Advances In Pharmacological Sciences[JOURNAL]
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200 papers
Toward Improving Medication Adherence: The Suppression of Bitter Taste in Edible Taste Films.
Cherian S, Lee BS, Tucker RM … +2 more , Lee K, Smutzer G
Adv Pharmacol Sci · 2018 · PMID 30046304 · Full text
Bitter taste is aversive to humans, and many oral medications exhibit a bitter taste. Bitter taste can be suppressed by the use of inhibitors or by masking agents such as sucralose. Another approach is to encapsulate bit...
Bitter taste is aversive to humans, and many oral medications exhibit a bitter taste. Bitter taste can be suppressed by the use of inhibitors or by masking agents such as sucralose. Another approach is to encapsulate bitter tasting compounds in order to delay their release. This delayed release can permit the prior release of bitter masking agents. Suppression of bitter taste was accomplished by encapsulating a bitter taste stimulus in erodible stearic acid microspheres, and embedding these 5 meter diameter microspheres in pullulan films that contain sucralose and peppermint oil as masking agents, along with an encapsulated masking agent (sucralose). Psychophysical tests demonstrated that films which encapsulated both quinine and sucralose produced a significant and continuous sweet percept when compared to films without sucralose microspheres. Films with both quinine and sucralose microspheres also produced positive hedonic scores that did not differ from control films that contained only sucralose microspheres or only empty (blank) microspheres. The encapsulation of bitter taste stimuli in lipid microspheres, and embedding these microspheres in rapidly dissolving edible taste films that contain masking agents in both the film base and in microspheres, is a promising approach for diminishing the bitter taste of drugs and related compounds.
Supplementation with Alpha-Tocopherol and Ascorbic Acid to Nonalcoholic Fatty Liver Disease's Statin Therapy in Men.
Hadzi-Petrushev N, Dimovska K, Jankulovski N … +2 more , Mitrov D, Mladenov M
Adv Pharmacol Sci · 2018 · PMID 29887885 · Full text
Oxidative stress and inflammation contribute to the pathogenesis and progression of nonalcoholic fatty liver disease (NAFLD), and the control of lipid status by statins may help to stop the progression of NAFLD. We hypot...
Oxidative stress and inflammation contribute to the pathogenesis and progression of nonalcoholic fatty liver disease (NAFLD), and the control of lipid status by statins may help to stop the progression of NAFLD. We hypothesized that the addition of antioxidant vitamins C and E to atorvastatin therapy is associated with improved serum enzyme antioxidant status. NAFLD-related serum parameters and the activity of antioxidant enzymes, before and after 3 months of treatment, were determined in patients receiving atorvastatin alone or atorvastatin plus antioxidants. Compared to healthy controls, the patients, before receiving therapy, had increased catalase and glutathione reductase, with no significant difference in glutathione peroxidase activity. After the treatment, the levels of all three antioxidant markers were reduced to the same degree in both groups of patients, indicating therapy-induced lower level of reactive oxygen species production and/or improved nonenzymatic antioxidant mechanisms. Both therapies led to the normalization of the serum lipid profile and aminotransferase levels in the patients, but the reduction in CRP, although significant, did not reduce levels to those of the controls. The obtained results favor the notion that therapy with atorvastatin alone is equally efficient during the early stages of NAFLD, regardless of the addition of antioxidant vitamins. This trial is registered with TCTR20180425001.
Astragalin: A Bioactive Phytochemical with Potential Therapeutic Activities.
Riaz A, Rasul A, Hussain G … +7 more , Zahoor MK, Jabeen F, Subhani Z, Younis T, Ali M, Sarfraz I, Selamoglu Z
Adv Pharmacol Sci · 2018 · PMID 29853868 · Full text
Natural products, an infinite treasure of bioactive chemical entities, persist as an inexhaustible resource for discovery of drugs. This review article intends to emphasize on one of the naturally occurring flavonoids, a...
