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The study aimed to investigate the constituents of the ethanolic extract of Micromeria fruticosa and evaluate its antimicrobial and burn healing activities and the isolated compound, rutin. The plant was extracted with ethanol and the active constituents were isolated. The antimicrobial activities of the extract and the isolated compounds were assessed. The burn healing potentiality was evaluated in a second-degree burn model on rats. Five compounds were isolated and identified namely, oleanolic acid 3-O-β-D-glucopyranoside, apigenin, tectochrysin, 7,4' dihydroxyflavone7-rhamnoglucoside, and rutin. Noticeable antimicrobial activities of the extract, fractions and rutin, were obtained. These effects could be attributed to the isolated flavonoids and triterpenes compounds. The topical application of the extract or rutin significantly reduced the wound size and improved the skin histology. The molecular docking simulations predicted potential inhibitory interaction between rutin and the active site of IKKβ that could be responsible for blocking NF-κB activation; this could explain the possible mechanism by which rutin enhances the burn wounds healing process. Ethanolic extract, fractions and isolated compound, rutin of M. fruticosa exhibited significant antimicrobial activities. The plant extract and rutin demonstrated high potentialities to heal burns.

Background: Cancer is one of the major causes of the death and affects people of all ages throughout the world. The drugs that are currently available to treat cancer have many side effects. Hence, there is considerable scientific interest in the continuing discovery of new anticancer agents from natural sources. The aim of this study was to prepare and characterize nanoparticles combining Indigofera intricata crude alcoholic extract and chitosan and to evaluate the anticancer cell proliferative activity for both extract and nanoparticles. Methods: Dried alcoholic extract was prepared and characterized for its phenolic and flavonoid contents. Chitosan extract nanoparticles was prepared by ionic gelation method and characterized by thin layer chromatography (TLC), Fourier-transform infrared spectroscopy (FTIR), particle size and zeta-potential analysis. The anticancer cell proliferative activities of both plant extract and nanoparticles at different concentrations were evaluated using breast cancer cell line (MCF 7). Results: The alcoholic extract showed high contents from both phenolic and flavonoid constituents (15 % and 22 % respectively). The interaction of polyphenolic compounds of the extract with chitosan was confirmed by the TLC and FTIR results. The particle size and zeta-potential of nanoparticles found to be 400.6nm ± 101.8 nm and +42.1 mV ± 9.27 mV respectively. The plant extract showed the lowest cell viability of 45.21% ± 4.8% at the highest dose (250 mg) tested in this investigation. Almost 500-fold reduction (from 250 mg to 0.5 mg) in the extract concentration required to achieve same anticancer cell proliferative activity when formulated as nanoparticles. Also 2.5 mg extract containing nanoparticles showed similar anticancer cell proliferative activity as 5 mg 5-FU. Conclusion: Our results revealed that traditional medicinal plants could be an excellent source of natural anticancer agents and the chitosan-extract nanoparticles is a promising formulation strategy to enhance their clinical effectiveness.

Cisplatin-induced renal and hepatic dysfunctions are major drawbacks and obstacles to its clinical applications. Induction of inflammation is a part of its molecular mechanism of toxicity. The impact of upadacitinib, a selective JAK1-inhibitory anti-inflammatory agent, on cisplatin-induced adverse effects, histopathologic changes, kidney and liver functions, oxidative stress, and inflammatory biomarkers were investigated compared to silymarin and losartan in male Wistar rats. The animals were treated with upadacitinib (10 mg/kg/day) for two weeks in addition to one dose of cisplatin (10 mg/kg) on the seventh day of treatment. The liver and kidney functions as well as the oxidative biomarkers and inflammatory burst, were biochemically measured. Upadacitinib pre-treatment significantly improved liver function markers (ALT and AST) and inhibited cisplatin-induced lipid profile aberrations (total cholesterol and triglycerides). Moreover, it protected the kidney functions as indicated by blood urea nitrogen, serum creatinine, creatinine clearance, and albumin levels. Upadacitinib also attenuated cisplatin-induced hepatic and renal inflammatory events, as indicated by the reduction of MDA and TNFα levels. In addition, it improved the superoxide dismutase (SOD) activity. Upadacitinib effectively diminished histopathologic structural damage in liver and kidney tissues. Western blotting of NF-kB and p-Akt confirmed the renoprotective effect of upadacitinib. Furthermore, the cell viability assay shows that upadacitinib did not have any inhibitory activity on cisplatin anticancer potency in MCF-7 and A549 cells. Moreover, upadacitinib has improved the potency of cisplatin against lung cancer cells in a dose-dependent pattern. These results highlight upadacitinib's protective effects from cisplatin-induced toxicity without impairing its anticancer activity.

