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1.
Pharmaceuticals (Basel) ; 17(3)2024 Mar 18.
Artículo en Inglés | MEDLINE | ID: mdl-38543172

RESUMEN

The emergence of drug-resistant microorganisms presents a substantial global public health threat. The increase in pathogens resistant to commonly prescribed antibiotics underscores the urgent requirement to explore alternative treatment strategies. This study adopts a novel approach by harnessing natural resources, specifically essential oils (EO), to combat bacterial pathogenicity. The primary aim of this research was to analyze the chemical composition of the aerial part of the Matricaria aurea (M. aureas) EO and evaluate its potential for inhibiting quorum sensing (QS) and disrupting biofilm formation in Pseudomonas aeruginosa (P. aeruginosa). The gas chromatography-mass spectrometry (GCMS) analysis unveiled that α-bisabolol oxide A constituted the predominant portion, comprising 64.8% of the total, with ß-bisabolene at 6.3% and α-farnesene at 4.8% following closely behind. The antibiofilm efficacy was observed at concentrations of 0.3, 0.15, and 0.08 mg/mL, demonstrating negligible effects on cell viability. Furthermore, the EO from M. aurea effectively inhibited the formation of P. aeruginosa biofilms by diminishing aggregation, hydrophobicity, and swarming motility. Significantly, the EO treatment resulted in a conspicuous decrease in the production of pyocyanin, rhamnolipid, and extracellular polymeric substances (EPS), along with a reduction in the enzymatic activity of protease and chitinase. The EO effectively hindered QS by disrupting QS mechanisms, resulting in a marked decline in the secretion of N-Acyl homoserine lactone (AHL) molecules and the expression of phazA1 and aprA genes. This investigation offers compelling evidence supporting the potential of M. aurea EO as a promising therapeutic candidate for addressing infectious diseases induced by biofilm formation.

2.
Exp Ther Med ; 26(1): 327, 2023 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-37346405

RESUMEN

Hepatitis B virus (HBV) causes acute and chronic liver diseases, leading to cirrhosis and hepatocellular carcinoma. Although direct-acting nucleoside analogs, such as lamivudine (LAM), adefovir and famciclovir, are available, emergence of drug-resistance due to mutations in HBV polymerase (POL) restricts their further use. Alternatively, numerous plant products and compounds isolated from plants have been reported to confer anti-HBV efficacies without any sign of resistance in vitro or in vivo. As, flavonoids and alkaloids are the most widely reported antivirals, the anti-HBV activities of the flavonoid acacetin (ACT) and the alkaloid acetyl-ß-carboline (ABC) from the aerial parts of Rhazya stricta were assessed in the present study. Both compounds were isolated from the ethyl acetate fraction of the total methanol extract using column and thin-layer chromatography, and their structures were determined by nuclear magnetic resonance spectroscopy (NMR). Both compounds (at 6.25-50 µg/ml) showed a lack of hepatocytotoxicity in cultured HepG2.2.15 cells. Anti-HBV ELISA [hepatitis B surface antigen (HBsAg) and hepatitis B pre-core-antigen (HBeAg)] on HepG.2.2.15 cells following treatment with selected concentrations (12.5, 25 and 50 µg/ml) of both compounds showed dose- and time-dependent anti-HBV activities. Compared with those in the untreated control at day 5, ACT and ABC (25 µg/ml, each) maximally inhibited HBsAg synthesis by 43.4 and 48.7%, respectively, whilst also maximally inhibiting HBeAg synthesis by 41.2 and 44.2%, respectively, in HepG2.2.15 cells. Comparatively, quercetin and LAM (standards; POL inhibitors) suppressed HBsAg (63.9 and 60.2%, respectively) and HBeAg synthesis (87.1 and 84.3%, respectively) by larger magnitudes. Molecular docking of ACT and ABC structures performed in AutoDock revealed their hydrogen bonding with the drug-sensitive [wild-type (wt)-POL] 'Tyr-Met-Asp-Asp' motif, in addition to the drug-resistant [mutant (mut)-POL] 'Tyr-Ile-Asp-Asp' motif residues of the polymerase binding-pocket, along with other electrostatic interactions. In the wt-POL complex, both compounds showed good interactions with Asp205. In the mut-POL complex, ACT and ABC interacted with Tyr203-Asp205 and Tyr203-Ile204, respectively. In conclusion, to the best of our knowledge, the present study demonstrates anti-HBV efficacies of ACT and ABC in vitro for the first time, endorsed by in silico data. However, further molecular and pharmacological studies are required to validate their pre-clinical therapeutic potential.