Natural products, an infinite treasure of bioactive chemical entities, persist as an inexhaustible resource for discovery of drugs. This review article intends to emphasize on one of the naturally occurring flavonoids, astragalin (kaempferol 3-glucoside), which is a bioactive constituent of various traditional medicinal plants such as . This multifaceted compound is well known for its diversified pharmacological applications such as anti-inflammatory, antioxidant, neuroprotective, cardioprotective, antiobesity, antiosteoporotic, anticancer, antiulcer, and antidiabetic properties. It carries out the aforementioned activities by the regulation and modulation of various molecular targets such as transcription factors (NF-B, TNF-, and TGF-1), enzymes (iNOS, COX-2, PGE2, MMP-1, MMP-3, MIP-1, COX-2, PGE-2, HK2, AChe, SOD, DRP-1, DDH, PLC1, and GPX), kinases (JNK, MAPK, Akt, ERK, SAPK, IB, PI3K, and PKC2), cell adhesion proteins (E-cadherin, vimentin PAR-2, and NCam), apoptotic and antiapoptotic proteins (Beclin-1, Bcl-2, Bax, Bcl-x, cytochrome c, LC3A/B, caspase-3, caspase-9, procaspase-3, procaspase-8, and IgE), and inflammatory cytokines (SOCS-3, SOCS-5, IL-1, IL-4, IL-6, IL-8, IL-13, MCP-1, CXCL-1, CXCL-2, and IFN-). Although researchers have reported multiple pharmacological applications of astragalin in various diseased conditions, further experimental investigations are still mandatory to fully understand its mechanism of action. It is contemplated that astragalin could be subjected to structural optimization to ameliorate its chemical accessibility, to optimize its absorption profiles, and to synthesize its more effective analogues which will ultimately lead towards potent drug candidates.
Antibacterial Activity of Two Flavans from the Stem Bark of .
Guyasa B, Melaku Y, Endale M
Adv Pharmacol Sci · 2018 · PMID 29853867 · Full text
Vatke is one of the medicinal plants used traditionally for treatment of intestinal tape worm, dysmenorrheal, bacterial, and fungal infections. Phytochemical screening test of the dichloromethane/methanol (1 : 1) and met...
Vatke is one of the medicinal plants used traditionally for treatment of intestinal tape worm, dysmenorrheal, bacterial, and fungal infections. Phytochemical screening test of the dichloromethane/methanol (1 : 1) and methanol extracts revealed the presence of phenols, alkaloids, tannins, and flavonoids whereas terpenoids, glycoside, and phytosterols were absent. Silica gel column chromatographic separation of the methanol extract afforded 3,5,7,3',4'-pentahydroxyflavan, named epicatechin (), along with a close flavan derivative (). Structures of the compounds were elucidated by spectroscopic techniques (1D and 2D NMR, FTIR, and UV-Vis). The crude extracts and isolated compounds were screened for antibacterial activity against strains of , , , , and . Epicatechin () exhibited comparable antibacterial activity against and (15 and 12 mm zone of inhibition, resp.) to that of the control antibiotic gentamicin, with zone of inhibition of 15 and 12 mm, respectively, at a concentration of 20 g/mL.
Efficacy of , , and Cream on the Skin Wound Infected with MRSA.
Prakoso YA, Setiyo Rini C, Wirjaatmadja R
Adv Pharmacol Sci · 2018 · PMID 29849604 · Full text
The tropical area has a lot of herbal medicines such as (AV), (AC), and (SM). All the three have a unique potential effect as an antibacterial and wound-healing promoter. The aim of this study is to explore the role o...
The tropical area has a lot of herbal medicines such as (AV), (AC), and (SM). All the three have a unique potential effect as an antibacterial and wound-healing promoter. The aim of this study is to explore the role of AV, AC, and SM on the skin wound infected with methicillin-resistant (MRSA). Forty-five adult female Sprague Dawley rats weighing 250-300 grams were divided into 5 groups. All the groups were exposed to two round full-thickness punch biopsy and infected with MRSA. The group C was the control group/untreated; group BC was treated with base cream/without extract; group AV was treated with 75% AV cream; group AC was treated with 75% AC cream, and group SM was treated with 75% SM cream. The wounds were observed on days 5, 10, and 15. The healing of skin wounds was measured by a percentage of closure, skin tensile strength, and histopathology. The result showed that AV, AC, and SM have a similar potential effect on healing in the wound that was infected with MRSA compared to the groups C and BC ( < 0.05). It shows that all the three herbal formulations can be used as the alternative therapy to the wound infected with MRSA.
