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1.
Integr Pharm Res Pract ; 13: 61-68, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38827648

RESUMO

Purpose: Traditional herbal medicines (THMs) are widely used in Sudan, but there is scarcity of research on pharmacy students' attitudes and utilization of THMs. This study aims to assess the attitudes and practices of pharmacy students toward THM. Methods: A descriptive cross-sectional study was conducted among randomly selected undergraduate pharmacy students at the University of Khartoum (Sudan). Data were collected using a validated self-administered questionnaire adapted from previous studies. A statistical package for the social sciences was used for data analysis. Results: Among the 264 respondents, the average age was 21.8 years, and 84.8% of them were females. Nearly 85% of respondents were residents of Khartoum. The overall respondent's attitudes towards THMs were positive, it ranged from high (19.7%), moderate (79.9%). About 87.8% of respondents are interested in learning more about THMs. In addition, 36.4%, and 50.4% of respondents strongly agreed or agreed that THMs should be officially licensed and controlled. A 17.8% and 63.3% of respondents, respectively, reported using traditional herbal remedies either always or occasionally. Supermarkets (35.2%) and friends/family (36.4%) were the main sources of THMs for the participants, and oral administration was the most used route (87.1%). More than 90% of respondents said they would suggest THMs to others, and the most common justifications for doing so were their accessibility (46.6%) and affordability (16.3%). The most widely used herbs were Mentha spicata, Zingiber officinale, Acacia nilotica, Hibiscus sabdariffa, and Syzygium aromaticum. Data revealed a significant association between attitude levels and respondents' gender (p=0.046), year of study (p=0.000), and residence (p=0.017). Conclusion: Most undergraduate pharmacy students had a positive attitude and utilized THMs. Development of effective educational initiatives, research, and regulations are recommended to ensure the appropriate utilization of traditional herbal remedies.

2.
Integr Pharm Res Pract ; 13: 51-60, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38736676

RESUMO

Background: Cow's milk protein allergy is the most frequent type of food allergy in newborns and young children. It affects numerous body systems. A community pharmacist possessing adequate knowledge and appropriate practices is crucial for the management of the disease. Objectives: : This study aimed to assess the knowledge and attitude of community pharmacists toward the complications and treatment of cow milk protein allergy. Methods: A descriptive cross-sectional study was conducted among 332 randomly selected community pharmacists in the Capital of Sudan (Khartoum state). Data were collected using a validated and internally consistent (Cronbach Alpha = 0.712) self-administered questionnaire Descriptive statistics and Chi-square analysis were conducted using Statistical Package for the Social Sciences version 25. Results: The response rate was 95.8%, and about 47.8% of the population had 1-5 years of experience as community pharmacists, and 37.4% of them had a post-graduate degree. Only 30.8% of respondents had good knowledge, while 40.6% had poor knowledge, and 28.6% had scored as having fair knowledge of complications of Cow's milk protein allergy. Regarding knowledge toward treatment, 65.1% of respondents had a poor knowledge, 24.5% had fair knowledge, and only 10.4% had good knowledge. Overall, 39.62% of participants had a positive attitude, and 60.38% had a negative attitude toward this disease. Data analysis showed no significant association between the sociodemographic characteristics of respondents and their knowledge and attitude. Conclusion: Community pharmacists in Khartoum State had inadequate knowledge and attitude about the complications and treatment of cow milk protein allergy. As a result, we recommend the implementation of strategies to raise pharmacists' knowledge and attitude.

3.
Integr Pharm Res Pract ; 12: 77-85, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37038390

RESUMO

Background: Community pharmacists are uniquely positioned at the heart of communities, and their patient counseling role is the cornerstone for achieving the required therapeutic goals. Therefore, the main objective of this study is to explore the perceptions of community pharmacists regarding patient counseling, and their perception towards continuing pharmacy education programs. Methods: A descriptive, cross-sectional design was performed among randomly selected 238 community pharmacies in Khartoum locality (Sudan) from September 2022 to December 2022. The data were collected using a self-administered questionnaire adopted from a previous study with few minor modifications, which was adding three sociodemographic questions. Descriptive statistics were carried out according to the study objective to analyze the pharmacists' responses. Results: The majority of the community pharmacists gave counseling and understood its importance to the patients, most of them (70.6%) took 1-5 minutes during the dispensing process. The dose was the most provided information by community pharmacists (26.7%) followed by administration (23.7%) and duration (22.4%). Few (28.2%) of the patients ask the pharmacists about the cost of the medication. Lack of patients' interest (55%) was the major barrier to effective counseling followed by lack of time (47.9%). Almost all (96.2%) pharmacists in this study were interested in continuing pharmacy education programs, and they preferred programs focusing on common diseases (36.6%), and common drugs (30.3%). Conclusion: This study showed that the majority of community pharmacists in the Khartoum locality had positive perceptions toward patient counseling and they were interested in continuing pharmacy education programs.