3.
Molecules ; 28(3)2023 Jan 18.
Artículo en Inglés | MEDLINE | ID: mdl-36770645

RESUMEN

Quinazolines are nitrogen-containing heterocycles that consist of a benzene ring fused with a pyrimidine ring. Quinazolinones, oxidized quinazolines, are promising compounds with a wide range of biological activities. In the pharmaceutical field, quinazolinones are the building blocks of more than 150 naturally occurring alkaloids isolated from different plants, microorganisms, and animals. Scientists give a continuous interest in this moiety due to their stability and relatively easy methods for preparation. Their lipophilicity is another reason for this interest as it helps quinazolinones in penetration through the blood-brain barrier which makes them suitable for targeting different central nervous system diseases. Various modifications to the substitutions around the quinazolinone system changed their biological activity significantly due to changes in their physicochemical properties. Structure-activity relationship (SAR) studies of quinazolinone revealed that positions 2, 6, and 8 of the ring systems are significant for different pharmacological activities. In addition, it has been suggested that the addition of different heterocyclic moieties at position 3 could increase activity. In this review, we will highlight the chemical properties of quinazolinones, including their chemical reactions and different methods for their preparation. Moreover, we will try to modify some of the old SAR studies according to their updated biological activities in the last twelve years.


Asunto(s)
Alcaloides , Quinazolinonas , Caballos , Animales , Quinazolinonas/farmacología , Quinazolinonas/química , Quinazolinas/química , Relación Estructura-Actividad , Descubrimiento de Drogas
4.
BMC Health Serv Res ; 22(1): 1533, 2022 Dec 16.
Artículo en Inglés | MEDLINE | ID: mdl-36527035

RESUMEN

BACKGROUND: The use of complementary alternative medicines (CAMs) has risen globally in recent times. Such medications are exclusively and readily available in the Riyadh region of Saudi Arabia through community pharmacies and other retail outlets, exposing the consumers to various risks like harmful drug interactions. These situations take pharmacists to a responsible position where they should provide evidence-based information to help consumers make safe consumption. The consumption of CAMs can be ensured safe if pharmacists have appropriate knowledge and training about their use, dosing, side effects, etc. This study aimed to investigate and evaluate the pharmacist's factual knowledge, perception and dispensing practice related to various aspects of CAMs based on gender and experience. METHODS: The study followed a structured self-administered questionnaire-based cross-sectional survey design. Out of 200, with a response rate of 89.5%, 179 pharmacists (115 males; 64 females) from the Riyadh region of Saudi Arabia participated in this study. The knowledge scores of male and female pharmacists were compared using an unpaired t-test. The correlation between pharmacists' knowledge and their work experience was determined using Pearson's correlation coefficient test, keeping the significance value at p < 0.05. RESULTS: Almost all the respondents (99%) reported that they had never attended any lecture or course related to CAMs. Results show low knowledge scores, indicating poor respondents' knowledge concerning the use of CAMs. No significant difference was observed in knowledge scores based on gender, and no significant correlation between pharmacists' knowledge scores and their work experiences. CONCLUSION: Therefore, the study concluded that both male and female pharmacists possess equal knowledge concerning the use of CAMs, and their work experience doesn't differentiate in their knowledge. Various factors like lack of time, etc., prevented respondents from interacting with patients. Regular organization of mandatory continuing education programs about the safe use of CAMs that can improve their knowledge is recommended. In addition, establishing a pharmacy connection network system can enhance patient monitoring and CAMs vigilance. This study lays a foundation for further work to assess pharmacists' knowledge and practice patterns in Saudi Arabia. TRIAL REGISTRATION: Not applicable.


Asunto(s)
Farmacias , Farmacéuticos , Humanos , Masculino , Femenino , Estudios Transversales , Conocimientos, Actitudes y Práctica en Salud , Arabia Saudita
5.
Nanomaterials (Basel) ; 12(11)2022 May 31.
Artículo en Inglés | MEDLINE | ID: mdl-35683744

RESUMEN

Aluminum oxide nanoparticles (Al2O3 NPs) were synthesized using a simple, eco-friendly green synthesis approach in an alkaline medium from the extract of grapefruit peel waste. The pre-synthesized, nano-crystalline Al2O3 NPs were characterized by using spectroscopic (UV-vis, FTIR, XRD, and EDX) and microscopic (SEM and TEM) techniques. The formed Al2O3 NPs exhibited a pronounced absorption peak at 278 nm in the UV-vis spectrum. The average particle size of the as-prepared Al2O3 NPs was evaluated to be 57.34 nm, and the atomic percentages of O and Al were found to be 54.58 and 45.54, respectively. The fabricated Al2O3 NPs were evaluated for antioxidant, anti-inflammatory, and immunomodulatory properties. The Al2O3 NPs showed strong antioxidant potential towards all the four tested assays. The anti-inflammatory and immunomodulatory potential of Al2O3 NPs was investigated by measuring the production of nitric oxide and superoxide anion (O2•-), as well as proinflammatory cytokines tumour necrosis factor (TNF-α, IL-6) and inhibition of nuclear factor kappa B (NF- κB). The results revealed that Al2O3 NPs inhibited the production of O2•- (99.4%) at 100 µg mL-1 concentrations and intracellular NO•- (55%), proinflammatory cytokines IL-6 (83.3%), and TNF-α (87.9%) at 50 µg mL-1 concentrations, respectively. Additionally, the Al2O3 NPs inhibited 41.8% of nuclear factor kappa B at 20 µg mL-1 concentrations. Overall, the outcomes of current research studies indicated that Al2O3 NPs possess anti-inflammatory and immunomodulatory properties and could be used to treat chronic and acute anti-inflammatory conditions.