Synthesis and Pharmacological Valorization of Derivatives of 4-Phenyl-1,5-Benzodiazepin-2-One.
Nguema Ongone T, Achour R, El Ghoul M … +6 more , El Ouasif L, Taghzouti K, El Jemli M, Cherrah Y, Alaoui K, Zellou A
Adv Pharmacol Sci · 2018 · PMID 29808085 · Full text
The objective of our work is to make a pharmacological study of molecules derived from 4-phenyl-1,5-benzodiazepin-2-one carrying long chains so that they have a structure similar to surfactants, with the benzodiazepine a...
The objective of our work is to make a pharmacological study of molecules derived from 4-phenyl-1,5-benzodiazepin-2-one carrying long chains so that they have a structure similar to surfactants, with the benzodiazepine as a hydrophilic head and a carbon chain as a hydrophobic tail. First, we studied the acute toxicity of the above mentioned 4-phenyl-1,5-benzodiazepin-2-one derivatives. This study was conducted according to OECD 423 guidelines in female mice and revealed that these compounds are nontoxic. We then assessed the psychotropic effects of our products on the central nervous system (CNS). The results obtained show that 4-phenyl-1,5-benzodiazepin-2-one has no sedative effect at therapeutic doses of 100 and 200 mg/kg. On the other hand, its long-chain derivatives possess them. Moreover, all these products have no cataleptic and hypnotic effects at the doses studied. But at 100 mg/kg, these compounds all have the ability to significantly prolong the hypnotic effect of thiopental sodium.
Studies on the Dual Cytotoxicity and Antioxidant Properties of Extracts and Its Main Constituent Berberine.
El Khalki L, Tilaoui M, Jaafari A … +2 more , Ait Mouse H, Zyad A
Adv Pharmacol Sci · 2018 · PMID 29805448 · Full text
The present study attempts to investigate the cytotoxic activity of ethanol and ethyl acetate extracts of the Moroccan and its major component berberine, together with exploring their antioxidant properties. It also con...
The present study attempts to investigate the cytotoxic activity of ethanol and ethyl acetate extracts of the Moroccan and its major component berberine, together with exploring their antioxidant properties. It also consists of studying the combination effect of berberine and S-nitroso-N-acetylpenicillamine (SNAP), a nitric oxide (NO) donor, against the human breast adenocarcinoma cell line (MCF-7). Using the MTT assay, we report a differential cytotoxic effect of ethanol and ethyl acetate extracts since the ethanol extract is more cytotoxic than the ethyl acetate one, with IC = 3.54 μg/mL and 596.71 μg/mL, respectively. Interestingly, no cytotoxic effect was observed against normal cells. Furthermore, these extracts showed a remarkable antioxidant activity as measured by the DPPH free radicals scavenging assay. In fact, the IC values are 69.65 μg/mL and 77.75 μg/mL for the ethanol and ethyl acetate extracts, respectively. In addition, several concentrations of berberine, when combined with the NO donor used at IC, induced a synergistic cytotoxic activity at concentrations ranging from 8.40 μM to 33.60 μM, as revealed by the combination index values, using the Chou-Talalay method. However, at the other concentrations tested, an antagonistic effect was observed. The observed cytotoxicity was related to apoptosis induction as demonstrated by the annexin-V-streptavidin FITC-staining analysis.
Antibacterial and Antioxidant Compounds from the Flower Extracts of .