4.
Biomed Res Int ; 2022: 3670946, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35872840

RESUMO

The goal of this study was to use polymeric konjac glucomannan (KGM), Kollidon VA 64 (KVA64), and glutaraldehyde to ameliorate stomach specific floating microspheres (SSFM) using domperidone (DoN) to increase in vivo bioavailability and emerging health pathologies. The SSFM were made using the emulsion cross-linking process, and the polymer was chosen based on its ability to get cross-linked. The thermodynamic parameters were used to determine the AL classes of phase solubility curves using ideal complexes produced with KVA64. The optimal interaction constants at 25 and 37°C were found to be 116.14 and 128.05 M-1, respectively. The prepared SSFM had an average particle size (PS) of 163.71 ± 2.26 mm and a drug content of 96.66 ± 0.32%. It can be determined from in vitro drug release experiments that drug release is good in terms of regulated drug release after 12 h (92.62 ± 2.43%). The SSFMs were approximately sphere-shaped and had smooth surfaces, according to the morphological data. SSFMs were investigated using Fourier transform infrared (FT-IR) spectroscopy, X-ray diffraction (XRD), and differential scanning calorimetry (DSC), and no chemical structural changes were identified. The SSFMs produces a considerable gastric residence time with optimal DoN release and absorption in stomach fluid, and the mean residence time (17.36 ± 1.4 h) and t 1/2 (10.47 ± 0.6 h) were considerably longer (p < 0.05) than those obtained following i.v. treatment (MRT = 8.42 ± 1.2 h; t 1/2 = 9.07 ± 0.7 h). The SSFMs maintained good physical stability for three months when stored at room temperature.


Assuntos
Domperidona , Polímeros , Varredura Diferencial de Calorimetria , Mananas , Microesferas , Tamanho da Partícula , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Estômago
5.
Adv Med Educ Pract ; 13: 309-317, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35431591

RESUMO

Background: Pharmacy educator has a number of roles and responsibilities, an information provider, clinical trainer, role model on-the-job, formal teaching settings, course planner and resource material creator, student assessor, and curriculum evaluator. Objective: This study aimed to assess the perception and commitment of pharmacy teachers in Sudanese governmental universities about their roles and educational responsibilities. Materials and Methods: Descriptive cross-sectional study was conducted at governmental pharmacy colleges in Sudan from November 2020 to July 2021. Data were collected using an online self-administered questionnaire adapted from the Association for Medical Education in Europe (AMEE) Guide No. 20. Data were analyzed using Statistical Package for Social Sciences (SPSS) version 26 and Microsoft Excel version 16. Results: Out of 125 participants, 61.6% were female and 65.6% were lecturers. Approximately half of them had less than five years' experience. The most important role perceived and the highest committed one was a lecturer in the classroom setting. Only half of the participants had good perceptions and commitment regarding teachers' roles. Age, designation, and continuous professional development were significantly associated with participants' commitment. Also, a significant association was found between the perception and practice of the participants. Conclusion: Only half of pharmacy educators were found to have a good perception and good commitment regarding their role as teachers.

