The diabetic control and ISO control groups showed a decrease in mean arterial pressure (MAP) and diastolic arterial pressure (DAP) and an increase in systolic arterial pressure (SAP). The rat myocardium was activated by corosolic acid treatment, which elevated PPAR-γ expression. A histopathological analysis showed a significant reduction in myocardial damage by reducing myonecrosis and edema. It was found that myocardial levels of CK-MB and LDH levels were significantly increased after treatment with corosolic acid. By decreasing lipid peroxidation and increasing endogenous antioxidant levels, corosolic acid therapy showed a significant improvement over the ISO diabetic group. In conclusion, our results prove that corosolic acid can ameliorate ISO-induced acute myocardial injury in rats. Based on these results, corosolic acid seems to be a viable new target for the treatment of cardiovascular diseases and other diseases of a similar nature.


Assuntos
Diabetes Mellitus Experimental , PPAR gama , Ratos , Animais , PPAR gama/metabolismo , Ratos Wistar , Diabetes Mellitus Experimental/metabolismo , Miocárdio/metabolismo , Isoproterenol/metabolismo
7.
J Cosmet Dermatol ; 22(5): 1613-1627, 2023 May.
Artigo em Inglês | MEDLINE | ID: mdl-36606381

RESUMO

BACKGROUND: Numerous studies have shown that various products of Citrus sinensis, for example, crude extracts, essential oil, and purified components, possess anti-acne properties. However, the development of chlorogenic acid-functionalized silver nanoparticles of C. sinensis in gel matrix aiding QbD design has not been evaluated for acne treatment. AIM: In this study, we have developed chlorogenic acid-functionalized silver nanoparticles of C. sinensis in a gel matrix employing a QbD approach for acne treatment. MATERIAL AND METHOD: Citrus sinensis extract-loaded silver nanoparticles were functionalized with chlorogenic acid, which acted as a bio-reducing agent and further improved anti-acne properties. The developed formulation was optimized via Box-Behnken Design. The formulation morphology was evaluated by transmission electron microscopy (TEM). The release profile of C. sinensis extract formulation was assessed by an in vitro release study and confocal laser scanning microscopy (CLSM). Moreover, the characterization study of the gel was performed that included an evaluation of the extrudability and spreadability of the developed gel. Furthermore, the anti-oxidant efficacy of AgN-CA formulation was validated using the DPPH test. RESULTS: The results showed a particle size of 71.78 nm, a polydispersity index of 0.297, a zeta potential of -36.12 mV, and an entrapment efficiency of 79.42% ± 6.79%. The results also indicated a uniform particle size. The release profile of C. sinensis extract revealed that 73.95% of the drug was released, whereas CLSM pictures of mice skin evidently demonstrated that the rhodamine B-treated AgN-CA gel penetrated much more extensively in comparison to the control. Furthermore, the anti-oxidant efficacy of AgN-CA formulation was validated using the DPPH test. Moreover, the characterization study of the developed gel, including its extrudability and spreadability, was found to be 16.02 ± 3.21 g and 30.73 ± 5.94 g cm/s, respectively. Also, texture analysis findings revealed that AgN-CA gel had firmness, consistency, cohesiveness, and viscosity index of 159.69 g, 634.95 g s, -116.33 g, and -501.80 g s, respectively, indicating that the AgN-CA gel was stable. CONCLUSION: The current study showed that AgN-CA is an effective drug carrier system for the topical administration of C. sinensis extract for the treatment of acne.


Assuntos
Acne Vulgar , Citrus sinensis , Nanopartículas Metálicas , Nanopartículas , Camundongos , Animais , Ácido Clorogênico/uso terapêutico , Prata , Nanopartículas Metálicas/química , Antioxidantes/uso terapêutico , Micro-Ondas , Acne Vulgar/tratamento farmacológico , Tamanho da Partícula , Nanopartículas/química
8.
Molecules ; 27(19)2022 Oct 07.
Artigo em Inglês | MEDLINE | ID: mdl-36235206

