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1.
Saudi Pharm J ; 32(5): 102023, 2024 May.
Artículo en Inglés | MEDLINE | ID: mdl-38550333

RESUMEN

The escalation of many coronavirus variants accompanied by the lack of an effective cure has motivated the hunt for effective antiviral medicines. In this regard, 18 Saudi Arabian medicinal plants were evaluated for SARS CoV-2 main protease (Mpro) inhibition activity. Among them, Terminalia brownii and Acacia asak alcoholic extracts exhibited significant Mpro inhibition, with inhibition rates of 95.3 % and 95.2 %, respectively, at a concentration of 100 µg/mL. Bioassay-guided phytochemical study for the most active n-butanol fraction of T. brownii led to identification of eleven compounds, including two phenolic acids (1, and 2), seven hydrolysable tannins (3-10), and one flavonoid (11) as well as four flavonoids from A. asak (12-15). The structures of the isolated compounds were established using various spectroscopic techniques and comparison with known compounds. To investigate the chemical interactions between the identified compounds and the target Mpro protein, molecular docking was performed using AutoDock 4.2. The findings identified compounds 4, 5, 10, and 14 as the most potential inhibitors of Mpro with binding energies of -9.3, -8.5, -8.1, and -7.8 kcal mol-1, respectively. In order to assess the stability of the protein-ligand complexes, molecular dynamics simulations were conducted for a duration of 100 ns, and various parameters such as RMSD, RMSF, Rg, and SASA were evaluated. All selected compounds 4, 5, 10, and 14 showed considerable Mpro inhibiting activity in vitro, with compound 4 being the most powerful with an IC50 value of 1.2 µg/mL. MM-GBSA free energy calculations also revealed compound 4 as the most powerful Mpro inhibitor. None of the compounds (4, 5, 10, and 14) display any significant cytotoxic activity against A549 and HUVEC cell lines.

2.
Saudi Pharm J ; 32(3): 101967, 2024 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-38362039

RESUMEN

Phytotherapy, which involves the use of plant extracts and natural compounds for medicinal purposes, is indeed a promising alternative for managing urinary lithiasis. Many plants have been studied for their potential to prevent and treat kidney stones, and they may offer a more natural and potentially less harmful approach compared to conventional treatments. Additionally, phytotherapy may be more cost-effective. The aim of the present study was to investigate the antilithic potential of extracts and essential oils of Saussurea costus (Falc) Lipsch in two in vivo models, one on ethylene glycol-induced calcium oxalate crystal formation and the other to assess the effects of these extracts on magnesium oxide-induced struvite crystal formation. The experiment involved the administration of different doses of aqueous and ethanolic extracts of S. costus (200 and 400 mg/kg) and essential oils (25 and 50 mg/kg) to male Wistar rats, followed by the evaluation of various physiological, biochemical and histopathological parameters. The results demonstrated that the administration of S. costus essential oils and extracts had significant effects on the rats, influencing body weight, urine volume, crystal deposition, cytobacteriological examination of urine, and serum biochemical parameters. Histopathological examinations revealed varying impacts on the kidneys and livers of the treated rats. The findings suggest that S. costus extracts and essential oils may hold promise in inhibiting calcium oxalate crystal formation in vivo and influencing various physiological and biochemical parameters in rats. Overall, the 200 mg/kg ethanolic extract of S. costus demonstrated antilithiatic efficacy, did not exhibit signs of toxicity and reduced the number of crystals in the kidneys. Furthermore, the study did not find a significant effect on reducing struvite crystals.