6.
Adv Med Educ Pract ; 13: 189-197, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35250327

RESUMO

BACKGROUND: Academic stress is a common problem among medical students, and the COVID-19 health crisis lockdown further worsened it. High academic stress has a negative impact on students learning and overall performance. OBJECTIVE: To assess perceived academic stress, causes, and coping strategies among undergraduate pharmacy students during the COVID-19 pandemic. METHODS: A descriptive cross-sectional study was conducted among undergraduate pharmacy students at the University of Khartoum. Data were collected from randomly selected participants using three validated self-administered questionnaires; perceived stress scale, study habits inventory, and mental health inventory. Data were analyzed using SPSS software, and descriptive statistics and chi-square were employed. RESULTS: The response rate in our study was 99.6% (251/252). About 87% of the participants were females. The majority of participants (92%) experience academic stress, with a mean score (24.99 ± 5.159), the level of academic stress ranging from low (4.3%), moderate (73.2%), to high (22.5%). Approximately 80% of the percipients reported academic stress during all exam times with a mean score (25.33 ± 4.976). The level of academic stress was significantly associated with participants' gender (P-value: 0.042), and living conditions (P-value: 0.001). The most common factors that were significantly associated with academic stress were difficulty in remembering all that is studied (66.7%, P=0.006) and worrying about the exams (54.1%, P=0.011). Moreover, the most frequent strategies used to cope with academic stress were praying (84.4%) and maintaining some control over the situation (61.9%). CONCLUSION: The study revealed a high prevalence of academic stress among percipients. Academic counseling, monitoring of mental status, and implementation of stress reduction programs are highly recommended.

7.
Pharmacy (Basel) ; 10(1)2022 Feb 07.
Artigo em Inglês | MEDLINE | ID: mdl-35202075

RESUMO

The pharmacy profession has expanded and adapted to changes in community needs. Although career planning and understanding the determinants of career choice are essential, there remains a lack of studies exploring factors influencing future career plans. This study was conducted to identify career preferences and factors influencing future career choices among undergraduate pharmacy students. A cross-sectional study was carried out at the Faculty of Pharmacy, University of Khartoum. A self-administered questionnaire was used to collect data from randomly selected participants. Out of 220 respondents, 85.9% were females. The average age of the respondents was 21.7 ± 1.5 years. Clinical pharmacy was selected as the most preferred future career domain (30%), followed by academia and research (12%), the pharmaceutical industry (11%), and community pharmacy (10.5). Approximately 20% of participants reported a preference for moving abroad for work. Regarding factors influencing future career domain choice, participants ranked training in the workplace (80%) and curriculum content (70%) as the top faculty-related factors, while interaction with practicing pharmacists (71.8%) and salary (78%) were the major personal-related and job-related factors. This study emphasized the importance of understanding job preferences and the factors influencing career choice, and could be useful in ensuring a future balance between professional domains and meeting society's evolving expectations.

8.
Molecules ; 27(3)2022 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-35164217

RESUMO

Hepatitis B virus (HBV) infection is prevalent and continues to be a global health concern. In this study, we determined the anti-hepatitis B virus (HBV) potential of the Socotra-endemic medicinal plant Dracaena cinnabari and isolated and characterized the responsible constituents. A bioassay-guided fractionation using different chromatographic techniques of the methanolic extract of D. cinnabari led to the isolation of two chalcone derivatives. Using a variety of spectroscopic techniques, including 1H-, 13C-, and 2D-NMR, these derivatives were identified as 2,4'-dihydroxy-4-methoxydihydrochalcone (compound 1) and 2,4'-dihydroxy-4-methoxyhydrochalcone (compound 2). Both compounds were isolated for the first time from the red resin (dragon's blood) of D. cinnabari. The compounds were first evaluated for cytotoxicity on HepG2.2.15 cells and 50% cytotoxicity concentration (CC50) values were determined. They were then evaluated for anti-HBV activity against HepG2.2.15 cells by assessing the suppression of HBsAg and HBeAg production in the culture supernatants and their half maximum inhibitory concentration (IC50) and therapeutic index (TI) values were determined. Compounds 1 and 2 indicated inhibition of HBsAg production in a dose- and time-dependent manner with IC50 values of 20.56 and 6.36 µg/mL, respectively.


Assuntos
Chalconas/isolamento & purificação , Chalconas/farmacologia , Dracaena/química , Vírus da Hepatite B/efeitos dos fármacos , Hepatite B/tratamento farmacológico , Extratos Vegetais/farmacologia , Resinas Vegetais/farmacologia , Células Hep G2 , Hepatite B/virologia , Humanos , Árvores/química
9.
ACS Omega ; 6(43): 29100-29110, 2021 Nov 02.
Artigo em Inglês | MEDLINE | ID: mdl-34746599