RESUMO

Background: Due to the high expense, less effectiveness and more side effects of available synthetic medicine, the researchers and communities are focusing on phyto-based natural bioactive compounds, which are considered safer for the treatment of syndromes and chronic diseases. Aim: The current project was aimed to determine the phytochemicals constituents available in the aerial parts of methanol extract of Carduus edelbergii via GC-MS, fabrication of AuNPs mediated with the mentioned extract; characterization and evaluation of antimicrobial, antioxidant and antidiabetic potency of the synthesized AuNPs. Methods: Confirmation of green synthesis of AuNPs, functional groups responsible for the reduction in Au+, size and crystallinity, morphology and quantity of gold (Au) were carried out by Ultraviolet-Visible (UV-Vis) spectroscopy, Transform Infrared (FTIR) spectroscopy, Scanning Electron Microscopy (SEM), X-ray Diffraction (XRD) and dispersive X-ray (EDX), respectively, whereas in vitro antioxidant characteristics were assessed by DPPH and ABTS assays. Wistar albino rats were used to test the anti-diabetic properties of the methanol extract and AuNPs. Results: GC-MS revealed that the diluted methanol extract of Carduus edelbergii consists of about 19 chemical constituents. Among the identified compounds, the 13-Docosenoic acid, methyl ester, (Z)­has the highest concentration (38.16%), followed by 9-Octadecenoic acid, methyl ester, (E)­(15.72%) and n-Hexadecanoic acid (15.07%). Methanol extract and its fabricated nanoparticles showed significant antioxidant and antimicrobial activities. In vivo antidiabetic study revealed a noteworthy (p < 0.05) decline in body weight and HDL and elevated concentration of blood glucose, bilirubin, creatinine, urea, triglyceride, VLDL, LDL, ALP, ALT and AST in diabetic control. The said changes were recovered significantly (p < 0.05) by treatment of diabetic rats with methanol extract (150 and 300 mg/Kg BW) and AuNPs of Carduus edelbergii (5 and 10 mg/Kg BW). Conclusion: The green synthesized AuNPs exhibit significant antioxidant, antimicrobial and antidiabetic characteristics.


Assuntos
Carduus , Diabetes Mellitus Experimental , Nanopartículas Metálicas , Animais , Antibacterianos/química , Antibacterianos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Bilirrubina , Glicemia , Creatinina , Diabetes Mellitus Experimental/tratamento farmacológico , Ésteres , Ouro/química , Química Verde/métodos , Hipoglicemiantes/farmacologia , Nanopartículas Metálicas/química , Metanol , Ácido Oleico , Ácido Palmítico , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Ratos , Ratos Wistar , Espectroscopia de Infravermelho com Transformada de Fourier , Triglicerídeos , Ureia
9.
Healthcare (Basel) ; 10(9)2022 Sep 13.
Artigo em Inglês | MEDLINE | ID: mdl-36141370

RESUMO

Antibiotics have completely transformed medical practice by enabling the treatment of infections that were formerly fatal. However, misuse of antibiotics encourages the formation and spread of germs that are resistant to therapy, hastening the emergence of bacterial resistance. This was a retrospective study that aimed to gather information about the variation in bacterial susceptibility of various patient age groups in a public hospital in Qassim, Saudi Arabia from January 2020 to December 2021. The study included reviewing bacterial susceptibility results that were collected from the laboratory department of the hospital. Four thousand seven hundred and sixty-two isolates were collected. The age of 46.41% of the patients was more than 63 years and the age of 28.96% of the patients was less than 48 years. The most prevalent bacteria were Staphylococcus aureus, Escherichia coli, and Klebsiella pneumoniae. The resistance of gram-positive and gram-negative bacteria to different antibiotics in the elderly group was generally higher than the resistance rates in younger patients. For example, in patients less than 48 years old, the resistance of Staphylococcus haemolyticus to clindamycin (53.3%), ampicillin (91.4%), ciprofloxacin (68.2%), erythromycin (86.1%), and penicillin (93.18%) was high. In patients aged more than 63 years, Staphylococcus haemolyticus was highly resistant to sulfamethoxazole (54.8%), clindamycin (63.9%), ampicillin (98.1%), ciprofloxacin (79.1%), erythromycin (93.2%), gentamicin (63.6%), and penicillin (98.7%). Before prescribing the antibiotics, it is important to assess the microbes that patients have and to be aware of the bacterial isolates' patterns of antibiotic susceptibility among patients of various age groups.