6.
Pharmaceutics ; 13(12)2021 Dec 19.
Artículo en Inglés | MEDLINE | ID: mdl-34959478

RESUMEN

The current study is focused on the biosynthesis of nutmeg oil/ polyurethane/ZnONPs bionanocomposite film for immunomodulatory and antioxidant activities. The fabricated film was prepared by using naturally extracted nutmeg oil functionalized with ZnONPs in the presence of polyutherane (PU) medium. The bionanocomposite film was obtained by incorporating dropwise 10 % (w/v) of nutmeg oil to the PU solution/ZnONPs blend. The active constituents of nutmeg oil were determined by gas chromatography coupled with mass spectrometry (GC-MS). The morphological characteristics of the resulting bionanocomposite film were confirmed using various microscopic and spectroscopic methods. Immunomodulatory potential of bionanocomposite was evaluated for RAW 264.7 macrophages. The results exhibited an excellent reduction in inflammatory cytokines (IL-6, IL-10, and TNFα) secretions after the treatment with bionanocomposite. The bionanocomposite exerted the highest inhibitory effects on certain cell signaling constituents that influence the initiation of expression of proinflammatory cytokines. The bionanocomposite was also tested for DPPH and ABTS free radicals scavenging assays and showed excellent antioxidant potential with IC50 values (0.28 ± 0.22 and 0.49 ± 0.36), respectively. The outcomes suggested promising immunomodulatory and antioxidant potentials for the biogenic synthesized nutmeg oil/PU/ZnONPs polymeric bionanocomposite.

7.
Saudi J Biol Sci ; 28(10): 5609-5616, 2021 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-34588871

RESUMEN

The hydroalcoholic extract (MIT) of Micromeria imbricata (Forssk.) growing in Saudi Arabia in addition to the chloroform (MIC) and n-butanol (MIB) fractions were investigated for the first time using UPLC-ESI-MS/MS. The analysis revealed the tentative identification of fifty-eight compounds including three organic acids, twenty-five phenolic compounds, three coumarins, two anthocyanins, twenty-one flavonoids, three terpenes, and one miscellaneous. Moreover, the therapeutic potential of M. imbricata (MIT) and its fractions (MIC and MIB) were determined by in vitro evaluation of their cytotoxic, antioxidant, and anti-obesity characteristics. The MIT extract showed the highest phenolic (125.23 ± 0.87 mg gallic acid equivalent/100 gm extract) and flavonoid (112.24 ± 2.45 mg quercetin equivalent/100 gm extract) contents followed by n-butanol and chloroform fractions. The MIT extract revealed a potent cytotoxic activity against HepG-2 (Hepatocellular carcinoma) and MCF-7 (Breast carcinoma) with IC50 28.5 ± 2.0 and 35.2 ± 1.2 µg/mL, respectively. Additionally, the tested hydroalcoholic extract exhibited a significant DPPH scavenging activity with SC50 28.4 ± 1.2 µg/mL and a remarkable lipase inhibitory activity with IC50 54.2 ± 1.2 µg/mL. In conclusion, the current study presents the first insights into the phytochemical constituents and pharmacological properties of M. imbricata extract and its chloroform and n-butanol fractions. The results revealed that M. imbricata hydroalcoholic extract might be a prolific source of bioactive constituents with potent antioxidant, cytotoxic and anti-obesity potential. It might be a natural alternative therapy and nutritional strategy for obesity treatment.

8.
Int J Pharm ; 606: 120867, 2021 Sep 05.
Artículo en Inglés | MEDLINE | ID: mdl-34242629

RESUMEN

Jatropha pelargoniifolia (JP) is a medicinal plant that is widely used in traditional medicine owing to its broad range of therapeutic activities. Despite its promising pharmacological activities, the use of plant extracts has several limitations which can be overcome using pharmaceutical nanotechnology. The aim of this study was to systematically investigate the effect of nanoencapsulation on the antimicrobial and anticancer activities of JP extract. JP-loaded chitosan nanoparticles (JP-CSNPs) were prepared using the ionic gelation method and characterized in terms of size, polydispersity index, zeta potential, encapsulation efficiency, and release profile. Transmission electron microscopy was used to observe the morphology of the nanoparticles. The mean particle size, zeta potential, and encapsulation efficiency of optimized JP-CSNPs were 185.5 nm, 44 mV, and 78.5%, respectively. The release profile of the JP-CSNPs was mainly dependent on the pH of the surrounding medium, and the JP extract was released in a controlled manner over time. The total phenolic and flavonoid contents in JP extract were 191.8 mg GAE/g extract and 51.4 mg of QE/g extract, respectively. The results of a 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay showed that JP-CSNPs retained the antioxidant activity of unencapsulated JP extract. JP-CSNPs also exhibited higher antimicrobial activity against gram-positive bacteria than against gram-negative bacteria, and their minimum inhibitory concentration was 1.6-fold lower than that of blank nanoparticles, indicating the synergy between JP extract and nanoparticles. In vitro cytotoxicity studies using A549 human lung adenocarcinoma cells revealed that JP-CSNPs had a 2-fold lower half-maximal inhibitory concentration than free extract. Molecular docking analyses revealed that the active phytoconstituent of JP extract, linarin, binds strongly to the active sites of bacterial DNA gyrase B and human DNA topoisomerase IIα and thus, may inhibit their activities. Computational analysis results supported the in vitro finding that JP-CSNPs act as an anticancer and antimicrobial agent. Taken together, the results of this study highlighted the advantages of using CSNPs as a nanocarrier for herbal extracts, thus providing a potential strategy for improving plant-based therapeutics.