3.
Life (Basel) ; 13(11)2023 Oct 29.
Artículo en Inglés | MEDLINE | ID: mdl-38004275

RESUMEN

Juncus acutus, acknowledged through its indigenous nomenclature "samar", is part of the Juncaceae taxonomic lineage, bearing considerable import as a botanical reservoir harboring conceivable therapeutic attributes. Its historical precedence in traditional curative methodologies for the alleviation of infections and inflammatory conditions is notable. In the purview of Eastern traditional medicine, Juncus species seeds find application for their remedial efficacy in addressing diarrhea, while the botanical fruits are subjected to infusion processes targeting the attenuation of symptoms associated with cold manifestations. The primary objective of this study was to unravel the phytochemical composition of distinct constituents within J. acutus, specifically leaves (JALE) and roots (JARE), originating from the indigenous expanse of the Nador region in northeastern Morocco. The extraction of plant constituents was executed utilizing an ethanol-based extraction protocol. The subsequent elucidation of chemical constituents embedded within the extracts was accomplished employing analytical techniques based on high-performance liquid chromatography (HPLC). For the purpose of in vitro antioxidant evaluation, a dual approach was adopted, encompassing the radical scavenging technique employing 2,2-diphenyl-1-picrylhydrazyl (DPPH) and the total antioxidant capacity (TAC) assay. The acquired empirical data showcase substantial radical scavenging efficacy and pronounced relative antioxidant activity. Specifically, the DPPH and TAC methods yielded values of 483.45 ± 4.07 µg/mL and 54.59 ± 2.44 µg of ascorbic acid (AA)/mL, respectively, for the leaf extracts. Correspondingly, the root extracts demonstrated values of 297.03 ± 43.3 µg/mL and 65.615 ± 0.54 µg of AA/mL for the DPPH and TAC methods. In the realm of antimicrobial evaluation, the assessment of effects was undertaken through the agar well diffusion technique. The minimum inhibitory concentration, minimum bactericidal concentration, and minimum fungicidal concentration were determined for each extract. The inhibitory influence of the ethanol extracts was observed across bacterial strains including Staphylococcus aureus, Micrococcus luteus, and Pseudomonas aeruginosa, with the notable exception of Escherichia coli. However, fungal strains such as Candida glabrata and Rhodotorula glutinis exhibited comparatively lower resistance, whereas Aspergillus niger and Penicillium digitatum exhibited heightened resistance, evincing negligible antifungal activity. An anticipatory computational assessment of pharmacokinetic parameters was conducted, complemented by the application of the Pro-tox II web tool to delineate the potential toxicity profile of compounds intrinsic to the studied extracts. The culmination of these endeavors underpins the conceivable prospects of the investigated extracts as promising candidates for oral medicinal applications.

4.
Saudi Pharm J ; 31(12): 101850, 2023 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-37965491

RESUMEN

Peptic ulcer disease is the greatest digestive disorder that has increased incidence and recurrence rates across all nations. Prangos pabularia (L.) has been well documented as a folkloric medicinal herb utilized for multiple disease conditions including gastric ulcers. Hence, the target study was investigation the gastro-protection effects of root extracts of Prangos pabularia (REPP) on ethanol-mediated stomach injury in rats. Sprague Dawley rats were clustered in 5 cages: A and B, normal and ulcer control rats pre-ingested with 1 % carboxymethyl cellulose (CMC)); C, reference rats had 20 mg/kg omeprazole; D and E, rats pre-supplemented with 250 and 500 mg/kg of REPP, respectively. After one hour, group A was given orally 1 % CMC, and groups B-E were given 100 % ethanol. The ulcer area, gastric acidity, and gastric wall mucus of all stomachs were determined. The gastric tissue homogenates were examined for antioxidant and MDA contents. Moreover, the gastric tissues were analyzed by histopathological and immunohistochemically assays. Acute toxicity results showed lack of any toxic effects or histological changes in rats exposed to 2 and 5 g/kg of REPP ingestion. The ulcer controls had extensive gastric mucosal damage with lower gastric juice and a reduced gastric pH. REPP treatment caused a significant reduction of the ethanol-induced gastric lacerations represented by an upsurge in gastric mucus and gastric wall glycoproteins (increased PAS), a decrease in the gastric acidity, leukocyte infiltration, positively modulated Bax and HSP 70 proteins, consequently lowered ulcer areas. REPP supplementation positively modulated oxidative stress (increased SOD, CAT, PGE2, and reduced MDA) and inflammatory cytokines (decreased serum TNF-α, IL-6, and increased IL-10) levels. The outcomes could be scientific evidence to back-up the folkloric use of A. Judaica as a medicinal remedy for oxidative stress-related disorders (gastric ulcer).

5.
Molecules ; 28(3)2023 Jan 31.
Artículo en Inglés | MEDLINE | ID: mdl-36771022

RESUMEN

The present study was conducted to evaluate the acute toxicity and anti-inflammatory effect in vivo, as well as the antioxidant activity, of the essential oil of Thymus leptobotrys Murb. The results indicate that the tested essential oil is non-toxic, with an estimated LD50 of 2500 mg kg-1 of mice body weight. The anti-inflammatory test revealed that, at a dose of 200 mg kg-1, the essential oil reduced rat paw edemas by 89.59% within 3 h of oral administration, this reduction in edema size was greater than that obtained with indomethacin (75.78%). The antioxidant activity (IC50) of Thymus leptobotrys Murb essential oil was 346.896 µg mL-1 and 861.136 mg Trolox equivalent/g essential oil in the 2.2-diphenyl1-picryl-hydrazyl radical scavenging capacity (DPPH) and Trolox equivalent antioxidant capacity (TEAC) assays, respectively. The toxicity test reveals an LD50 greater than 2500 mg kg-1 of body weight of mice which classifies it within category 5 of non-toxic substances that can be administered orally. These results suggest that the essential oil of Thymus leptobotrys Murb is not toxic, and it represents a valuable source of anti-inflammatory and antioxidant metabolites.