Habtamu A, Melaku Y
Adv Pharmacol Sci · 2018 · PMID 29755517 · Full text
is traditionally used in Ethiopia to treat various diseases. This prompted us to isolate bioactive compounds from the flowers of this plant. The CHCl extract after silica gel column chromatography has led to the isolatio...
is traditionally used in Ethiopia to treat various diseases. This prompted us to isolate bioactive compounds from the flowers of this plant. The CHCl extract after silica gel column chromatography has led to the isolation of two compounds identified as tricosane and vernolide , while the acetone extract furnished isorhamnetin and luteolin . The acetone extract and isorhamnetin significantly scavenged the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical by 91.6 and 94%, respectively. It was also shown that the acetone extract and isorhamnetin inhibited lipid peroxidation by 74 and 80%, respectively. The extracts and isolated compounds were also evaluated for their antibacterial activity with the CHCl extract and vernolide showing strong activity against with an inhibition zone of 21 and 19 mm, respectively. On the other hand, the acetone extract and isorhamnetin were active against all bacterial pathogens tested. The work presented herein has demonstrated that vernolide and isorhamnetin had antibacterial activity. The antioxidant activity displayed by the flowers of is accounted to the presence of isorhamnetin. Therefore, the biological activities displayed by the extracts and isolated compounds from this plant corroborate the traditional uses of this plant by the local people against various diseases.
Downregulation of Thromboxane A Receptor Occurs Mainly via Nuclear Factor-KappaB Signaling Pathway in Rat Renal Artery.
Zhang Y, Mi M, Xie YH … +3 more , Wang SW, Edvinsson L, Xu CB
Adv Pharmacol Sci · 2017 · PMID 28775740 · Full text
Thromboxane A (TXA) acts on TXA receptors (TP) to regulate renal artery blood flow and subsequently contributes to the pathogenesis of renal ischemia. The present study was designed to examine if nuclear factor-kappaB (N...
Thromboxane A (TXA) acts on TXA receptors (TP) to regulate renal artery blood flow and subsequently contributes to the pathogenesis of renal ischemia. The present study was designed to examine if nuclear factor-kappaB (NF-B) signaling pathway is involved in the downregulation of TP receptors in rat renal artery. Rat renal artery segments were organ cultured for 6 or 24 h. Downregulation of TP receptors was monitored using myograph (contractile function), real-time PCR (receptor mRNA), and immunohistochemistry (receptor protein). Specific inhibitors (MG-132 and BMS345541) for NF-B signaling pathway were used to dissect the underlying molecular mechanisms involved. Compared to fresh (noncultured) segments, organ culture of the renal artery segments for 24 h induced a significant rightward shift of U46619 (TP receptor agonist) contractile response curves (pEC: 6.89 ± 0.06 versus 6.48 ± 0.04, < 0.001). This decreased contractile response to U46619 was paralleled with decreased TP receptor mRNA and protein expressions in the renal artery smooth muscle cells. Specific inhibitors (MG-132 and BMS345541) for NF-B signaling pathway significantly abolished the decreased TP protein expression and receptor-mediated contractions. In conclusion, downregulation of TP receptors in the renal artery smooth muscle cells occurs mainly via the NF-B signaling pathway.
Chemical Composition and Cytotoxic and Antibacterial Activities of the Essential Oil of Palau Grown in Morocco.
Oukerrou MA, Tilaoui M, Mouse HA … +3 more , Leouifoudi I, Jaafari A, Zyad A
Adv Pharmacol Sci · 2017 · PMID 28694822 · Full text
The aim of this work is to investigate the cytotoxic and antibacterial effects of the essential oils of Palau, harvested in different regions of Morocco. The chemical profile was established using gas chromatography-ma...
The aim of this work is to investigate the cytotoxic and antibacterial effects of the essential oils of Palau, harvested in different regions of Morocco. The chemical profile was established using gas chromatography-mass spectrometry analysis. The cytotoxic activity against P815, MCF7, and VERO cell lines as well as the normal human peripheral blood mononuclear cells (PBMCs) was evaluated using the MTT assay. Standard, ATCC, strains of bacteria (, , and ) were cultivated in Muller Hinton media. Then, agar disc diffusion, minimum inhibitory concentrations (MICs), and minimal bactericidal concentrations (MBCs) were determined using microdilution method. The essential oils obtained were predominantly composed of -spathulenol (15.61%), Ar-curcumene (14.15%), trans-caryophyllene oxide (14.14%), and neral (10.02%). The results of the assays showed that the cytotoxic effect of the essential oil of was high on P815 and moderate on MCF7 and on VERO cell lines. However, no cytotoxic effect was observed on PBMCs. On the other hand, essential oils showed a significant antimicrobial activity against both Gram-negative and Gram-positive bacteria. MICs ranged between 2.84 and 8.37 mg/ml. Essential oil of leaves possesses significant antibacterial effect and cytotoxic activity against tumor cell lines.