RESUMO

Natural or plant products, because of their structural diversity, are a potential source for identifying new anti-hepatitis B virus (HBV) agents. Here, we report the anti-HBV activity of Euphorbia schimperi and its quercetin (QRC) and kaempferol derivatives. The anti-HBV-active methanol fraction of E. schimperi was subjected to chromatographic techniques, leading to isolation of three flavonols, following their structure determination by 1H and 13C NMR spectroscopies. Their cytotoxicity and anti-HBV potential were assessed using HBV reporter HepG2.2.15 cells, and their modes of action were delineated by molecular docking. The isolated compounds identified as quercetin-3-O-glucuronide (Q3G), quercetin-3-O-rhamnoside (Q3R), and kaempferol-3-O-glucuronide (K3G) were non-cytotoxic to HepG2.2.15 cells. The viral HBsAg/HBeAg production on day 5 was significantly inhibited by K3G (∼70.2/∼73.4%), Q3G (∼67.8/∼72.1%), and Q3R (∼63.2%/∼68.2%) as compared to QRC (∼70.3/∼74.8%) and lamivudine (∼76.5/∼84.5%) used as standards. The observed in vitro anti-HBV potential was strongly supported by in silico analysis, which suggested their structure-based activity via interfering with viral Pol/RT and core proteins. In conclusion, this is the first report on the anti-HBV activity of E. schimperi-derived quercitrin-3-O-glucuronide, quercitrin-3-O-rhamnoside, and kaempferol-3-O-glucuronide, most likely through interfering with HBV proteins.

10.
Integr Pharm Res Pract ; 10: 145-152, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34815972

RESUMO

BACKGROUND: Acute diarrhea is one of the most common health problems globally as a minor ailment, it is widely managed by community pharmacists (CPs). Professional patient counseling provided in community pharmacies is essential to decide about acute diarrhea and avoid treatment failure properly. OBJECTIVE: To assess CPs' history-taking practice, medication dispensing, and patient counseling in response to acute diarrhea in adults. METHODS: A cross-sectional, covert simulated patient (SP) study was conducted in 235 community pharmacies in the Khartoum locality. Two scenarios were used, one scenario assesses afterwards compliance to treatment guidelines and patient counseling, and second scenario determines afterwards if pharmacists referred patients to medical consultation. Six final-year pharmacy students were involved as SPs. All encounters were audio-recorded by SP. Then the investigator filled the checklist that was intended to evaluate the overall practice of pharmacists. RESULTS: As planned, 235 pharmacies were visited twice, resulting in a total of 470 visits (visit completion rate: 100%). In history taking, the most asked questions were the patient's age (89.8% for scenario 1 and 88.5% for scenario 2). Followed by the presence of blood in the stool (25.5% for scenario 1 and 28.1% for scenario 2). In scenario 1, loperamide was the most dispensed medication (81.3%), while oral rehydration solution (ORS) was dispensed in 0.9% of the visits. In counseling, verbal and written instructions were provided in 47.7% of the visits. Duration of medications was mentioned in 3.8%, advice about fluid intake was offered in 7.2% of the visits. In scenario 2, 17% of the pharmacists managed patient history well to refer patients to medical consultation, while 42.6% recommended referral after sufficient information was provided by the SP. CONCLUSION: CPs' practice in counseling toward acute diarrhea was poor; referral to medical consultation was below expectation. The current CPs dispensing practices need improvement; thus, professional education should be encouraged.

11.
Saudi Pharm J ; 28(5): 550-559, 2020 May.
Artigo em Inglês | MEDLINE | ID: mdl-32435135

RESUMO

Recently, we have shown in vitro anti-hepatitis B virus (HBV) activity of G. senegalensis J.F. Gmel leaves, and Identified quercetin and other flavonoids by HPTLC. Here we report bioassay-directed fractionation of G. senegalensis leaves using column chromatography and isolation of two flavonoinds from the n-butanol fraction, their structure determination (1H NMR, 13C NMR and 2D-NMR) and assessment of antiviral activities (HBsAg and HBeAg assay) in HBV-reporter HepG2.2.2.15 cells. Further molecular docking was performed against HBV polymerase (Pol/RT) and capsid (Core) proteins as well as host-receptor sodium taurocholate co-transporting polypeptide (NTCP). The two isolated bioactive compounds were identified as quercetin and myricetin-3-O-rhamnoside. Quercetin significantly inhibited synthesis of HBsAg and HBeAg by about 60% and 62%, respectively as compared to myricetin-3-O-rhamnoside by 44% and 35%, respectively. Molecular docking of the two anti-HBV flavonoids revealed their higher binding affinities towards Pol/RT than Core and NTCP. In conclusion, this is the first report on anti-HBV active myricetin-3-O-rhamnoside along with quercetin isolated from G. senegalensis leaves. Their possible mode of anti-HBV activities are suggested through binding with viral Pol/RT and Core as well as host NTCP proteins.