Asunto(s)
Antioxidantes , Aceites Volátiles , Ratas , Ratones , Animales , Antioxidantes/química , Aceites Volátiles/química , Aceites de Plantas/química , Antiinflamatorios/química , Fitoquímicos/farmacología , Fitoquímicos/uso terapéutico , Extractos Vegetales/química , Edema/inducido químicamente , Edema/tratamiento farmacológico
6.
Plants (Basel) ; 11(5)2022 Feb 24.
Artículo en Inglés | MEDLINE | ID: mdl-35270086

RESUMEN

Ilex dipyrena Wall (Aquifoliaceae), is a traditional medicinal plant abundantly found in India and Pakistan. In the current research work, initially, the anatomical characteristics were recorded through microscopic examination of selected plant parts, such as leaf, petiole, and midrib. Then, the quantitative phytochemical screening was performed using standard tests reported in literature. The whole-plant powdered sample was then soaked in methanol to obtain crude extract, which was then fractionated into solvents of different polarities to obtain ethyl acetate, chloroform, butanol, hexane, and aqueous extracts. The phytochemical composition of the crude ethyl acetate and chloroform extracts (being the most active fractions) was then confirmed through HPLC analyses, where the possible phytochemical present were predicted through comparison of retention time of a given compound peak with the available standards. The extracts were also evaluated for their in vitro antioxidant and ani-lipoxygenase potentials using standard methods. The microscopic examination revealed the presence of anomocytic type stomata on the abaxial side of the leaf as well as unicellular trichrome and calcium oxalate druses crystals in the midrib and petiole, with a single, centered U-shaped collateral arterial bundle, which was directed toward the adaxial and the phloem toward the abaxial sides of the selected plant parts, respectively. Almost all tested representative groups of phytochemicals and essential minerals were detected in the selected plant, whereas five possible phytochemicals were confirmed in crude and chloroform extract and seven in ethyl acetate fraction. As antioxidant, chloroform fraction was more potent, which exhibited an IC50 value of 64.99, 69.15, and 268.52 µg/mL, determined through DPPH, ABTS, and FRAP assays. Ethyl acetate extract was also equally potent against the tested free radicals. Chloroform and ethyl acetate extracts were also potent against lipoxygenase, with IC50 value of 75.99 and 106.11 µg/mL, respectively. Based on the results of biological studies, Ilex dipyrena was found to good inhibitor of free radicals and lipoxygenase that could be further investigated to isolate compounds of medicinal importance.

7.
Molecules ; 27(3)2022 Jan 30.
Artículo en Inglés | MEDLINE | ID: mdl-35164217

RESUMEN

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.


Asunto(s)
Chalconas/aislamiento & purificación , Chalconas/farmacología , Dracaena/química , Virus de la Hepatitis B/efectos de los fármacos , Hepatitis B/tratamiento farmacológico , Extractos Vegetales/farmacología , Resinas de Plantas/farmacología , Células Hep G2 , Hepatitis B/virología , Humanos , Árboles/química
8.
Plants (Basel) ; 10(12)2021 Dec 20.
Artículo en Inglés | MEDLINE | ID: mdl-34961288

RESUMEN

Several studies have demonstrated the possible synergistic effect as an effective strategy to boost the bioactivity of essential oils. Using this framework, this study was conducted to effectively establish the ideal combination of six essential oils from different plants (Origanum compactum, Origanum majorana, Thymus serpyllum, Mentha spicata, Myrtus communis, and Artemisia herba-alba) that would express the best antioxidant activity. Each mixture was optimized using a mixture design approach to generate the most effective blend. The 2,2-diphenyl-1-picrylhydrazyl radical scavenging method was used as a reference method to assess the antioxidant activity. Each essential oil's composition was identified using the GC/MS method. The single essential oil activities demonstrated variable antioxidant effects, and following the mixture design approach, the optimal antioxidant blend was revealed, as two mixtures demonstrated the best antiradical activity with 79.46% obtained with the mixture of O. majorana (28%) and M. spicata (71%) and 78.8% obtained with the mixture O. compactum (64%), O. majorana (13%), and T. serpyllum (21%). This study proposes a practical way to elaborate mixtures in the search for a boosting effect that can be oriented for the food or pharmaceutical industry.