10.
Pharmaceuticals (Basel) ; 15(9)2022 Aug 31.
Artigo em Inglês | MEDLINE | ID: mdl-36145310

RESUMO

Opophytum forsskalii (O. forsskalii) is a desert plant that belongs to the Aizoaceae family. Although it is a natural food source for Bedouin tribes in northern Saudi Arabia, there is little information on its active metabolites. Therefore, the secondary metabolites of the hydroalcoholic extract from the leaves of this species were analyzed by liquid chromatography-mass chromatography (LC-MS). LC-MS identified a total of 30 secondary metabolites. These compounds represented two main categories among sixteen classes. Among them, flavonoids represented the largest proportion with eleven metabolites while fatty acids provided seven compounds. In addition, the extract was evaluated for its gastroprotective effect against gastric lesions induced by different models, such as indomethacin, stress, and necrotizing agents (80% ethanol, 0.2 mol/L NaOH, and 25% NaCl), in rats. For each method, group 1 was used as the control group while groups 2 and 3 received the leaf extract at doses of 200 and 400 mg/kg, respectively. The ulcer index (UI) and intraluminal bleeding score (IBS) were measured for each method. In addition, gastric tissue from the ethanol method was used for the analysis of nonprotein sulfhydrates (NP-SH), malondialdehyde (MDA), total protein (TP), and histopathologic evaluation. Pretreatment with O. forsskalii significantly decreased UI (p < 0.01) and IBS (p < 0.01) at 400 mg/kg. Pretreatment with O. forsskalii significantly improved total protein levels (p < 0.01) and NP-SH (p < 0.001) compared to the ethanol ulcer groups. MDA levels increased from 0.5 to 5.8 nmol/g in the normal groups compared to the ethanol groups and decreased to 2.34 nmol/g in the O. forsskalii pretreatment. In addition to the gastroprotective markers, histopathological examination of gastric tissue confirmed the gastroprotective potential of O. forsskalii extract against ethanol.

11.
Chem Biodivers ; 19(8): e202200499, 2022 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-35797203

RESUMO

Nine xanthone derivatives (1-9) were isolated from the roots of Polygala azizsancarii, which is a narrow endemic species for the flora of Türkiye. Based on all of the evidence, the structures of 1-9 were established as two previously undescribed xanthone O-glucosides, 3-O-ß-D-glucopyranosyloxy-1,6-dihydroxy-2,5,7-trimethoxyxanthone (1), 3-O-ß-D-glucopyranosyloxy-1,6-dihydroxy-2,7-dimethoxyxanthone (2), and seven previously described xanthones, 1,3,6-trihydroxy-2,5,7-trimethoxyxanthone (3), 1,3,6-trihydroxy-2,7-dimethoxyxanthone (4), 1,2,3,4,7-pentamethoxyxanthone (5), 1,3-dihydroxy-2,5,6,7-tetramethoxyxanthone (6), 1,3-dihydroxy-4,7-dimethoxyxanthone (7), 1,7-dihydroxy-3-methoxyxanthone (8), and 1,7-dihydroxy-2,3-methylenedioxyxanthone (9). The structures of the compounds were determined by spectroscopic methods, including 1D-NMR (1 H-NMR, 13 C-NMR, DEPT-135), 2D-NMR (COSY, NOESY, HSQC, HMBC, INADEQUATE), and HR-MS. The solid-state structures of 1-4, including the absolute configurations of the stereogenic carbons of the sugar moiety in 1 and 2, were established by X-ray crystal-structure analyses. For the newly described compounds, the trivial names sancarosides A (1) and B (2) are proposed.