The Effects of Flower Extract on Skin Injuries Induced by Burn in Rats.
Nasiri E, Hosseinimehr SJ, Akbari J … +2 more , Azadbakht M, Azizi S
Adv Pharmacol Sci · 2017 · PMID 28203250 · Full text
. We compared the efficacy of (P) flower extract with that of silver sulfadiazine (SSD) for treating thermal burn injuries in rats. . Ten Wistar rats in each group were topically given base cream, normal saline, cream c...
. We compared the efficacy of (P) flower extract with that of silver sulfadiazine (SSD) for treating thermal burn injuries in rats. . Ten Wistar rats in each group were topically given base cream, normal saline, cream containing 1% SSD, or creams containing 5% or 10% flower extract. The treatments were administered once daily until complete wound healing was observed. The wound area and healing time were assessed. In addition, percentage wound contraction and histopathological characteristics such as neovascularization and collagen formation were determined. The tannin content in extract was determined. . The decrease in the average size of wounds on day 15 of the treatment was higher in rats treated with creams containing extract than in rats treated with cream containing SSD (2.8 ± 0.9 cm versus 8.4 ± 3.2 cm). The wounds completely healed on day 25 of the treatment in rats treated with creams containing flower extract compared with those in rats treated with the other agents. . These results indicated that flower extract promoted wound healing in rats and could be used for managing burn injuries.
Neuroprotection in Glaucoma: Old and New Promising Treatments.
Rusciano D, Pezzino S, Mutolo MG … +3 more , Giannotti R, Librando A, Pescosolido N
Adv Pharmacol Sci · 2017 · PMID 30723498 · Full text
Glaucoma is a major global cause of blindness, but the molecular mechanisms responsible for the neurodegenerative damage are not clear. Undoubtedly, the high intraocular pressure (IOP) and the secondary ischemic and mech...
Glaucoma is a major global cause of blindness, but the molecular mechanisms responsible for the neurodegenerative damage are not clear. Undoubtedly, the high intraocular pressure (IOP) and the secondary ischemic and mechanical damage of the optic nerve have a crucial role in retinal ganglion cell (RGC) death. Several studies specifically analyzed the events that lead to nerve fiber layer thinning, showing the importance of both intra- and extracellular factors. In parallel, many neuroprotective substances have been tested for their efficacy and safety in hindering the negative effects that lead to RGC death. New formulations of these compounds, also suitable for chronic oral administration, are likely to be used in clinical practice in the future along with conventional therapies, in order to control the progression of the visual impairment due to primary open-angle glaucoma (POAG). This review illustrates some of these old and new promising agents for the adjuvant treatment of POAG, with particular emphasis on forskolin and melatonin.
Phytochemical and Pharmacological Review of (Lindl.) Schlechter.
Osafo N, Mensah KB, Yeboah OK
Adv Pharmacol Sci · 2017 · PMID 29750083 · Full text
ETHNOPHARMACOLOGICAL RELEVANCE: is a scrambling thin-stemmed shrub found in Africa. Traditionally in West Africa, it is employed in the treatment of malaria, diarrhea, and respiratory conditions. This review discusses t...
ETHNOPHARMACOLOGICAL RELEVANCE: is a scrambling thin-stemmed shrub found in Africa. Traditionally in West Africa, it is employed in the treatment of malaria, diarrhea, and respiratory conditions. This review discusses the traditional importance as well as the phytochemical, ethnomedical, pharmacological, and toxicological importance of this plant. MATERIALS AND METHODS: Excerpta Medica Database, Google Scholar, Springer, and PubMed Central were the electronic databases used to search for and filter primary studies on . RESULTS: The detailed review of various studies conducted on and some of its constituents gives an important body of proof of its potential therapeutic benefits and also of its use as a source of lead compounds with therapeutic potentials. CONCLUSION: The review on is important in identifying grey areas in the research on this medicinal plant and also provides comprehensive data thus far to continue research on this plant.