12.
J Diabetes Metab Disord ; 19(2): 1397-1406, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-33553032

RESUMO

PURPOSE: Diabetic foot infection (DFI) is one of the most feared complications of diabetes. In Sudan, the number of cases and the problems associated with diabetic foot infections increased in recent years. This study aimed to assess the bacteriological profile of patients with DFIs and their antibiotic susceptibility pattern. METHODS: A descriptive retrospective cross-sectional study was carried out at Surgery Department of Ribat University Hospital. All medical records of patients with DFIs during the period from September 2017 to February 2019 were reviewed using data collection sheet. The collected data were analyzed using Statistical Package for Social Sciences. RESULTS: Out of 250 DFI patients, 73.2% of them were males, and 86.4% of them had type 2 diabetes mellitus, and most of them suffered from diabetes for more than 10 years. Regarding culture results, 64.7% and 35.3% of the samples revealed presence of single microorganism and mixed infections, respectively. A total of 335 bacterial isolates were identified, gram-negative were more prevalent than gram-positive organisms. The most frequently isolated organisms were Proteus spp. Staphylococcus aureus, and Escherichia coli. Furthermore, antibiotic susceptibility pattern showed that imipenem, amikacin and vancomycin have the highest activity against isolated bacteria, and all isolates were found to be completely resistant to different cephalosporin drugs. CONCLUSION: Among the studied samples, gram-negative bacteria were found to be more common in DFI patients, Proteus spp. and S. aureus were the most common microorganisms. Moreover, different isolated microorganisms showed to have different degrees of resistance and sensitivity to various antibacterial drugs.

13.
BMC Complement Altern Med ; 19(1): 154, 2019 Jul 03.
Artigo em Inglês | MEDLINE | ID: mdl-31269948

RESUMO

BACKGROUND: Of over 35 Saudi plants traditionally used to treat liver disorders, majority still lack scientific validations. We therefore, evaluated the anti-oxidative, anti-apoptotic and hepatoprotective potential of Solanum surattense leaves total ethanol-extract (SSEE). METHODS: The cytoprotective (4,5-dimethylthiazol-2-yl-2,5-diphenyltetrazolium bromide/ MTT assay) and anti-apoptotic (caspase-3/7) potential of SSEE (25-200 µg/mL) were assessed in cultured HepG2 cells against dichlorofluorescein (DCFH)-induced toxicity. The hepatoprotective salutation of SSEE (100 and 200 mg/kg.bw/day) in carbon tetrachloride (CCl4)-intoxicated rats was evaluated by serum biochemistry and histopathology. The anti-oxidative activity of SSEE (31.25-500 µg/mL) was tested by 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical-scavenging and linoleic acid bleaching assays. Also, SSEE was subjected to qualitative phytochemical analysis, and standardized by validated high-performance liquid chromatography (HPTLC). RESULTS: SSEE at doses 50, 100 and 200 µg/mL showed HepG2 cell proliferative and protective potential by about 61.0, 67.2 and 95%, respectively through inhibition of caspase-3/7 against DCFH-toxicity. In CCl4-injured rats, SSEE (200 mg/kg) significantly (P < 0.001) normalized serum transaminases, alkaline phosphatase, bilirubin, cholesterol, triglycerides, and total protein, including tissue malondialdehyde and nonprotein sulfhydryls levels, supported by the liver histopathology. SSEE further showed strong in vitro anti-oxidative and anti-lipid peroxidative activities, evidenced by the presence of alkaloids, flavonoids, tannins, sterols and saponins. Identification of ß-sitosterol (3.46 µg/mg) strongly supported the anti-oxidative and hepatoprotective salutation of SSEE. CONCLUSION: Our findings suggest the therapeutic potential of S. surattense against chemical-induced oxidative stress and liver damage. However, isolation of the active principles and elucidation of mechanism of action remain to be addressed.