Assuntos
Polygala , Xantonas , Glucosídeos , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Raízes de Plantas/química , Xantonas/química
12.
Nanomaterials (Basel) ; 12(5)2022 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-35269321

RESUMO

Background: Type-2 diabetes mellitus (T2DM) is a non-communicable, life-threatening syndrome that is present all over the world. The use of eco-friendly, cost-effective and green synthesised nanoparticles (NPs) as a medicinal therapy in the treatment of T2DM is an attractive option. Aim: The present study aimed to evaluate the anti-diabetic potential of the phyto-synthesised silver nanoparticles (AgNPs) obtained from Phagnalon niveum plant methanolic extract. Methods: The green synthesised AgNPs made from Phagnalon niveum plant methanolic extract were analysed by Ultraviolet-Visible (UV-Vis) spectroscopy, and the functional groups involved in the reduction of the silver ions (Ag+) were characterised by Fourier Transform Infrared (FTIR) spectroscopy. The size and crystallinity were assessed via X-ray Diffraction (XRD). The morphology of AgNPs was confirmed using Scanning Electron Microscopy (SEM). The amount of silver (Ag) was estimated via energy dispersive X-ray (EDX) analysis. An intraperitoneal injection of 200 mg alloxan per kg albino Wistar rats' body weight, at eight weeks old and weighing 140-150 g, was used to induce diabetes mellitus (N = 25; n = 5/group). Group C: untreated normal control rats that only received distilled water, group DAC: diabetic control rats that received alloxan 200 mg/Kg body weight, DG: diabetic rats treated with glibenclamide at 0.5 mg/kg body weight, DE: diabetic rats that received methanolic P. niveum extract at 10 mg/Kg body weight, and DAgNPs: diabetic rates that received AgNPs synthesised from P. niveum at 10 mg/kg body weight. The blood glucose levels were monitored on days 0, 7, and 14, while lipid, liver, and kidney profiles were checked after dissection at the end of treatment (day 21). On the final day of the period study (day 21), an oral glucose tolerance test was carried out by administering orally 2 g/kg body weight of glucose to the respective groups, and the blood glucose level was checked. A fasting glucose level was measured using a glucometer. Urine samples were collected from each animal and analysed using lab-made assay kits for glucose, bilirubin, pH, leukocytes, and nitrite, among other factors. For statistical analyses, a one-way ANOVA and Dunnett's test were applied. Results: The green-mediated synthesis of AgNPs using P. niveum methanolic extract produced spherical and mono-dispersed NPs with a size ranging from 12 to 28 nm (average: 21 nm). Importantly, a significant reduction of blood glucose levels and an increase in body weight, as well as a remarkable improvement in lipid, liver, and kidney profiles, were noticed. Conclusions: The biosynthesised AgNPs significantly improved the abnormalities in body weight, urine, and serum levels, indicating that it is a promising anti-diabetic agent.

13.
Molecules ; 27(3)2022 Jan 21.
Artigo em Inglês | MEDLINE | ID: mdl-35163950

RESUMO

Polygala species are frequently used worldwide in the treatment of various diseases, such as inflammatory and autoimmune disorders as well as metabolic and neurodegenerative diseases, due to the large number of secondary metabolites they contain. The present study was performed on Polygala inexpectata, which is a narrow endemic species for the flora of Turkey, and resulted in the isolation of nine known compounds, 6,3'-disinapoyl-sucrose (1), 6-O-sinapoyl,3'-O-trimethoxy-cinnamoyl-sucrose (tenuifoliside C) (2), 3'-O-(O-methyl-feruloyl)-sucrose (3), 3'-O-(sinapoyl)-sucrose (4), 3'-O-trimethoxy-cinnamoyl-sucrose (glomeratose) (5), 3'-O-feruloyl-sucrose (sibiricose A5) (6), sinapyl alcohol 4-O-glucoside (syringin or eleutheroside B) (7), liriodendrin (8), and 7,4'-di-O-methylquercetin-3-O-ß-rutinoside (ombuin 3-O-rutinoside or ombuoside) (9). The structures of the compounds were determined by the spectroscopic methods including 1D-NMR (1H NMR, 13C NMR, DEPT-135), 2D-NMR (COSY, NOESY, HSQC, HMBC), and HRMS. The isolated compounds were shown in an in silico setting to be accommodated well within the inhibitor-binding pockets of myeloperoxidase and inducible nitric oxide synthase and anchored mainly through hydrogen-bonding interactions and π-effects. It is therefore plausible to suggest that the previously established anti-inflammatory properties of some Polygala-derived phytochemicals may be due, in part, to the modulation of pro-inflammatory enzyme activities.