Changes in IL-2 and IL-10 during Chronic Administration of Isoniazid, Nevirapine, and Paracetamol in Rats.
Bekker Z, Walubo A, Du Plessis JB
Adv Pharmacol Sci · 2016 · PMID 27990159 · Full text
The aim of this study was to illustrate the initial subclinical drug-induced liver injury and the associated adaptive immune response by monitoring for the changes in plasma IL-2, IL-10, and some cytochrome P450 activity...
The aim of this study was to illustrate the initial subclinical drug-induced liver injury and the associated adaptive immune response by monitoring for the changes in plasma IL-2, IL-10, and some cytochrome P450 activity during chronic administration of nevirapine (NVP), isoniazid (INH), and paracetamol (PAR) in rats without clinical hepatotoxicity. Male Sprague-Dawley (SD) rats were divided into four groups (saline (S), NVP, INH, and PAR) of 25 animals each. The drugs were administered daily for 42 days at therapeutic doses (NVP 200 mg/kg, PAR 500 mg/kg, and INH 20 mg/kg) to the respective groups by oral gavage and five rats per group were sacrificed weekly. All the three drugs induced a subclinical liver injury in the first 2-3 weeks followed by healing, indicating adaption. The liver injury was pathologically similar and was associated with immune stimulation and increased cytochrome P450 activity. NVP- and PAR-induced liver injury lasted up to 14 days while that for INH lasted for 28 days. NVP-induced liver injury was associated with increased IL-2, CD4 count, and CYP3A2 activity, followed by increased IL-10 during the healing phase. In conclusion, the initial drug-induced subclinical liver injury, its spontaneous healing, and the associated adaptive immune response have been demonstrated.
The Methanolic Extract from L. Inhibits Glutamate-Induced Pain and Involves ATP-Sensitive K Channel as Antinociceptive Mechanism.
Sharmin Ani N, Chakraborty S, Moniruzzaman M
Adv Pharmacol Sci · 2016 · PMID 27812367 · Full text
L. is a perennial shrub, belonging to the family Rutaceae. Traditionally, the leaves of this plant are extensively used in treatment of a wide range of diseases and disorders including pain and inflammation. Although res...
L. is a perennial shrub, belonging to the family Rutaceae. Traditionally, the leaves of this plant are extensively used in treatment of a wide range of diseases and disorders including pain and inflammation. Although researchers have revealed the antinociceptive effects of this plant's leaves during past few years, the mechanisms underlying these effects are still unknown. Therefore, the present study evaluated some antinociceptive mechanisms of the methanolic extract of (MEMK) leaves along with its antinociceptive potential using several animal models. The antinociceptive effects of MEMK were evaluated using formalin-induced licking and acetic acid-induced writhing tests at the doses of 50, 100, and 200 mg/kg. In addition, we also justified the possible participations of glutamatergic system and ATP-sensitive potassium channels in the observed activities. Our results demonstrated that MEMK significantly ( < 0.01) inhibited the pain thresholds induced by formalin and acetic acid in a dose-dependent manner. MEMK also significantly ( < 0.01) suppressed glutamate-induced pain. Moreover, pretreatment with glibenclamide (an ATP-sensitive potassium channel blocker) at 10 mg/kg significantly ( < 0.05) reversed the MEMK-mediated antinociception. These revealed that MEMK might have the potential to interact with glutamatergic system and the ATP-sensitive potassium channels to exhibit its antinociceptive activities. Therefore, our results strongly support the antinociceptive effects of leaves and provide scientific basis of their analgesic uses in the traditional medicine.
Thrombus Degradation by Fibrinolytic Enzyme of Stenotrophomonas sp. Originated from Indonesian Soybean-Based Fermented Food on Wistar Rats.