Micromeria fruticosa (L.) Druce subsp. Serpyllifolia (Lamiaceae) has been used widely in folk medicine to alleviate various ailments such as abdominal pains, diarrhea, colds, eye infections, heart disorders and wounds. A few reports have confirmed different therapeutic potentialities of its extracts, including the anti-inflammatory, gastroprotective, analgesic, antiobesity and antidiabetic activities. This study aimed to investigate the mechanistic pathway of the antiproliferative activity of the ethanolic extract of M. fruticose on two different cancer cell lines, namely human breast (mammary carcinoma F7 (MCF-7)) and human colorectal (human colon tumor cells (HCT-116)) cell lines. The 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide tetrazolium (MTT) assay, Annexin V-FITC/PI, caspases 8/9 and cell cycle analyses, qRT-PCR and Western blot were used to assess the effect of M. fruticosa on cytotoxicity, apoptosis, cell cycle, cell cycle-related genes and protein expression profiles in MCF-7 and HCT-116. The extract inhibits cell proliferation in a time- and dose-dependent manner. The half-maximal inhibitory concentration (IC50) for both cell lines was found to be 100 &mu, g/mL. Apoptosis induction was confirmed by Annexin V-FITC/PI, that was related to caspases 8 and 9 activities induction. Furthermore, the cell cycle analysis revealed arrest at G2/M phase. The underlying mechanism involved in the G2/M arrest was found to be associated with the downregulation of CDK1, cyclin B1 and survivin that was confirmed by qRT-PCR and Western blotting.

Glucosinolate-producing plants have long been recognized for both their distinctive benefits to human nutrition and their resistance traits against pathogens and herbivores. Despite the accumulation of glucosinolates (GLS) in plants is associated with their resistance to various biotic and abiotic stresses, the defensive and biological activities of GLS are commonly conveyed by their metabolic products. In view of this, metabolism is considered the driving factor upon the interactions of GLS-producing plants with other organisms, also influenced by plant and plant attacking or digesting organism characteristics. Several microbial pathogens and insects have evolved the capacity to detoxify GLS-hydrolysis products or inhibit their formation via different means, highlighting the relevance of their metabolic abilities for the plants' defense system activation and target organism detoxification. Strikingly, some bacteria, fungi and insects can likewise produce their own myrosinase (MYR)-like enzymes in one of the most important adaptation strategies against the GLS-MYR plant defense system. Knowledge of GLS metabolic pathways in herbivores and pathogens can impact plant protection efforts and may be harnessed upon for genetically modified plants that are more resistant to predators. In humans, the interest in the implementation of GLS in diets for the prevention of chronic diseases has grown substantially. However, the efficiency of such approaches is dependent on GLS bioavailability and metabolism, which largely involves the human gut microbiome. Among GLS-hydrolytic products, isothiocyanates (ITC) have shown exceptional properties as chemical plant defense agents against herbivores and pathogens, along with their health-promoting benefits in humans, at least if consumed in reasonable amounts. Deciphering GLS metabolic pathways provides critical information for catalyzing all types of GLS towards the generation of ITCs as the biologically most active metabolites. This review provides an overview on contrasting metabolic pathways in plants, bacteria, fungi, insects and humans towards GLS activation or detoxification. Further, suggestions for the preparation of GLS containing plants with improved health benefits are presented.