Asunto(s)
Quitosano , Jatropha , Nanopartículas , Humanos , Simulación del Acoplamiento Molecular , Tamaño de la Partícula
9.
Saudi J Biol Sci ; 28(1): 785-792, 2021 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-33424368

RESUMEN

OBJECTIVE: To investigate the effect of the ethyl acetate fraction of the aerial parts of E. paralias L. F. Euphorbiaceae on nephroprotective, cytotoxic, and antioxidant. METHODS: different spectroscopic and spectrophotometric methods were applied to identify phytoconstituents. The nephroprotective potential of E. paralias ethyl acetate fraction (Ep EtOAc) was evaluated in male rats with thioacetamide-induced kidney injury, as wll as cytotoxic activity was evaluated using a viability assay, and the antioxidant activity was evaluated using the DPPH method. Results: quantitative estimation of total phenolics and flavonoids of E. paralias was performed using unique spectrophotometric methods. The polyphenolic compounds gallic acid (1), ellagic acid (2), kaempferol-3-O-(6″-O-galloyl-ß-D-glucopyranoside) (3), quercetin-3-O-ß-D-glucopyranoside (4) and quercetin-3-O-ß-D-arabinoside (5) were isolated from the ethyl acetate fraction of the aerial parts of E. paralias. The thioacetamide administration resulted in marked nephrotoxicity, but pretreatment with Ep EtOAc significantly attenuated the nephrotoxicity through alteration of kidney biomarkers, thereby improving the redox status of the tissue and restoring serum biochemical parameters nearly to normal levels. This study revealed a significant cytotoxic and strong antioxidant effect. Conclusion: we conclude that the Ep EtOAc may be used in the future as nephroprotective, cytotoxic, and antioxidant agent derived from a natural source.

10.
Food Sci Nutr ; 8(9): 5114-5127, 2020 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-32994972

RESUMEN

In the brain, propionic acid (PA) can cross cell membranes and accumulate within cells, leading to intracellular acidification, which may alter neurotransmitter release (NT), communication between neurons, and behavior. Such elevation in levels of PA constitutes a neurodevelopmental metabolic disorder called propionic acidemia, which could clinically manifest as autism. The purpose of this study was to investigate the protective effects of different fractions of bee pollen (BP) on PA-induced autism in rats, and to evaluate their effects on the expression of liver and renal biomarkers. Groups of rats received treatments of different fractions of BP at a dose of 250 mg/kg of body weight/day for a period of 1 month. Normal control group I and group II were orally administered with phosphate-buffered saline and propionic acid, respectively, for 3 days. BP contains various health-promoting phenolic components. Different fractions of BP administered pre- and post-treatment with PA showed significant reduction in the levels of liver and renal biomarkers (p < .05). Also, a significant enhancement in the levels of glutathione S-transferase (GST), catalase CAT), and ascorbic acid (VIT C) was observed. Supplementation with BP significantly reduced biochemical changes in the liver, kidneys, and brain of rats with PA-induced toxicity. It exhibited protective effects against oxidative damage and reactive oxygen species produced by PA-induced adverse reactions in rats. Taken together, our study shows that BP possesses protective effects in PA-induced liver and kidney damage.