Assuntos
Compostos Fitoquímicos/análise , Extratos Vegetais/farmacologia , Polygala/metabolismo , Anti-Inflamatórios/análise , Cromatografia Líquida de Alta Pressão/métodos , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Glucosídeos/isolamento & purificação , Glucosídeos/farmacologia , Simulação de Acoplamento Molecular , Estrutura Molecular , Fenilpropionatos/isolamento & purificação , Fenilpropionatos/farmacologia , Compostos Fitoquímicos/isolamento & purificação , Raízes de Plantas/química , Polygala/genética , Sacarose/isolamento & purificação , Sacarose/metabolismo , Turquia
14.
Molecules ; 27(3)2022 Jan 29.
Artigo em Inglês | MEDLINE | ID: mdl-35164196

RESUMO

The herbal plant Petroselinum crispum (P. crispum) (Mill) is commonly available around the world. In this study, the leaves of the herbal plant P. crispum were collected from the central region of Al-Kharj, Saudi Arabia, to explore their in vitro pharmacological activity. Essential oil from the leaves of P. crispum was isolated using the hydrodistillation method. The composition of P. crispum essential oil (PCEO) was determined using Gas chromatography-mass spectrometry (GC-MS). A total of 67 components were identified, representing approximately 96.02% of the total volatile composition. Myristicin was identified as the principal constituent (41.45%). The in vitro biological activity was assessed to evaluate the antioxidant, antimicrobial, and anti-inflammatory potential of PCEO. PCEO showed the highest antimicrobial activity against Candida albicans and Staphylococcus aureus among all the evaluated microbial species. In vitro anti-inflammatory evaluation using albumin and trypsin assays showed the excellent anti-inflammatory potential of PCEO compared to the standard drugs. An in silico study of the primary PCEO compound was conducted using online tools such as PASS, Swiss ADME, and Molecular docking. In silico PASS prediction results supported our in vitro findings. Swiss ADME revealed the drug likeness and safety properties of the major metabolites present in PCEO. Molecular docking results were obtained by studying the interaction of Myristicin with an antifungal (PDB: 1IYL and 3LD6), antibacterial (PDB: 1AJ6 and 1JIJ), antioxidant (PDB: 3NM8 and 1HD2), and anti-inflammatory (3N8Y and 3LN1) receptors supported the in vitro results. Therefore, PCEO or Myristicin might be valuable for developing anti-inflammatory and antimicrobial drugs.


Assuntos
Magnoliopsida/química , Folhas de Planta/química , Anti-Infecciosos/análise , Anti-Inflamatórios/farmacologia , Antifúngicos/farmacologia , Simulação por Computador , Técnicas In Vitro , Folhas de Planta/crescimento & desenvolvimento , Arábia Saudita
15.
Healthcare (Basel) ; 11(1)2022 Dec 26.
Artigo em Inglês | MEDLINE | ID: mdl-36611523

RESUMO

Healthcare-associated infections are widely considered one of the most common unfavorable outcomes of healthcare delivery. Ventilator-associated pneumonia, central line-associated bloodstream infections, and catheter-associated urinary tract infections are examples of healthcare-associated infections. The current study was a retrospective study conducted at a public hospital in Unaizah, Saudi Arabia, to investigate the frequency of healthcare-associated illnesses and adherence to healthcare-associated infection prevention techniques in the year 2021. Surgical site infections occurred at a rate of 0.1%. The average number of catheter-associated urinary tract infections per 1000 catheter days was 0.76. The average number of central line-associated bloodstream infections per 1000 central line days was 2.6. The rate of ventilator-associated pneumonia was 1.1 per 1000 ventilator days on average. The average number of infections caused by multidrug-resistant organisms per 1000 patient days was 2.8. Compliance rates were 94%, 100%, 99%, and 76% for ventilator-associated pneumonia, central line-associated bloodstream infections, catheter-associated urinary tract infections, and hand hygiene bundles, respectively. It is critical to participate in more educational events and workshops, particularly those that emphasize hand cleanliness and personal safety equipment.