Purpose : To evaluate the synergistic or antagonistic interaction between oral dabigitran etexilate (Pradaxa) and some foods. Methods : Aqueous extracts of sweet orange, cabbage, ginger, green tea, garlic and pineapple were prepared and lyophilized, and total phenolic acids and flavonoid contents evaluated. The residues of the aqueous extracts were given daily to the rats (500 mg/kg dose, oral) 1 h after administration of dabigatran (1.83 mg/kg dose) for 14 days. Bleeding time, International Normalized Ratio (INR), prothrombin time (PT) as well as alanine aminotransferase (ALT), aspartate aminotransferase (AST) and alkaline phosphatase (ALP) in blood were measured. Results : Oral administration of Pradaxa with all the test food (except cabbage) significantly increased bleeding time, INR and PT. Pradaxa interaction with cabbage significantly decreased bleeding tendencies but the drug did not produce any major elevation of liver enzyme levels (ALT, AST and ALP). Conversely, significant elevation in ALP level was observed only after aqueous extract of ginger was administered with Pradaxa. Green tea and garlic significantly increased ALT and AST levels. Conclusion : Synergistic interaction occurrs between dabigatran etexilate with the selected foods, but interaction with cabbage antagonistic. Keywords: Dabigatran etexilate, Anticoagulant, Foods, Liver enzymes, International Normalized Ratio, Prothrombin time

Background: Gastric ulcer is one of the most prevalent gastrointestinal diseases worldwide. Protection against peptic ulcer disease (PUD) was directed at using many natural products and medicinal plants extracts since it is believed that the natural remedies are giving good healing with little harm. The present study was undertaken to investigate the possible protective effect(s) of the alcoholic extract of Fagonia indica (Zygophyllaceae) in comparison to the documented beneficial effects of natural honey solution in a model of ethanol-induced gastric ulcer. Methods: Albino rats were used in the study, divided into four groups from which one received only the vehicle (1% CMC) and served as normal control. In the other three groups, fasting animals were subjected to induction of gastric ulcer by single ingestion of 80% ethanol solution, either alone or following oral treatment with either honey solution (150 mg/kg/day) or Fagonia indica extract (20 mg/ kg/day) for two weeks. Macroscopic as well as microscopic examination were carried out and statistical significance between every two groups was checked by students-t test. Results: These revealed a significant protection of Fagonia indica extract as compared to honey solution evidenced by producing marked lower ulcer index and ulcer score while producing higher preventive index (89% for the plant extract versus 69% for honey solution). On a microscopic level, both honey and Fagonia indica caused magnificent protection of the mucosa against the damage induced by ethanol resulting both in similar degrees of protection. Conclusion: The wide usage of Fagonia indica extract in folk medicine is therefore encouraged since it is now demonstrated to possess a potent gastroprotective effect against ethanol-induced gastric ulcer. Combination of both the plant extract and honey can be advised since expected to produce more protection.

Background Hyperglycemia is a complicated condition accompanied with high incidence of infection and dyslipidemia. This study aimed to explore the phyto-constituents of Crataegus azarolus var. eu- azarolus Maire leaves, and to evaluate the therapeutic potentials particularly antimicrobial, antihyperglycemic and antihyperlipidemic of the extract and the isolated compound (3β-O-acetyl ursolic acid). Methods Total phenolics and flavonoidal contents were measured by RP-HPLC analysis. Free radicals scavenging activity of different extraction solvents was tested in-vitro on DPPH free radicals. The antimicrobial activity of the ethanolic extract and its fractions as well as the isolated compounds were evaluated in-vitro on variable microorganisms. Animal models were used to evaluate the antihyperglycemic and antihyperlipidemic activities of the ethanolic extract along with the isolated compound (3β-O acetyl ursolic acid). Results RP- HPLC analysis of the phenolics revealed high content of rutin, salicylic and ellagic acids. Six compounds belonging to triterpenes and phenolics were isolated from chloroform and n-butanol fractions namely: ursolic acid, 3β-O-acetyl ursolic acid, ellagic acid, quercetin 3-O-β methyl ether, rutin and apigenin7-O-rutinoside. Ethanolic extract showed the highest DPPH radical scavenger activity compared to other solvents. Ethanolic extract, hexane fraction, ursolic acid, 3β-O acetyl ursolic acid and quercetin 3-O-methyl ether showed variable antimicrobial activity against E. coli, P. aeruginosa, S. aureus, and C. albicans. Administration of the ethanolic extract or 3β-O acetyl ursolic acid orally to the mice reduced blood glucose significantly in a time- and dose-dependent manner. Ethanolic extract significantly reduced LDL-C, VLDL-C, TC and TG and increased HDL-C in rats. Ethanolic extract and 3β-O acetyl ursolic acid reduced in-vitro activity of pancreatic lipase. Conclusion This study reveals that Crataegus azarolus var. eu- azarolus Maire has the efficiency to control hyperglycemia with its associated complications. This study is the first to evaluate antihyperglycemic and antihyperlipidemic potentials of 3β-O acetyl ursolic acid. Electronic supplementary material The online version of this article (doi:10.1186/s12906-017-1729-9) contains supplementary material, which is available to authorized users.