11.
Saudi Pharm J ; 28(9): 1129-1137, 2020 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-32922145

RESUMEN

Parkinsonia aculeata L. growing in Saudi Arabia was investigated for its phytochemical profile, antioxidant, and cytotoxic properties. UPLC-ESI-MS/MS was employed as a powerful technique for the characterization of secondary metabolites from a hydroalcoholic extract, dichloromethane, and ethyl acetate fractions of P. aculeata L. aerial parts. Sixty-nine compounds (flavonoids, anthocyanins, phenolics and fatty acids) were detected and characterized; flavonoids were the abundant components in the analyzed samples. The dichloromethane fraction was rich in phenolics as vanillic acid hexoside, flavonols as 3,7-dimthylquercetin, and flavones as 3'-hydroxymelanettin. However, the ethyl acetate fraction was rich in flavonoid-C-glycosides as luteolin-8-C-ß-D-glucoside (orientin) and apigenin-8-C-glucoside (vitexin), flavonoid- O, C-diglycosides such as luteolin 7-O-[6''-dihydrogalloyl]-glucosyl-8-C-pentosyl-(1 → 2)-glucoside and 2''-O-rhamnosyl isoorientin. These compounds were identified for the first time in dichloromethane and ethyl acetate fractions of Saudi P. aculeata L. Additionally, all the samples were assessed for antioxidant activity using DPPH radical scavenging method and for cytotoxic activity through MTT assay. Accordingly, the most active fraction was the ethyl acetate which showed the highest antioxidant activity (SC50 = 57.4 ±â€¯1.2 µg/mL) compared with the positive control, ascorbic acid (SC50 = 12.4 ±â€¯0.5 µg/mL) and moderate cytotoxicity against HepG-2 (hepatocellular carcinoma) and MCF-7 (breast carcinoma) cell lines with IC50 = 56.9 ±â€¯3.1 and 95.8 ±â€¯3.8 µg/mL, respectively compared with cisplatin (IC50 = 3.67 ±â€¯0.22 and 5.71 ±â€¯0.57 µg/mL, respectively for both cell lines). The antioxidant and cytotoxic activities may be attributed to the presence of high percentage of phenolic compounds and hydroxylated flavonoids detected in ethyl acetate fraction using UPLS-ESI-MS/MS.

12.
J Ayurveda Integr Med ; 10(4): 290-293, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-31753479

RESUMEN

Massage therapy (MT) is the physical manipulation of the soft tissues. It primarily consists of manual or hands-on techniques such as applying fixed or movable pressure, holding, and moving muscles and body tissues. MT is beneficial for pain relief, sport-related injury rehabilitation, stress reduction, and to address psychological disorders. MT is the most prevalent form of complementary and alternative (CAM) therapy worldwide. The aim of this study was to evaluate the knowledge, attitudes, and perceptions regarding MT among the Saudi community. A cross-sectional online survey using WhatsApp©, Google Forms©, Facebook©, and Twitter© was conducted among the general community of the Kingdom of Saudi Arabia (KSA) to assess the knowledge, attitudes, and perceptions regarding MT. Data was collected using a 20-item, self-administered questionnaire consisting of a series of both closed-ended and Likert-type questions. A total of 436 respondents completed the survey. Most of the respondents were female 84.2% (n = 367). Approximately 65% resided in the central region of KSA. The majority of the respondents, 81.4%, believed that MT is effective, 27.7% thought that MT leads to complications, and more than half of the residents, 55.7%, believed that patients should consult with their physicians prior to MT. The most common reasons for MT were to treat muscle pain, for relaxation purposes, to treat bone and joint pain, and backache relief, which were reported by 49%, 20%, 19%, and 16% of the participants, respectively. The knowledge, attitudes, and perceptions of the Saudi population towards MT are insufficient in some aspects. The establishment of community-based health education programs to improve knowledge of MT is recommended.

13.
Saudi Pharm J ; 27(5): 664-672, 2019 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-31297021

RESUMEN

Quorum sensing is an important regulatory factor of P. aeruginosa virulence induction such as BF, motility, formations of proteases, pyocyanin, and some toxins. The aim of the current study is to detect the effect of the pet.ether extract from onion husk and compound drive from it on quorum sensing and virulence formations of P. aeruginosa. Quorum sensing inhibiting effect of the pet.ether extract of onion husk and a compound drive from it, was evaluated by C. violaceum reporter using dilution method as well as an antioxidant by using DPPH. The efficacious of: Quorum sensing inhibiting on pet.ether fraction and compound derived from it, were investigated for their activities toward biofilm and pyocyanin synthesis as well as motility from P. aeruginosa. The pet.ether fraction and compound derived from it of onion husk exhibited potent antimicrobial, antioxidant and Quorum sensing inhibiting effects. The pet.ether fraction and compound derived from it possesses significant reduction on pyocyanin and biofilm induction of P. aeruginosa. Moreover, they significantly inhibited swimming motilities of P. aeruginosa. For the first time, our study showed the medical importance of Allium cepa L. as antimicrobial, antioxidant as well as Quorum sensing inhibiting and virulence suppressors of P. aeruginosa. Thus, these might emphasized on Allium cepa L as a natural source for attenuating toxins of the Pseudomonas.