Nailufar F, Tjandrawinata RR, Suhartono MT
Adv Pharmacol Sci · 2016 · PMID 27635131 · Full text
Objective. To evaluate thrombus degrading effect of a fibrinolytic enzyme from food origin Stenotrophomonas sp. of Indonesia. Methods. Prior to animal study, the enzyme safety was tested using cell culture. The effect on...
Objective. To evaluate thrombus degrading effect of a fibrinolytic enzyme from food origin Stenotrophomonas sp. of Indonesia. Methods. Prior to animal study, the enzyme safety was tested using cell culture. The effect on expression of tissue plasminogen activator was also analysed in the cell culture. For in vivo studies, 25 Wistar rats were used: normal control, negative control, treatment groups with crude and semipurified enzyme given orally at 25 mg/kg, and positive control group which received Lumbrokinase at 25 mg/kg. Blood clot in the tail was induced by kappa carrageenan injection at 1 mg/kg BW. Results. Experiment with cell culture confirmed the enzyme safety at the concentration used and increased expression of tPA. Decreasing of thrombus was observed in the positive group down to 70.35 ± 23.11% of the negative control animals (100%). The thrombus observed in the crude enzyme treatment was down to 56.99 ± 15.95% and 71.5 ± 15.7% for semipurified enzyme. Scanning electron microscopy showed clearly that bood clots were found in the animals injected with kappa carrageenan; however, in the treatment and positive groups, the clot was much reduced. Conclusions. Oral treatment of enzyme from Stenotrophomonas sp. of Indonesian fermented food was capable of degrading thrombus induced in Wistar rats.
Pharmacological Evaluation of Naproxen Metal Complexes on Antinociceptive, Anxiolytic, CNS Depressant, and Hypoglycemic Properties.
Hasan MS, Das N, Al Mahmud Z … +1 more , Abdur Rahman SM
Adv Pharmacol Sci · 2016 · PMID 27478435 · Full text
Purpose. The present study was designed to investigate the antinociceptive, anxiolytic, CNS depressant, and hypoglycemic effects of the naproxen metal complexes. Methods. The antinociceptive activity was evaluated by ace...
Purpose. The present study was designed to investigate the antinociceptive, anxiolytic, CNS depressant, and hypoglycemic effects of the naproxen metal complexes. Methods. The antinociceptive activity was evaluated by acetic acid-induced writhing method and radiant heat tail-flick method while anxiolytic activity was evaluated by elevated plus maze model. The CNS depressant activity of naproxen metal complexes was assessed using phenobarbitone-induced sleeping time test and the hypoglycemic test was performed using oral glucose tolerance test. Results. Metal complexes significantly (P < 0.001) reduced the number of abdominal muscle contractions induced by 0.7% acetic acid solution in a dose dependent manner. At the dose of 25 mg/kg body weight p.o. copper, cobalt, and zinc complexes exhibited higher antinociceptive activity having 59.15%, 60.56%, and 57.75% of writhing inhibition, respectively, than the parent ligand naproxen (54.93%). In tail-flick test, at both doses of 25 and 50 mg/kg, the copper, cobalt, silver, and zinc complexes showed higher antinociceptive activity after 90 minutes than the parent drug naproxen. In elevated plus maze (EPM) model the cobalt and zinc complexes of naproxen showed significant anxiolytic effects in dose dependent manner, while the copper, cobalt, and zinc complexes showed significant CNS depressant and hypoglycemic activity. Conclusion. The present study demonstrated that copper, cobalt, and zinc complexes possess higher antinociceptive, anxiolytic, CNS depressant, and hypoglycemic properties than the parent ligand.
MDMA Impairs Response to Water Intake in Healthy Volunteers.
Baggott MJ, Garrison KJ, Coyle JR … +4 more , Galloway GP, Barnes AJ, Huestis MA, Mendelson JE
Adv Pharmacol Sci · 2016 · PMID 27403159 · Full text
Hyponatremia is a serious complication of 3,4-methylenedioxymethamphetamine (MDMA) use. We investigated potential mechanisms in two double-blind, placebo-controlled studies. In Study 1, healthy drug-experienced volunteer...