Volatiles of Spathodea campanulata buds and expanded flowers were isolated by hydrodistillation / solvent extraction and direct solvent extraction. Products analysed included: primary and recovered oils (PO/RO) derived from distillates, chloroform extractives (CE) of the non-distilled fractions, and hexane concretes (HC). Number of components identified by GC-MS varied from 35-60 (88.56 - 98.17 % of the total composition). PO/RO showed close amounts of hydrocarbons and oxygenated compounds; yet, the latter prevailed in CE and HC samples. Hydrocarbon fraction was the least in buds CE (15.36 %) and greatest in flowers PO/RO (48.04 %); meanwhile, oxygenated constituents dominated flowers HC (74.04 %). Chief hydrocarbons were: alkanes and alkenes (flowers CE, 32.46 %; major phytane 16.41 %), and terpenoids (PO/RO: buds 22.44 %, major α-pinene 9.34 % vs. flowers 19.91 %, major β-selinene 8.51 %). Oxygenated constituents included: carbonyl compounds (flowers CE 31.83 %; major 6-benzofurancarboxyaldehyde...

Background Flavonoids and other polyphenols play a protective role in liver diseases and possess a high antioxidant capacity. Objective To compare and evaluate the antioxidant and hepatotoprotective activities of 4 deserts plants, Fagonia indica Burm. f., Calotropis procera R.Br., Zygophylum hamiense Schweinf. and Salsola imbricata Forssk. in correlation to their composition especially their phenolic content. Methods The influence of extracting solvent on total phenolic and flavonoidal contents was assessed spectrophotometrically. The flavonoid and other polyphenolic components of the methanol extracts were analyzed by RP-HPLC. DPPH radical scavenging potential of the different extracts was estimated. The hepatoprotective and antioxidant activities of the extracts against CCl4-induced hepatotoxicity in mice were evaluated. Results The flavonol quercitrin and rosmarinic acid were major in the F. indica, C. procera and S. imbricata samples, while rutin prevailed in that of Z. hamiense. The ethanolic and methanolic extracts showed noticeable DPPH radical-scavenging activity as compared to ascorbic acid. Assessment of liver enzymes revealed that oral administration of the extracts did not show any evidence of hepatotoxicity. Moreover, protection against CCl4-induced liver damage was evident upon administration of three plants extracts namely, F. indica, C. procera and S. imbricata. Conclusion Overall, hepatotoxicity induced by CCl4 was effectively prevented by the three plants extracts through scavenging of free radicals and by boosting the antioxidant capacity of the liver. The protective effect of the plants could be attributed to their high quercitrin and rosmarinic acid contents.