Assuntos
Antioxidantes/análise , Doença Hepática Induzida por Substâncias e Drogas/tratamento farmacológico , Fígado/efeitos dos fármacos , Extratos Vegetais/farmacologia , Solanum/química , Animais , Apoptose/efeitos dos fármacos , Intoxicação por Tetracloreto de Carbono/tratamento farmacológico , Avaliação Pré-Clínica de Medicamentos , Células Hep G2 , Humanos , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Ratos Wistar , Sitosteroides/análise
14.
Saudi Pharm J ; 27(4): 558-564, 2019 May.
Artigo em Inglês | MEDLINE | ID: mdl-31061625

RESUMO

In the present study we investigated the hepatotoprotective, hepatitis B virus (HBV) inhibitory and hepatic CYP450 enzyme (CYP3A4) modulatory potential of Cyperus rotundus rhizome fractions. The crude ethanol-extract, including different organic and aqueous fractions were tested for in vitro cytoprotection on HepG2 cells (MTT assay), followed by in vivo evaluation in Wistar rats (serum biochemistry and lipid profile). The in vitro anti-HBV activity was tested on HepG2.2.15 cells (HBsAg and HBeAg Elisa). Of these, the n-butanol and aqueous fractions showed the most promising, dose-dependent hepatoprotection in DCFH-injured HepG2 cells. Further, in CCl4-injured rats, oral administration of C. rotundus (100 and 200 mg/kg·bw/day) significantly normalized serum markers of healthy liver function (SGOT, SGPT, GGT, ALP and bilirubin) and lipid profile (cholesterol, HDL, LDL, VLDL, TG and MDA), including tissue NP-SH and TP levels. Compared to other fractions, the ethyl acetate, n-butanol and aqueous fractions exhibited the best inhibitory effects on viral HBsAg and HBeAg secretions in dose- and time-dependent manner. In addition, reporter gene assay (Dual-luciferase) of transfected HepG2 cells showed mild activation of nuclear PXR-mediated CYP3A4 gene by the three active fractions. Taken together, C. rotundus showed very promising hepatoprotective and anti-HBV potential in experimental settings. In addition, this is the first report on modulation of CYP3A4 by C. rotundus that suggests its safe consumption in relation to drug metabolism and efficacy. Our data could therefore, provide the basis for the ethnobotanical medicinal use of C. rotundus in metabolic liver disorder and hepatitis B patients.

15.
Saudi Pharm J ; 26(5): 685-693, 2018 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-29991912

RESUMO

Guiera senegalensis J.F. Gmel is a broad-spectrum African folk- medicinal plant, having activities against fowlpox and herpes viruses. Very recently, we have shown the anti-hepatitis B vius (HBV) potential of G. senegalensis leaves extract (GSLE). Here, we report the antioxidative and hepatoprotective efficacy of GSLE, including HPTLC quantification of four biomarkers of known antioxidative and antiviral activities. In cultured liver cells (HuH7) GSLE attenuated DCFH-induced oxidative stress and cytotoxicity. This was supported by in vitro DPPH radical-scavenging and ß-carotene-linoleic acid bleaching assays that showed strong antioxidant activity of GSLE. Further, two simple and sensitive HPTLC methods (I and II) were developed and validated to quantify ß-amyrin, ß- sitosterol, lupeol, ursolic acid in GSLE. While HPTLC-I (hexane: ethylacetate; 75:25; v/v) enabled quantification of ß-amyrin (Rf = 0.39; 20.64 µg/mg) and ß-sitosterol (Rf = 0.25; 18.56 µg/mg), HPTLC-II (chloroform: methanol; 97:3; v/v) allowed estimation of lupeol (Rf = 0.47; 6.72 µg/mg) and ursolic acid (Rf = 0.23; 5.81 µg/mg) in GSLE. Taken together, the identified biomarkers strongly supported the antioxidant and anti-HBV potential of GSLE, suggesting its activity via abating the oxidative stress. To our knowledge, this is the first report on HPTLC analysis of these biomarkers in G. senegalensis that could be adopted for standardization and quality-control of herbal-formulations.