9.
Molecules ; 26(20)2021 Oct 12.
Artículo en Inglés | MEDLINE | ID: mdl-34684724

RESUMEN

Green synthesis of silver nanoparticles (AgNPs) employing an aqueous plant extract has emerged as a viable eco-friendly method. The aim of the study was to synthesize AgNPs by using plant extract of Sanvitalia procumbens (creeping zinnia) in which the phytochemicals present in plant extract act as a stabilizing and reducing agent. For the stability of the synthesized AgNPs, different parameters like AgNO3 concentration, volume ratios of AgNO3, temperature, pH, and contact time were studied. Further, AgNPs were characterized by UV-visible spectroscopy, FT-IR (Fourier Transform Infrared Spectroscopy), XRD (X-ray Diffraction), SEM (Scanning Electron Microscopy), and EDX (Energy Dispersive X-ray Spectrometer) analysis. FT-IR analysis showed that the plant extract contained essential functional groups like O-H stretching of carboxylic acid, N-H stretching of secondary amides, and C-N stretching of aromatic amines, and C-O indicates the vibration of alcohol, ester, and carboxylic acid that facilitated in the green synthesis of AgNPs. The crystalline nature of synthesized AgNPs was confirmed by XRD, while the elemental composition of AgNPs was detected by energy dispersive X-ray analysis (EDX). SEM studies showed the mean particle diameter of silver nanoparticles. The synthesized AgNPs were used for photocatalytic degradation of Orange G and Direct blue-15 (OG and DB-15), which were analyzed by UV-visible spectroscopy. Maximum degradation percentage of OG and DB-15 azo dyes was observed, without any significant silver leaching, thereby signifying notable photocatalytic properties of AgNPs.


Asunto(s)
Asteraceae/metabolismo , Tecnología Química Verde/métodos , Nanopartículas del Metal/química , Compuestos Azo/química , Catálisis , Cistaceae , Microscopía Electrónica de Transmisión/métodos , Extractos Vegetales/química , Hojas de la Planta/química , Plata/química , Espectrometría por Rayos X/métodos , Espectroscopía Infrarroja por Transformada de Fourier/métodos , Difracción de Rayos X/métodos
10.
Front Pharmacol ; 12: 649046, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-34504421

RESUMEN

Background: Local communities use animals and plants as common traditional therapies for various diseases. The study aimed to document animals and animal-plant mixture recipes that are used as alternative and complementary medicine in southern regions of Khyber Pakhtunkhwa, Pakistan. Methods: The data were collected (2017-2018) in three remote areas (Dera Ismail Khan, Bannu, and Lakki Marwat) through questionnaires and face-to-face interviews with local inhabitants. Data on ethnomedicinal uses and cultural values of animal products or parts and their mixture with plants were analyzed using various indices such as frequency of citation (FC), informant consensus (FIC), and fidelity level (FL) to find the highly preferred species in the area. Results: A total of 185 informants (117 females and 68 males) were interviewed. The study documented 32 animal species, vertebrates (n = 24) and invertebrates (n = 8), for curing 37 types of diseases. Mammals (n = 13) were among the most commonly utilized species followed by birds (n = 8), arthropods (n = 7), reptiles (n = 2), and fishes and annelids (n = 1 each). Among the reported animals, Herpestes edwardsi (mongoose), Macaca mulatta (monkey), Labeo rohita (rohu), Oryctolagus cuniculus (rabbit), and Streptopelia decaocto (dove) were the newly reported species used as alternative medicine. The meat of Capra hircus (goat), monkey, and rabbit was used to treat chronic diseases such as hepatitis C, cancer, epilepsy, and asthma. A total of 17 plants belonging to 15 botanical families were used in combination with animal parts/products. The commonly used families were Piperaceae (31%) followed by Apiaceae (27%). The notable plant species in combination with animal products were Curcuma longa, Piper nigrum, Coriandrum sativum, Brassica rapa, and Phoenix dactylifera. Seeds were the highest used part in animal-plant mixture recipes. Gallus gallus (chicken) and Columba livia (pigeon) secured the highest (FC = 28) and (FL = 80%), respectively. FIC results had shown the highest degree of consensus for general body weakness (FIC = 0.88) and pyrexia (FIC = 0.86). Conclusion: Our findings suggest that local communities in the southern regions of Khyber Pakhtunkhwa have substantial knowledge about the formulation of ethnomedicines from both flora and fauna that need urgent documentation to avoid eroding and for conservational purposes. The newly reported phytozootherapeutic recipes and animal species can potentially be a source of pharmacologically active constituents and should be checked experimentally for further confirmation.

11.
Drug Des Devel Ther ; 15: 385-397, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33574657

RESUMEN

INTRODUCTION: Oleanolic acid, a pentacyclic triterpenic acid, is widely distributed in medicinal plants and is the most commonly studied triterpene for various biological activities, including anti-allergic, anti-cancer, and anti-inflammatory. METHODS: The present study was carried out to synthesize arylidene derivatives of oleanolic acid at the C-2 position by Claisen Schmidt condensation to develop more effective anti-inflammatory agents. The derivatives were screened for anti-inflammatory activity by scrutinizing NO production inhibition in RAW 264.7 cells induced by LPS and their cytotoxicity. The potential candidates were further screened for inhibition of LPS-induced interleukin (IL-6) and tumour necrosis factor-alpha (TNF-α) production in RAW 264.7 cells. RESULTS: The results of in vitro studies revealed that derivatives 3d, 3e, 3L, and 3o are comparable to that of the oleanolic acid on the inhibition of TNF-α and IL-6 release. However, derivative 3L was identified as the most potent inhibitor of IL-6 (77.2%) and TNF-α (75.4%) when compared to parent compound, and compounds 3a (77.18%), 3d (71.5%), and 3e (68.8%) showed potent inhibition of NO than oleanolic acid (65.22%) at 10µM. Besides, from docking score and Cyscore analysis analogs (3e, 3L, 3n) showed greater affinity towards TNF-α and IL-1ß than dexamethasone. CONCLUSION: Herein, we report a series of 15 new arylidene derivatives of oleanolic acid by Claisen Schmidt condensation reaction. All the compounds synthesized were screened for their anti-inflammatory activity against NO, TNF-α and IL-6. From the data, it was evident that most of the compounds exhibited better anti-inflammatory activity.