14.
Saudi Pharm J ; 26(7): 1060-1067, 2018 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-30416363

RESUMEN

The genus Hibiscus contains about 275 species of flowering plants widely grown in the tropics and sub-tropics. The available literature revealed that several Hibiscus species exhibited excellent anticancer activity against several cancer cells like lung, breast, and liver. This motivated the authors to explore the anticancer property of other Hibiscus species (Hibiscus calyphyllus, H. deflersii and H. micranthus) along with development of a validated HPTLC method for the concurrent analysis of three anticancer biomarkers (ursolic acid, ß-sitosterol and lupeol) in different Hibiscus species. The anticancer activity of various fractions (petroleum ether, toluene, dichloromethane, ethyl acetate and n-butanol) of all the Hibiscus species (aerial parts) were evaluated in vitro against HepG2 and MCF-7 cell lines using MTT assay. The HPTLC analysis was carried out using chloroform and methanol as mobile phase (97:3; v/v) on 20 × 10 cm glass-backed silica gel 60F254 plates and analyzed different phytoconstituents present in all fractions at λ = 575 nm wavelength. Of the tested fractions of H. calyphyllus, H. deflersii and H. micranthus, HdP (H. deflersii petroleum ether fraction) exhibited the most potent cytotoxic effect on HepG2 and MCF-7 (IC50: 14.4 and 11.1 µg/mL, respectively) cell lines. Using the developed HPTLC method a compact and intense peak of ursolic acid, ß-sitosterol and lupeol were obtained at Rf = 0.22, 0.39 and 0.51, respectively. The LOD/LOQ (ng) for ursolic acid, ß-sitosterol and lupeol were found as 42.30/128.20, 13.20/40.01 and 31.57/95.68, respectively in the linearity range 100-1200 ng/spot. The obtained result showed maximum presence of ursolic acid, ß-sitosterol and lupeol (5.50, 11.85 and 7.47 µg/mg, respectively) in HdP which also supported its strong anticancer effect. Our data suggest that H. deflersii petroleum ether fraction (HdP) can be further subjected to the isolation of active cytotoxic phytoconstituents and establishment of their mechanism of action. The maiden developed HPTLC method for concurrent analysis of anticancer biomarkers may be further employed in the in process quality control of herbal formulation containing the said biomarkers.

15.
Saudi Pharm J ; 26(2): 266-273, 2018 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-30166927

RESUMEN

In this study, we developed a validated HPTLC method for concurrent analysis of two natural antioxidant triterpenes, oleanolic acid (OA) and ß-amyrin (BA) in the biologically active fractions (petroleum ether, toluene, chloroform, ethyl acetate and n-butanol) of aerial parts of three Hibiscus species (H. calyphyllus, H. deflersii and H. micranthus). The chromatography was conducted on normal HPTLC (ready to use glass-plate coated with silica gel 60 F254) plate with chloroform and methanol (97:3, V/V) used as mobile phase. The derivatization of the developed plate was done with p-anisaldehyde and scanned at λmax = 575 nm. Well resolved and intense peaks of OA and BA were obtained at Rf = 0.36 and 0.57, respectively. The linear regression equation/correlation coefficient (r2) for OA and BA were Y = 6.65x + 553.35/0.994 and Y = 9.177x + 637.23/0.998, respectively in the linearity range of 100-1200 ng/spot indicated good linear relationship. The low values of %RSD for intra-day/inter-day precision of OA (1.45-1.61/1.38-1.59) and BA (1.52-1.57/1.50-1.53) suggested that the method was precise. The recovery/RSD (%) values for OA and BA were found to be 99.21-99.62/1.39-1.95 and 98.75-99.70/1.56-1.80, respectively assures the reasonably good accuracy of the proposed method. Fifteen samples were analyzed to check the content of OA and BA by using the developed HPTLC methods. The content of OA in different samples were found to be 3.87 (HmP) > 1.212 (HcP) > 0.673 (HdC) > 0.493 (HdP) > 0.168 (HdE) > 0.059 (HcC) > 0.015 (HcE) > 0.008 (HmT) µg/mg of the dried weight of extract. However the content of BA was found as: 2.293 (HmP) > 1.852 (HdT) > 0.345 (HdC) > 0.172 (HmT) > 0.041 (HdE) > 0.008 (HcC) µg/mg of the dried weight of extract. Some Hibiscus species fractions exhibited good antioxidant potential like: HcE (IC50 = 17.6 ±â€¯1.8) > HdB (IC50 = 32.16 ±â€¯0.9) > HmP (IC50 = 80.4 ±â€¯4.5) > HmT (IC50 = 99.7 ±â€¯8.2) when compared with ascorbic acid (IC50 = 14.2 ±â€¯0.5), while other fractions exhibited only mild antioxidant capability. The developed HPTLC method can be further exploited for analysis of these markers in the quality assessment of raw material as well as herbal formulations available in the market.