Hyponatremia is a serious complication of 3,4-methylenedioxymethamphetamine (MDMA) use. We investigated potential mechanisms in two double-blind, placebo-controlled studies. In Study 1, healthy drug-experienced volunteers received MDMA or placebo alone and in combination with the alpha-1 adrenergic inverse agonist prazosin, used as a positive control to release antidiuretic hormone (ADH). In Study 2, volunteers received MDMA or placebo followed by standardized water intake. MDMA lowered serum sodium but did not increase ADH or copeptin, although the control prazosin did increase ADH. Water loading reduced serum sodium more after MDMA than after placebo. There was a trend for women to have lower baseline serum sodium than men, but there were no significant interactions with drug condition. Combining studies, MDMA potentiated the ability of water to lower serum sodium. Thus, hyponatremia appears to be a significant risk when hypotonic fluids are consumed during MDMA use. Clinical trials and events where MDMA use is common should anticipate and mitigate this risk.
A Review on Medicinal Properties of Orientin.
Lam KY, Ling AP, Koh RY … +2 more , Wong YP, Say YH
Adv Pharmacol Sci · 2016 · PMID 27298620 · Full text
Medicinal plants continue to play an important role in modern medications and healthcare as consumers generally believe that most of them cause fewer or milder adverse effects than the conventional modern medicines. In o...
Medicinal plants continue to play an important role in modern medications and healthcare as consumers generally believe that most of them cause fewer or milder adverse effects than the conventional modern medicines. In order to use the plants as a source of medicinal agents, the bioactive compounds are usually extracted from plants. Therefore, the extraction of bioactive compounds from medicinal plants is a crucial step in producing plant-derived drugs. One of the bioactive compounds isolable from medicinal plants, orientin, is often used in various bioactivity studies due to its extensive beneficial properties. The extraction of orientin in different medicinal plants and its medicinal properties, which include antioxidant, antiaging, antiviral, antibacterial, anti-inflammation, vasodilatation and cardioprotective, radiation protective, neuroprotective, antidepressant-like, antiadipogenesis, and antinociceptive effects, are discussed in detail in this review.
Radical-Scavenging Activity and Ferric Reducing Ability of Juniperus thurifera (L.), J. oxycedrus (L.), J. phoenicea (L.) and Tetraclinis articulata (L.).
El Jemli M, Kamal R, Marmouzi I … +3 more , Zerrouki A, Cherrah Y, Alaoui K
Adv Pharmacol Sci · 2016 · PMID 27293428 · Full text
Objective. The aim of this work is to study and compare the antioxidant properties and phenolic contents of aqueous leaf extracts of Juniperus thurifera, Juniperus oxycedrus, Juniperus Phoenicea, and Tetraclinis articula...
Objective. The aim of this work is to study and compare the antioxidant properties and phenolic contents of aqueous leaf extracts of Juniperus thurifera, Juniperus oxycedrus, Juniperus Phoenicea, and Tetraclinis articulata from Morocco. Methods. Antioxidant activities of the extracts were evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical-scavenging ability, Trolox equivalent antioxidant capacity (TEAC), and ferric reducing antioxidant power (FRAP) assays. Also the total phenolic and flavonoids contents of the extracts were determined spectrophotometrically. Results. All the extracts showed interesting antioxidant activities compared to the standard antioxidants (butylated hydroxytoluene (BHT), quercetin, and Trolox). The aqueous extract of Juniperus oxycedrus showed the highest antioxidant activity as measured by DPPH, TEAC, and FRAP assays with IC50 values of 17.91 ± 0.37 μg/mL, 19.80 ± 0.55 μg/mL, and 24.23 ± 0.07 μg/mL, respectively. The strong correlation observed between antioxidant capacities and their total phenolic contents indicated that phenolic compounds were a major contributor to antioxidant properties of these plants extracts. Conclusion. These results suggest that the aqueous extracts of Juniperus thurifera, Juniperus oxycedrus, Juniperus phoenicea, and Tetraclinis articulata can constitute a promising new source of natural compounds with antioxidants ability.
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