Asunto(s)
Aldehídos/farmacología , Antiinflamatorios/farmacología , Diseño de Fármacos , Ácido Oleanólico/farmacología , Aldehídos/química , Animales , Antiinflamatorios/síntesis química , Antiinflamatorios/química , Supervivencia Celular/efectos de los fármacos , Citocinas/análisis , Citocinas/biosíntesis , Relación Dosis-Respuesta a Droga , Lipopolisacáridos/antagonistas & inhibidores , Lipopolisacáridos/farmacología , Ratones , Modelos Moleculares , Estructura Molecular , Óxido Nítrico/antagonistas & inhibidores , Óxido Nítrico/biosíntesis , Ácido Oleanólico/química , Células RAW 264.7 , Relación Estructura-Actividad
12.
Microsc Res Tech ; 84(3): 379-393, 2021 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-32954621

RESUMEN

Second-generation biofuels prove to be a distinctive and renewable source of sustainable energy and cleaner environment. The current study focuses on the exploration and identification of four nonedible sources, that is, Brassica oleracea L., Carthamus oxyacantha M.Bieb., Carthamus tinctorius L., and Beaumontia grandiflora Wall., utilizing light microscopy (LM) and scanning electron microscopy (SEM) for studying the detailed micromorphological features of these seeds. LM revealed that size ranges from 3 to 20 mm. furthermore, a great variety of color is observed from pitch black to greenish gray and yellowish white to off white. Seeds ultrastructure study with the help of SEM revealed a great variety in shape, size, color, sculpturing and periclinal wall shape, and so on. Followed by the production of fatty acid methyl esters from a novel source, that is, seeds oil of Brassica oleracea L. (seed oil content 42.20%, FFA content 0.329 mg KOH/g) using triple metal impregnated montmorillonite clay catalyst (Cu-Mg-Zn-Mmt). Catalyst was characterized using SEM-EDX, FT-IR. Maximum yield of Brassica oleracea L. biodiesel (87%) was obtained at the conditions; 1:9 of oil to methanol ratio, 0.5 g of catalyst, 5 hr reaction time, and 90°C of temperature. Synthesized biodiesel was characterized by FT-IR, GC-MS, and NMR. Fuel properties of the Brassica oleracea L. FAMES were determined and found in accordance with ASTM standards.


Asunto(s)
Aceites de Plantas , Semillas , Esterificación , Microscopía Electrónica de Rastreo , Espectroscopía Infrarroja por Transformada de Fourier
13.
J Recept Signal Transduct Res ; 41(2): 159-169, 2021 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-32718219

RESUMEN

INTRODUCTION: Natural products play a pivotal role in innovative drug discovery by providing structural leads for the development of new therapeutic agents against various diseases.The present study aims to focus on the in silico assessment of the therapeutic potential of antidiabetic phytoconstituents which were identified and isolated from the extracts of Bauhinia rufescens Lam, a medicinal plant traditionally used for various pharmacotherapeutic purposes. METHOD: The physicochemical and pharmacokinetic parameters of the previously isolated thirty eight compounds were predicted using SwissADME web tool whereas OSIRIS Property Explorer was used for toxicity risk assessment and drug- likeliness. Twelve compounds were selected for docking on human α-glucosidase and α-amylaseenzymes using Autodock 4.0 software. Furthermore, the active extract was in vivo tested for the antidiabetic activity and then identified usingTLC bioautographic method. RESULTS AND DISCUSSION: Eriodictyol was found to have the highest potential as an inhibitor against α-amylase with binding energy of -9.92 kcal/mol. Rutin was the most potent against α-glucosidase with binding energy of-9.15 kcal/mol. A considerable number of hydrogen bonds and hydrophobic interactions were computed between the compounds and the enzymes thereby making them energetically favorable and suggesting inhibition of these two enzymes as a plausible molecular mechanism for their antidiabetic effect. CONCLUSION: These two flavonoids could therefore be used as potential leads for structure- based design of new effective hypoglycemic agents.