Background Hyperurecemia is usually associated with gout and various metabolic arthritis disorders. Limited medications are available to manage such conditions. This study aimed to isolate the triterpenes constituent of the plant and to assess xanthine oxidase (XO) inhibitory and antihyperuricemic activities of Tribulus arabicus ethanolic extract, its fractions and the isolated compound using in vitro and in vivo approaches. Methods The ethanolic extract, fractions; n-hexane, chloroform and n-butanol and the isolated compound (ursolic acid) were evaluated in vitro for their XO inhibitory activity. Those that demonstrated significant activity were further evaluated for their antihyperuricemic activity on potassium oxonate-induced hyperuricemia in mice. Results The ethanolic extract was found to be safe up to 5000 mg/kg. The extract and its n-hexane fraction exhibited significant inhibitory activity on XO, whilst only a modest reduction in the enzymatic activity was noticed with n-butanol and chloroform fractions. Furthermore, administration of the ethanolic extract at low and high doses significantly reduced serum urate levels in mice by 31.1 and 64.6% respectively. The isolated active constituent, ursolic acid, showed potent XO inhibition activity (Half maximal inhibitory concentration, IC50 = 10.3 μg/mL), and significantly reduced uric acid level in vivo by 79.9%. Virtually, the binding mode of ursolic acid with XO was determined using molecular docking simulations. Conclusions The activity of the ethanolic extract of T. arabicus and its n-hexane fraction can be attributed to the isolated compound, ursolic acid. Ursolic acid has good hypouricemic activity and therefore has high potential to be used for the treatment of gout and hyperuricemia-related diseases.

Reported researches dealing with either composition or bioactivity ofSalsola imbricataare limited. This study was conducted aiming to investigate the phenolic composition of the plant and evaluate its efficacy as male contraceptive. Polyphenols, namely, phenolic acids and flavonoids, were qualitatively and quantitatively analysed by RP-HPLC in the hydrolysed methanol extract using two different wavelengths, 280 and 330 nm. The efficiency of different solvents in extracting the plant phenolics was assessed via spectrophotometric determination of the total phenolic and flavonoid contents. Acute toxicity study was carried out on the ethanolic extract to ascertain its safety prior to biological evaluation. The contraceptive effect was assessed, in male rats, by oral administration of the extract at two doses (250 and 500 mg/kg b. wt.), over a period of 65 days. HPLC analyses allowed the identification and quantification of a total of 13 and 8 components in the hydrolysed-methanol extract; the overall phenolic composition was dominated by quercitrin (12.692%) followed by coumaric acid (4.251%). Prolonged oral administration of the ethanolic extract caused slight reduction in the testis weight only. A significant decrease in the sperm count was observed(P<0.01)in the two treated groups while significant decrease in the epididymal sperm motility was only observed in the high dose group. Morphological abnormalities were observed in sperms of treated animals. No distinct change in serum FSH, LH, and testosterone concentration was recorded. The histopathological findings supported to a high extent these results. The male contraceptive activity ofSalsola imbricatacould be ascribed to its phenolic components, especially quercitrin.

The aim of this study was to evaluate the potential protective effect of ozonized olive oil (OZO) in 2,4-dinitrobenzene sulphuric acid (DNBS) induced colitis in rats and to elucidate the role of so...

The anthelmintic activity of the ethanolic extracts of stems and leaves of Meryta denhamii Seem. against adult liver flukes "Fasciola gigantica" was studied in vitro. Although leaves extract was inactive, stems extract exhibited anthelmintic activity and recorded LC50 and LC90 values, 16 and 26 gm/l respectively. The mode of action of the ethanolic extract of the stems on the adult flukes was evaluated by scanning electron microscopy (SEM). Tegumental sloughing, loss of spines and deformity of suckers were observed. These damages are responsible for the vermicidal effect of the ethanolic extract of the stems. The saponin contents of the stems (4.25%) and leaves (2.45%) were determined using haemolytic index. The plant was identified based on the macro and micromorphological features of the stem and leaf.

Pregnane glycosides previously isolated from genus Caralluma ( C. Penicillata, C. tuberculata and C. russelliana ) were tested for their antitrypanosomal activity. Penicilloside E showed the highest antitrypanosomal activity (IC 50 1.01 μg/ml) followed by caratuberside C (IC 50 1.85 μg/ml), which exhibited the highest selectivity index (SI 12.04). It was noticed that acylation is required for the antitrypanosomal activity while glycosylation at C-20 has no significant effect on the activity.