16.
Saudi Pharm J ; 25(5): 715-723, 2017 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-28725144

RESUMO

The present study assessed the comparative antioxidant potential of the ethanol extract (EE) of leaves of four Acacia species (Acacia salicina, AS; Acacia laeta, AL; Acacia hamulosa AH; and Acacia tortilis, AT) grown in Saudi Arabia, including RP-HPTLC quantification of antioxidant biomarker rutin. In vitro DPPH radical scavenging and ß-carotene-linoleic acid bleaching assays showed the promising antioxidant activities of Acacia extracts: ASEE (IC50: 60.39 and 324.65 µg/ml) >ALEE (IC50: 217.06 and 423.36 µg/ml) >ATEE (IC50: 250.13 and 747.50 µg/ml) >AHEE (IC50: 255.83 and 417.28 µg/ml). This was comparable to rutin tested at 500 µg/ml. Further, a RP- HPTLC densitometric method was developed (acetonitrile:water; 6:4; v/v) using glass-backed RP-18 silica gel F254 plate, and scanned at UV max 254 nm. The method was validated as per the ICH guidelines. Analysis of the validated RP-HPTLC displayed an intense peak (Rf = 0.65 ± 0.004) of rutin that was estimated (µg/mg dry weight) to be highest in ASEE (10.42), followed by ALEE (2.67), AHEE (1.36) and ATEE (0.31). Taken together, presence of rutin strongly supported the high antioxidant property of the tested Acacia species, especially Acacia salicina. The developed RP-HPTLC method therefore, affirms its application in the quality control of commercialized herbal drugs or formulation containing rutin.

17.
Pharm Biol ; 55(1): 1317-1323, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-28283004

RESUMO

CONTEXT: Guiera senegalensis J.F. Gmel (Combretaceae) is a folk medicinal plant used in various metabolic and infectious diseases. In addition to its antiviral activities against herpes and fowlpox, the anti-HBV efficacy is very recently reported. OBJECTIVE: To develop and validate simple, sensitive RP-/NP-HPTLC methods for quantitative determination of biomarkers rutin, quercetin, naringenin, and gallic acid in the anti-HBV active G. senegalensis leaves ethanol-extract. MATERIALS AND METHODS: RP-HPTLC (rutin & quercetin; phase- acetonitrile:water, 4:6) and NP-HPTLC (naringenin & gallic acid; phase- toluene:ethyl acetate:formic acid, 6:4:0.8) were performed on glass-backed silica gel plates 60F254-RP18 and 60F254, respectively. The methods were validated according to the ICH guidelines. RESULTS: Well-separated and compact spots (Rf) of rutin (0.52 ± 0.006), quercetin (0.23 ± 0.005), naringenin (0.56 ± 0.009) and gallic acid (0.28 ± 0.006) were detected. The regression equations (Y) were 12.434x + 443.49, 10.08x + 216.85, 11.253x + 973.52 and 11.082x + 446.41 whereas the coefficient correlations (r2) were 0.997 ± 0.0004, 0.9982 ± 0.0001, 0.9974 ± 0.0004 and 0.9981 ± 0.0001, respectively. The linearity ranges (ng/spot) were 200-1400 (RP-HPTLC) and 100-1200 (NP-HPTLC). The LOD/LOQ (ng/band) were 33.03/100.1 (rutin), 9.67/29.31 (quercetin), 35.574/107.8 (naringenin), and 12.32/37.35 (gallic acid). Gallic acid (7.01 µg/mg) was the most abundant biomarker compared to rutin (2.42 µg/mg), quercetin (1.53 µg/mg) and naringenin (0.14 µg/mg) in the extract. CONCLUSION: The validated NP-/RP-HPTLC methods were simple, accurate, and sensitive for separating and quantifying antiviral biomarkers in G. senegalensis, and endorsed its anti-HBV activity. The developed methods could be further employed in the standardization and quality-control of herbal formulations.


Assuntos
Antivirais/análise , Combretaceae , Flavanonas/análise , Ácido Gálico/análise , Quercetina/análise , Rutina/análise , Cromatografia em Camada Fina/métodos , Vírus da Hepatite B , Extratos Vegetais/análise , Folhas de Planta
18.
Food Nutr Res ; 60: 30864, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27059702