16.
Braz. J. Pharm. Sci. (Online) ; 58: e18851, 2022. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1374568

RESUMO

Abstract Some plants of the genus Pulicaria have been used in traditional medicines for treating back pain and inflammation. They possess various bioactivities such as antipyretic, analgesic, and hepatoprotective. This study aimed to investigate the potential analgesic, antipyretic, anti- inflammatory, and hepatoprotective activities of Pulicaria crispa (P. crispa) extract (PCE). Analgesic activity was evaluated using the hot plate and acetic acid-induced writhing tests. Antipyretic and anti-inflammatory activities were evaluated using rectal temperature and carrageenan-induced hind paw edema methods, respectively. CCl4-intoxication was used for hepatoprotective activity. Also, liver histopathology was assessed. PCE, at 500 mg/kg, exhibited significant analgesic, antipyretic, and anti-inflammatory effects. The increased serum levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), gamma-glutamyl transferase (GGT), and bilirubin of CCl4-exposed rats reflects their liver injury. PCE significantly decreased the elevated liver markers. The hepatoprotective effect of PCE was confirmed, as it successfully reversed the altered levels of total protein, malondialdehyde (MDA), and non-protein sulfhydryls (NP-SH) in the liver tissues of CCl4-exposed rats. Histopathological studies confirmed the hepatoprotective nature of PCE. Pretreatment of rats with PCE reduced the severity of CCl4-induced liver damage. These findings concluded that PCE possesses analgesic, antipyretic, anti-inflammatory, and hepatoprotective activities.


Assuntos
Extratos Vegetais/análise , Asteraceae/classificação , Pulicaria/anatomia & histologia , Antipiréticos/classificação , Analgésicos/classificação
17.
Molecules ; 26(23)2021 Dec 04.
Artigo em Inglês | MEDLINE | ID: mdl-34885954

RESUMO

The aim of this study was to explore the composition and evaluate the in silico and in vitro antioxidants and antimicrobial and anti-inflammatory effects of Apium graveolens var. dulce leaves essential oil (AGO) collected from Al-Kharj (Saudi Arabia). AGO was isolated using the hydro-distillation method, and its composition was studied using gas-chromatography-mass Spectrometry (GC-MS), antimicrobial activities using well diffusion assay, and antioxidant and anti-inflammatory activities using spectrophotometric methods. The pharmacological activities of their major compounds were predicted using PASS (prediction of activity spectra for substances) and drug-likening properties by ADME (absorption, distribution, metabolism, and excretion) through web-based online tools. Isocnidilide (40.1%) was identified as the major constituent of AGO along with ß-Selinene, Senkyunolide A, Phytyl acetate, and 3-Butylphthalide. AGO exhibited a superior antibacterial activity, and the strongest activity was detected against Gram-positive bacteria and Candida albicans. Additionally, it exhibited a weaker antioxidant potential and stronger anti-inflammatory effects. PASS prediction supported the pharmacological finding, whereas ADMET revealed the safety of AGO. The molecular docking of isocnidilide was carried out for antibacterial (DNA gyrase), antioxidant (tyrosinase), and anti-inflammatory (cyclooxygenase-2) activities. The docking simulation results were involved hydrophilic interactions and demonstrated high binding affinity of isocnidilide for anti-inflammatory protein (cycloxygenase-2). The presence of isocnidilide makes AGO a potential anti-inflammatory and antimicrobial agent. AGO, and its major metabolite isocnidilide, may be a suitable candidate for the future drug development.


Assuntos
Anti-Infecciosos/química , Anti-Inflamatórios/química , Antioxidantes/química , Apium/química , Óleos Voláteis/química , Anti-Infecciosos/farmacologia , Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Humanos , Simulação de Acoplamento Molecular , Óleos Voláteis/farmacologia , Folhas de Planta/química , Arábia Saudita
18.
Front Biosci (Landmark Ed) ; 26(9): 423-441, 2021 07 30.
Artigo em Inglês | MEDLINE | ID: mdl-34590457