Asunto(s)
Bauhinia/química , Inhibidores de Glicósido Hidrolasas/química , Hipoglucemiantes/química , alfa-Amilasas/química , alfa-Glucosidasas/química , Productos Biológicos/química , Productos Biológicos/uso terapéutico , Simulación por Computador , Diabetes Mellitus/tratamiento farmacológico , Descubrimiento de Drogas , Flavonoides/química , Flavonoides/uso terapéutico , Inhibidores de Glicósido Hidrolasas/uso terapéutico , Humanos , Hipoglucemiantes/uso terapéutico , Simulación del Acoplamiento Molecular , Extractos Vegetales/química , Extractos Vegetales/uso terapéutico , Plantas Medicinales/química , alfa-Amilasas/antagonistas & inhibidores , alfa-Glucosidasas/efectos de los fármacos
14.
Saudi J Biol Sci ; 27(12): 3449-3455, 2020 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-33304155

RESUMEN

The development of antibiotic resistant in K. pneumoniae is an emerging thread worldwide due to the poor antimicrobial drugs. To overcome this issue, researchers are focused on plant material and their essential oils to fight against multi drug resistant bacteria. In this context, the current study was concentrated in medicinal plant of guva leaves and their essential oils to combat multi drug resistant bacterial infections. The essential oils were successfully screened and confirmed by HRLC-MS analysis. The anti-bacterial ability of the compounds were loaded into the chitosan nanoparticles and proved by FT-IR analysis. In addition, the chitosan loaded essential oils morphology was compared with chitosan alone in SEM analysis and suggested that the material was loaded successfully. Further, the anti-bacterial ability of the chitosan loaded essential oils were primarily confirmed by agar well diffusion method. At the 100 µg/mL of lowest concentration of chitosan loaded essential oils, the multi-drug resistant K. pneumoniae was inhibited with 96% and confirmed by minimum inhibition concentration experiment. Hence, all the experiments were proved that the essential oils were successfully loaded into the chitosan nanoparticles, and it has more anti-bacterial activity against multi-drug resistant K. pneumoniae.

15.
Risk Manag Healthc Policy ; 13: 1523-1531, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-32982510

RESUMEN

PURPOSE: Dietary supplements (DSs) are popular in many countries, and their use among individuals is increasing worldwide. Therefore, this study aimed to assess the prevalence and use of DSs among pharmacy students in King Saud University College of Pharmacy, Riyadh, Saudi Arabia. METHODS: This study used a cross-sectional design targeting male senior pharmacy students in their fourth and fifth years of Bachelor and Doctor of Pharmacy courses. The data were collected between August and October 2019 using paper-based questionnaires. RESULTS: A total of 46.8% of the students used DSs. Of all students surveyed, 19% used branded supplements whereas 9.7% used generic or local supplements and 12.3% used both generic and branded supplements. Furthermore, 8.2% students suffered from side effects, including 5.6% who suffered from nausea, vomiting, and diarrhea and 2.6% who suffered from headache, confusion, and disorientation. Approximately 24.6% of students used fiber DSs whereas 19% and 16.4% used DSs for protein and glucosamine/omega 3 fatty acids, respectively. CONCLUSION: The study findings indicated that the prevalence of DS use is increasing. However, approximately half of the respondents encourage the use of DSs only with a doctor's recommendation. Educating about the safe use of DSs is warranted.

16.
Artículo en Inglés | MEDLINE | ID: mdl-33488745

RESUMEN

Earlier studies revealed the potential therapeutic values of Loranthus regularis (L. regularis). This study evaluated Loranthus regularis (L. regularis) extract systemic antidiabetic effects and benefits against diabetic hepatocellular injuries through antioxidant and anti-inflammatory pathways using the streptozotocin (STZ) model in Wistar albino rats. After diabetes induction, animals were orally treated with L. regularis extract for 4 weeks. Serum levels of glucose, insulin, alanine aminotransferase (ALT), aspartate aminotransferase (AST), total cholesterol (TC), total triglycerides (TG), low-density lipoprotein (LDL), and high-density lipoprotein (HDL) were estimated. Furthermore, tumor necrosis factor alpha (TNF-α), interleukin-1 beta (IL-1ß), interleukin-6 (IL-6), caspase-3, nitric oxide (NO), and prostaglandin E-2 (PGE-2) were estimated in serum. In liver, thiobarbituric acid reactive substances (TBARSs) and reduced glutathione (GSH) as well as the proinflammatory cytokines and enzymatic activities of superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPx), glutathione reeducates (GR), and glutathione-S-transferase (GST) were assayed. Finally, the degree of hepatic tissue damage was evaluated histologically. Treatment of the diabetic rats with L. regularis extract markedly reduced the elevated serum levels of glucose, ALT, AST, TC, TG, LDL, TNF-α, IL-1ß, IL-6, caspase-3, NO, and PGE-2. L. regularis extract also improved serum levels of insulin and HDL. The elevated TBARS, TNF-α, IL-1ß, and IL-6 levels in hepatic tissue of diabetic animals were reduced by L. regularis. Moreover, L. regularis extract significantly restored the diminished hepatic GSH level and enzymatic activities of SOD, CAT, GPx, GR, and GST in diabetic animals. The biochemical protective effects of L. regularis were associated with improved histological hepatocellular integrity and architecture. Taken together, L. regularis has therapeutic effects against diabetic-induced hepatic complications. The restored liver functions and cellular damage might be mediated through free radicals scavenging and proinflammatory cytokine inhibition.