16.
Pak J Pharm Sci ; 30(5(Supplementary)): 1971-1979, 2017 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-29105630

RESUMEN

Onion peel is a common bio-waste, occasionally used in traditional medicine in treatment of liver ailment and inflammation. However, a phytochemical and biological study is further required to provide the scientific evidence for this use. A phenolic-rich extract of red onion peels (coded as ACPE) was primarily prepared and then subjected to chromatographic separation. From the extract, six phenolic antioxidant compounds along with two phytosterols were isolated and identified by means of spectroscopic (NMR and MS) analyses. The in vivo protective activity of the ACPE against the oxidative stress induced by carbon tetrachloride (CCl4) free radicals, in liver and kidney, was assessed in rats. Relative to the CCl4-challenged animals, pre-treatment with ACPE could significantly ameliorate the hepatonephrolinked serum and tissue markers in a dose-dependent response. The flavonol- and phenolic acid-based nature of constituents, the high phenolic content (72.33±5.30 mg gallic acid equivalent per one gram) and the significant antioxidant capacity (>1/3 potency of rutin) of ACPE may be thus attributed strongly to the hepatonephro-protective and anti-inflammatory effect of ACPE. The results suggest that red onion peels can serve as a convenient and cost-effective source of high-value antioxidant nutraceuticals for protection against oxidative stress-related disorders.


Asunto(s)
Antioxidantes/farmacología , Enfermedad Hepática Inducida por Sustancias y Drogas/prevención & control , Enfermedades Renales/prevención & control , Riñón/efectos de los fármacos , Hígado/efectos de los fármacos , Cebollas/química , Estrés Oxidativo/efectos de los fármacos , Fenoles/farmacología , Extractos Vegetales/farmacología , Raíces de Plantas/química , Analgésicos/aislamiento & purificación , Analgésicos/farmacología , Animales , Antiinflamatorios/aislamiento & purificación , Antiinflamatorios/farmacología , Antioxidantes/aislamiento & purificación , Antioxidantes/toxicidad , Biomarcadores/sangre , Tetracloruro de Carbono , Enfermedad Hepática Inducida por Sustancias y Drogas/sangre , Enfermedad Hepática Inducida por Sustancias y Drogas/etiología , Enfermedad Hepática Inducida por Sustancias y Drogas/patología , Citoprotección , Modelos Animales de Enfermedad , Relación Dosis-Respuesta a Droga , Riñón/metabolismo , Riñón/patología , Enfermedades Renales/sangre , Enfermedades Renales/inducido químicamente , Enfermedades Renales/patología , Peroxidación de Lípido/efectos de los fármacos , Hígado/metabolismo , Hígado/patología , Masculino , Cebollas/toxicidad , Fenoles/aislamiento & purificación , Fenoles/toxicidad , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/toxicidad , Raíces de Plantas/toxicidad , Ratas Wistar
17.
Front Microbiol ; 8: 1675, 2017.
Artículo en Inglés | MEDLINE | ID: mdl-28928721

RESUMEN

The resistance and pathogenesis of bacteria could be related to their ability to sense and respond to population density, termed quorum sensing (QS). Inhibition of the QS system is considered as a novel strategy for the development of antipathogenic agents, especially for combating drug-resistant bacterial infections. In the present study, the anti-QS activity of Onion peel ethylacetate fraction (ONE) was tested against Chromobacterium violaceum CV12472 and Pseudomonas aeruginosa PAO1. ONE inhibit the QS-mediated virulence factors production such as violacein in C. violaceum and elastase, pyocyanin in P. aeruginosa. Further, the treatment with sub-MICs of ONE significantly inhibited the QS-mediated biofilm formation, EPS (Extracellular polymeric substances) production and swarming motility. Further, quercetin 4'-O-ß-D glucopyranoside (QGP) was isolated from ONE and its anti-QS potential was confirmed after observing significant inhibition of QS-controlled virulence factors such as violacein, elastase, pyocyanin and biofilm formation in test pathogens. Molecular docking analysis predicted that QGP should be able to bind at the active sites of Vfr and LasR, and if so blocks the entry of active sites in Vfr and LasR.

18.
Afr J Tradit Complement Altern Med ; 13(5): 170-177, 2016.
Artículo en Inglés | MEDLINE | ID: mdl-28487908

RESUMEN

BACKGROUND: Complementary and alternate medicine (CAM) has been defined as a group of diverse medical and healthcare systems, practices, and products not presently considered part of conventional medicine (CM). Studies in different countries have revealed a geographical difference in the knowledge about CAM therapies, especially among medical school staff and students. This study aimed to assess the extent of CAM use among staff working in paramedical colleges in the Riyadh region of Saudi Arabia and to examine their perception and attitudes towards such medicines. MATERIALS AND METHODS: Eighty paramedical staff members of different age groups and specializations were invited to participate in the study. A self-administered questionnaire adapted from similar studies was used in this study. RESULTS: The response rate was 99%. The majority of respondents (56%) reported believing that CAM therapies play an important complementary role to the action ofCM. CONCLUSION: To the best of the authors' knowledge, this is the first study of its kind to assess peoples' attitudes towards CAM use in the region. As the use of healing practices outside of CM rise among patients, ignorance of CAM by future medical practitioners can cause a communication gap between people and the profession that serves them. It is encouraging that the majority of medical staff in this study recognizes and is enthusiastic to rectify this lack of knowledge. List of Non-Standard Abbreviations: CAM: Complementary and alternate medicine; CM: Conventional medicine.