RESUMO

Introduction: Breast cancer is the most common type of cancer globally and its treatment with many FDA-approved synthetic drugs manifests various side effects. Alternatively, phytochemicals are natural reserves of novel drugs for cancer therapy. Punica granatum commonly known as pomegranate is a rich source of phytopharmaceuticals. Methods: The phytoconstituents of Punica granatum leaves were profiled using GC-MS/MS in the present work. Cytoscape-assisted network pharmacology of principal and prognostic biomarkers, which are immunohistochemically tested in breast cancer tissue, was carried out for the identification of protein target. Followed by, rigorous virtual screening of 145 phytoconstituents against the three ER isoforms (α, ß and γ) was performed using Discovery Studio. The docked complexes were further evaluated for their flexibility and stability using GROMACS2016 through 50 ns long molecular dynamic simulations. Results: In the current study, we report the precise and systematic GC-MS/MS profiling of phytoconstituents (19 novel metabolites out of 145) of hydromethanolic extract of Punica granatum L. (pomegranate) leaves. These phytocompounds are various types of fatty acids, terpenes, heterocyclic compounds and flavonoids. 4-coumaric acid methyl ester was identified as the best inhibitor of ER isoforms with drug-likeness and no toxicity from ADMET screening. γ-ligand binding domain complex showed the best interactions with minimum RMSD, constant Rg, and the maximum number of hydrogen bonds. Conclusion: We conclude that 4-coumaric acid methyl ester exhibits favourable drug-like properties comparable to tamoxifen, an FDA-approved breast cancer drug and can be tested further in preclinical studies.


Assuntos
Punica granatum , Cromatografia Gasosa-Espectrometria de Massas , Humanos , Farmacologia em Rede , Compostos Fitoquímicos , Extratos Vegetais , Folhas de Planta , Receptores de Estrogênio , Espectrometria de Massas em Tandem
19.
Plants (Basel) ; 10(6)2021 Jun 02.
Artigo em Inglês | MEDLINE | ID: mdl-34199475

RESUMO

Anvillea garcinii is a medicinal plant used in the Arab region for intestinal diseases, lung and liver diseases, digestive problems, and as an antidiabetic agent. Repeated chromatographic purifications of A. garcinii leaves led to the isolation of three undescribed guaiane sesquiterpene derivatives, named garcinamines F-H, characterized by the presence of an amino acid unit, along with five known sesquiterpene lactones (garcinamines B-E and 9ß-hydroxyparthenolide). The structures of the new compounds were established using spectroscopic (1D and 2D NMR) and spectrometric methods (ESIMS). Garcinamine H possesses a double bond at the Δ1,10 position, a structural feature rarely reported in guaianolide-type sesquiterpenes. The antiproliferative activity of the isolated sesquiterpenes was screened against three different cancer cell lines, and 9ß-hydroxyparthenolide and garcinamines C and D displayed significant effects against lung carcinoma (A549), colon carcinoma (LoVo), and breast carcinoma (MCF7) cell lines.

20.
Molecules ; 26(11)2021 May 26.
Artigo em Inglês | MEDLINE | ID: mdl-34073527

RESUMO

This article studies the solubility, Hansen solubility parameters (HSPs), and thermodynamic behavior of a naturally-derived bioactive thymoquinone (TQ) in different binary combinations of isopropanol (IPA) and water (H2O). The mole fraction solubilities (x3) of TQ in various (IPA + H2O) compositions are measured at 298.2-318.2 K and 0.1 MPa. The HSPs of TQ, neat IPA, neat H2O, and binary (IPA + H2O) compositions free of TQ are also determined. The x3 data of TQ are regressed by van't Hoff, Apelblat, Yalkowsky-Roseman, Buchowski-Ksiazczak λh, Jouyban-Acree, and Jouyban-Acree-van't Hoff models. The maximum and minimum x3 values of TQ are recorded in neat IPA (7.63 × 10-2 at 318.2 K) and neat H2O (8.25 × 10-5 at 298.2 K), respectively. The solubility of TQ is recorded as increasing with the rise in temperature and IPA mass fraction in all (IPA + H2O) mixtures, including pure IPA and pure H2O. The HSP of TQ is similar to that of pure IPA, suggesting the great potential of IPA in TQ solubilization. The maximum molecular solute-solvent interactions are found in TQ-IPA compared to TQ-H2O. A thermodynamic study indicates an endothermic and entropy-driven dissolution of TQ in all (IPA + H2O) mixtures, including pure IPA and pure H2O.


Assuntos
2-Propanol/química , Benzoquinonas/química , Química Farmacêutica/métodos , Água/química , Técnicas de Química Analítica , Desenho de Fármacos , Análise de Regressão , Reprodutibilidade dos Testes , Solubilidade , Solventes , Temperatura , Termodinâmica
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