17.
Molecules ; 24(14)2019 Jul 22.
Artículo en Inglés | MEDLINE | ID: mdl-31336582

RESUMEN

The essential oil of Meriandra dianthera (Konig ex Roxb.) Benth. (Synonym: Meriandra bengalensis, Lamiaceae) collected from Saudi Arabia was studied utilizing GC and GC/MS. Forty four constituents were identified, representing 96.8% of the total oil. The M. dianthera essential oil (MDEO) was characterized by a high content of oxygenated monoterpenes (76.2%). Camphor (54.3%) was the major compound in MDEO followed by 1,8-cineole (12.2%) and camphene (10.4%). Moreover, MDEO was assessed for its cytotoxic, antimicrobial, and antioxidant activities. MDEO demonstrated an interesting cytotoxic activity against all cancer cell lines with IC50 values of 83.6 to 91.2 µg/mL, especially against MCF-7 cancer cells. Using labeling with annexin VFITC and/or propidium iodide (PI) dyes and flow cytometer analysis, the apoptosis induction was quantitatively confirmed for MCF-7 cells. The MDEO exhibited a considerable antimicrobial activity against all bacterial and fungal strains with minimum inhibitory concentration (MIC)-values of 0.07 to 1.25 mg/mL. The most sensitive microbial strain was Staphylococcus aureus (MIC: 0.07 mg/mL). Minimum bactericidal concentration (MBC) or minimum fungicidal concentration (MFC) values were determined one time higher than that of MIC's. Additionally, the MDEO revealed a strong activity for reducing ß-carotene bleaching with a total antioxidant value of 72.6% and significant DPPH free radical scavenging activity (78.4%) at the concentration 1000 µg/mL.


Asunto(s)
Antiinfecciosos/química , Antiinfecciosos/farmacología , Antineoplásicos/química , Antineoplásicos/farmacología , Antioxidantes/química , Antioxidantes/farmacología , Aceites Volátiles/química , Aceites Volátiles/farmacología , Salvia/química , Apoptosis/efectos de los fármacos , Canfanos , Relación Dosis-Respuesta a Droga , Medicamentos Herbarios Chinos/química , Medicamentos Herbarios Chinos/farmacología , Humanos , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Panax notoginseng , Fitoquímicos/química , Fitoquímicos/farmacología , Aceites de Plantas/química , Aceites de Plantas/farmacología , Salvia miltiorrhiza , Arabia Saudita
18.
Saudi Pharm J ; 27(2): 162-170, 2019 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-30766425

RESUMEN

Natural products from medicinal plants represent major resource of novel therapeutic substances for combating serious diseases including cancers and microbial infections. The genus Plectranthus (Family: Labiatae) represents a large and widespread group of species with a diversity of traditional uses in treatment of various ailments. Therefore, this research study aimed to evaluate the cytotoxic, antimicrobial and antioxidant activities of three Plectranthus species growing in Saudi Arabia namely P. cylindraceus Hocst. ex Benth., P. asirensis JRI Wood and P. barbatus Andrews. Moreover, this work focused on the isolation of the active constituents responsible for the activities from the most active Plectranthus species. The extracts were tested for their cytotoxic activity against three cancer cell lines (Hela, HepG2 and HT-29), using MTT-test, antimicrobial activity against Gram positive, Gram negative bacterial and fungal strains using broth micro-dilution assay for minimum inhibitory and bactericidal concentrations (MIC and MBC) and antioxidant activity using scavenging activity of DPPH radical and ß-carotene-linoleic acid methods. The ethanolic extracts of the Plectranthus species showed remarkable cytotoxic activity against all cancer cell lines with IC50 values ranging between 10.1 ±â€¯0.33 to 102.6 ±â€¯8.66 µg/mL and a great and antimicrobial activity with MIC values between 62.5 and 250 µg/mL. In addition, the three Plectranthus species showed almost moderate antioxidant activity. The most interesting cytotoxic and antimicrobial results were observed with the extract of P. barbatus. Consequently, this extract was partitioned between water and n-hexane, chloroform and n-butanol and tested. The cytotoxic activity resided predominantly in the n-hexane and chloroform fractions. The analysis of the chloroform fraction led to the isolation of four diterpenoid compounds, two of labdane- and two of abietane-type, which were identified as coleonol B, forskolin, sugiol and 5,6-dehydrosugiol. Purification of the n-hexane fraction led to isolation of a major abietane-type diterpene, which was identified as ferruginol. Sugiol, 5,6-dehydrosugiol and ferruginol were isolated for the first time from P. barbatus in this study. The isolated diterpenoids showed variable cytotoxic effects with IC50 values between 15.1 ±â€¯2.03 and 242 ±â€¯13.3 µg/mL, a great antimicrobial activity with MIC values between 15.6 and 129 µg/mL and a total antioxidant activity ranging from 23.1 ±â€¯2.9 to 69.2 ±â€¯3.8%.