Asunto(s)
Técnicos Medios en Salud/psicología , Actitud del Personal de Salud , Terapias Complementarias/psicología , Conocimientos, Actitudes y Práctica en Salud , Adulto , Femenino , Humanos , Masculino , Arabia Saudita , Facultades de Medicina , Encuestas y Cuestionarios , Adulto Joven
19.
Pharmacogn Mag ; 11(Suppl 1): S173-81, 2015 May.
Artículo en Inglés | MEDLINE | ID: mdl-26109764

RESUMEN

BACKGROUND: Antioxidant natural products and chemoprevention are considered nowadays as an effective approach against health various disorders and diseases induced by oxidative stress or free radicals. OBJECTIVE: The aim of this study was to assess the hepato- and nephroprotective activity of a standardized red vine leaf aqueous extract AS195 (Antistax(®)). METHODS: The protective activity of AS195 (100 mg/kg) was investigated on carbon tetrachloride (CCl4)-intoxicated rats in comparison with silymarin. The flavonoid/proanthocyanidin nature of AS195 was identified by phytochemical and nuclear magnetic resonance (NMR) analyses, while its total phenol/proanthocyanidin/flavonoid content and antioxidant activity were determined by Folin-Ciocalteau, vanillin-sulfuric acid, AlCl3, and 2, 2-diphenyl-2-picrylhydrazyl radical scavenging assays, respectively. RESULTS: Relative to the control CCl4 -intoxicated group, pretreatment with AS195 could significantly suppressed the elevated serum levels of alanine aminotransferase, alkaline phosphatase, γ-glutamyl transferase, total cholesterol, low-density lipoprotein cholesterol, very low-density lipoprotein cholesterol, triglycerides, bilirubin, creatinine, uric acid, and calcium, whereas it significantly increased the diminished serum levels of high-density lipoprotein cholesterol, albumin and total protein. Moreover, AS195 significantly decreased malondialdehyde formation in the tissues of liver and kidney, whereas it significantly elevated and nonprotein sulfhydryl groups, compared with the intoxicated control. The improvement in biochemical parameters by AS195 was obviously observed and further confirmed by restoration of normal histological features in the two organs. CONCLUSIONS: The results of the present study revealed the capacity of AS195 to enhance the recovery from xenobiotic-induced hepatorenal toxicity initiated by free radicals.

20.
J Med Food ; 18(3): 280-9, 2015 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-25569813

RESUMEN

A hydroacetone extract was prepared from seeds of Phoenix dactylifera L. var. Khalas, which is an industrial by-product of date processing. The proanthocyanidin nature of the extract (coded as DTX) was characterized by phytochemical and nuclear magnetic resonance (NMR) analyses. The total phenol/proanthocyanidin content and antioxidant activity of DTX were estimated by Folin-Ciocalteu, vanillin-sulfuric acid, and 2,2-diphenyl-1-picrylhydrazyl (DPPH) assays, respectively. The hepatorenal protective activity of DTX was evaluated using CCl4-induced toxicity model in rats, in comparison with silymarin (SYL). Results of the histopathological examination and measurements of various hepatorenal serum indices and tissue biochemical markers demonstrated that DTX displayed marked protective potential against CCl4-induced liver and kidney injury at 100 mg/kg/rat. Relative to the control CCl4-intoxicated group, pretreatment with DTX significantly (P<.001) suppressed the elevated serum levels of alanine aminotransferase and aspartate aminotransferase (ALT and AST), alkaline phosphatase (ALP), γ-glutamyl transferase (GGT), total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), bilirubin, creatinine, and calcium, whereas it significantly (P<.001) increased the diminished serum levels of high-density lipoprotein cholesterol (HDL-C) and total protein (TP). Moreover, DTX significantly decreased malondialdehyde (MDA) formation and increased TP synthesis in hepatorenal tissues compared with the intoxicated control. The improvement in biochemical parameters by DTX was observed in a dose-dependent manner and confirmed by restoration of normal histological features. The acute toxicity test of DTX in rats revealed safety of the extract. This study reveals that DTX enhances the recovery from xenobiotics-induced toxicity initiated by free radicals.


Asunto(s)
Antioxidantes/uso terapéutico , Enfermedad Hepática Inducida por Sustancias y Drogas/tratamiento farmacológico , Enfermedades Renales/tratamiento farmacológico , Phoeniceae/química , Fitoterapia , Proantocianidinas/uso terapéutico , Semillas/química , Animales , Antioxidantes/farmacología , Biomarcadores/sangre , Compuestos de Bifenilo/metabolismo , Tetracloruro de Carbono , Enfermedad Hepática Inducida por Sustancias y Drogas/sangre , Enfermedad Hepática Inducida por Sustancias y Drogas/patología , Enfermedades Renales/sangre , Enfermedades Renales/inducido químicamente , Enfermedades Renales/patología , Hígado/efectos de los fármacos , Hígado/metabolismo , Masculino , Fenoles/farmacología , Fenoles/uso terapéutico , Picratos/metabolismo , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Proantocianidinas/farmacología , Ratas Wistar
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