RESUMO

BACKGROUND: Liver diseases, the fifth most common cause of global death, can be metabolic, toxin-induced, or infective. Though approximately 35 Saudi medicinal plants are traditionally used to treat liver disorders, the hepatoprotective potential of Aerva javanica has not been explored. OBJECTIVE: To investigate the antioxidative and hepatoprotective effect of Aerva javanica. DESIGN: Total ethanol extract of A. javanica aerial parts was prepared and tested on DCFH-toxicated HepG2 cells ex vivo, and in CCl4-injured Wistar rats in vivo. MTT assay was used to determine cell viability and the serum biochemical markers of liver injury as well as histopathology was performed. In vitro 1,1-diphenyl-2-picrylhydrazyl and ß-carotene free-radical scavenging assay and phytochemical screening of the extract were done. Furthermore, A. javanica total extract was standardized and validated by high-performance thin layer chromatographic method. RESULTS: MTT assay showed that, while DCFH-injured cells were recovered to ~56.7% by 100 µg/ml of the extract, a 200 µg/ml dose resulted in hepatocytes recovery by ~90.2%. Oral administration of the extract (100 and 200 mg/kg.bw/day) significantly normalized the serum glutamate oxaloacetate transaminase, serum glutamate pyruvate transaminase, gamma-glutamyl transferase, alkaline phosphatase, bilirubin, cholesterol, high-density lipoprotein, low-density lipoprotein, very-low-density lipoprotein, triglyceride, and malondialdehyde levels, including tissue nonprotein sulfhydryl and total protein in CCl4-injured rats. In addition, the histopathology of dissected liver also revealed that A. javanica cured the tissue lesion compared to silymarin treatment. In vitro assays revealed strong free-radical scavenging ability of the extract and presence of alkaloids, flavonoids, tannins, sterols, and saponins where rutin, a well-known antioxidant flavonoid, was identified. CONCLUSIONS: Our findings demonstrate the potential of A. javanica in the attenuation of ex vivo and in vivo hepatotoxicity and oxidative damage. This further suggests its therapeutic value in various liver diseases. However, isolations of the active principles, their mechanisms of action, and other therapeutic contributions remain to be addressed.

19.
Molecules ; 21(4): 409, 2016 Mar 25.
Artigo em Inglês | MEDLINE | ID: mdl-27023509

RESUMO

A novel series of sulfonamide derivatives (14 compounds) bearing thiourea moieties were efficiently synthesized and evaluated for their possible in vitro anticancer activity against four human tumor cell lines. The results indicated that compound 6 was the most potent, showing effectiveness on all the tested cell lines. Compounds 7 and 10 also showed promising results.


Assuntos
Antineoplásicos/química , Proliferação de Células/efeitos dos fármacos , Sulfonamidas/química , Antineoplásicos/administração & dosagem , Antineoplásicos/síntese química , Linhagem Celular Tumoral , Humanos , Sulfonamidas/administração & dosagem , Sulfonamidas/síntese química , Tioureia/química
20.
Curr Pharm Des ; 22(3): 286-93, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-26561057

RESUMO

Hepatitis B virus (HBV) is inherently a hepatotropic virus that causes acute and chronic hepatitis in about one-third of world population. Of the estimated 360 million chronically infected individuals, more than one million die of liver cirrhosis, fulminant liver failure or hepatocellular carcinoma (HCC) every year. Though there is an effective vaccine available, failure to protection because of vaccine-escape viral mutants in some population is also reported. Moreover, all the currently approved antiviral drugs have their limitations, too. Interferon (IFN-α) has limited efficacy and a high incidence of adverse side-effects in a proportion of chronic patients. Nucleos(t)ide analogs like, lamivudine, adefovir, tenofovir and entecavir are very effective in treating chronic hepatitis B (CHB), but long-term therapy eventually leads to drug-resistance. As an alternative approach, natural or plant products have provided promising therapeutics in modern pharma industry. Owing to their characteristics of high chemical diversity and biochemical specificity, natural products offer great promises as potentially effective antiviral drugs. A broad spectrum of phytochemicals including flavonoids (e.g., Vogonin), terpenes (e.g., Artemisinin), alkaloids (e.g., Oxymatrine), polyphenolics (e.g., geraniin), saponins (e.g., Astragaloside IV) and lignans (e.g., Helioxanthin) has been isolated and investigated for anti-HBV activities in vitro as well as in vivo. Nevertheless, these promising compounds have different and overlapping mechanisms of action by either inhibiting viral antigens secretion or suppression of DNA replication. The present article reviews the recent developments in anti-HBV natural products.


Assuntos
Antivirais/uso terapêutico , Descoberta de Drogas/métodos , Vírus da Hepatite B/efeitos dos fármacos , Hepatite B Crônica/tratamento farmacológico , Preparações de Plantas/uso terapêutico , Antivirais/administração & dosagem , Antivirais/isolamento & purificação , Farmacorresistência Viral , Vírus da Hepatite B/genética , Hepatite B Crônica/virologia , Humanos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Preparações de Plantas/administração & dosagem , Preparações de Plantas/isolamento & purificação , Plantas Medicinais/química
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