19.
BMC Complement Altern Med ; 18(1): 237, 2018 Aug 10.
Artículo en Inglés | MEDLINE | ID: mdl-30097042

RESUMEN

BACKGROUND: Cancers and microbial infections are still a major health problem, therefore research on new anticancer and antimicrobial agents ought to be continued. Natural products including essential oils from medicinal plants continue to be an important resource to manage various diseases. Thus, the particular objectives of this study are to investigate the chemical composition, cytotoxic, antimicrobial and antioxidant activities of three Plectranthus species namely P. cylindraceus Hocst. ex Benth., P. asirensis JRI Wood and P. barbatus Andrews grown in Saudi Arabia. METHODS: The essential oils of the three Plectranthus species were obtained by hydrodistllation and analyzed using GC/FID and GC-MS. The essential oils were further assessed for their cytotoxic, antimicrobial and antioxidant activities. Determination of the cytotoxic activity was carried out against Hela, HepG2 and HT-29 cancer cell lines by utilizing MTT-assay. The antimicrobial activity was assessed against six bacterial and fungal strains by using broth micro-dilution assay. In addition, the antioxidant activity was evaluated utilizing the DPPH and ß-Carotene-linoleic acid assays. RESULTS: The GC/FID and GC-MS analysis led to the identification of 59, 60 and 42 compounds representing 89.0% 95.0 and 97.1% of the total essential oils of P. cylindraceus, P. asirensis and P. barbatus, respectively. The essential oils were characterized by a high content of oxygenated sesquiterpenes in P. cylindraceus, sesquiterpene hydrocarbons in P. asirensis and monoterpene hydrocarbons in P. barbatus where maaliol (42.8%), ß-caryophyllene (13.3%) and α-pinene, (46.2%) were the predominant compounds. Additionally, the oils particularly of P. cylindraceus and P. barbatus exhibited remarkable cytotoxic and antimicrobial activities with IC50-values between 3.8 and 7.5 µg/mL and MIC-values ranging from 0.137 to 4.40 mg/mL. Moreover, the oils showed moderate to high radical scavenging and antioxidative activities ranging from 52 to 75% at the highest concentration of 1 mg/mL. CONCLUSIONS: The observed results back the suggestion that these three Plectranthus species represent a promising source of cytotoxic and antimicrobial agents.


Asunto(s)
Antibacterianos , Antioxidantes , Aceites Volátiles , Aceites de Plantas , Plectranthus/química , Antibacterianos/química , Antibacterianos/farmacología , Antibacterianos/toxicidad , Antioxidantes/química , Antioxidantes/farmacología , Antioxidantes/toxicidad , Bacterias/efectos de los fármacos , Candida/efectos de los fármacos , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Cromatografía de Gases y Espectrometría de Masas , Humanos , Pruebas de Sensibilidad Microbiana , Aceites Volátiles/química , Aceites Volátiles/farmacología , Aceites Volátiles/toxicidad , Aceites de Plantas/química , Aceites de Plantas/farmacología , Aceites de Plantas/toxicidad , Arabia Saudita
20.
Artículo en Inglés | MEDLINE | ID: mdl-30069222

RESUMEN

Tuberculosis (TB) remains a common deadly infectious disease and worldwide a major health problem. The current study was therefore designed to investigate the in vitro antimycobacterial activity of different extracts of Alpinia galanga and Tinospora cordifolia. Moreover, a safety assessment for both plants was carried out. Dichloromethane and ethanolic extracts of each plant were examined against H37Rv INH-sensitive and resistant INH strains of Mycobacterium tuberculosis. The safety assessment of both plants has been performed through in vivo acute and chronic toxicity studies in animal model. Body weight, food consumption, water intake, organ's weight, and haematological and biochemical parameters of blood and serum were evaluated. The extracts of A. galanga and T. cordifolia produced significant and dose-dependent inhibitory activity with maximum effect of 18-32% at 50 µg/ml against both strains of M. tuberculosis. No effect on the body weight or food and water consumption was observed but A. galanga caused significantly an increase in the relative weight of the heart, liver, spleen, and kidney. Haematological studies of both plants revealed a slight but significant fall in the RBC and WBC level as well as haemoglobin and platelets. In addition, A. galanga extracts increased significantly liver enzymes and bilirubin and glucose.

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