SciCombinator

Discover the most talked about and latest scientific content & concepts.

Journal: Pharmaceutical biology

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Context: Curcumin is a yellow-orange polyphenol derived from turmeric [Curcuma longa L. (Zingiberaceaerhizomes)]. Turmeric is a main ingredient of Indian, Persian, and Thai dishes. Extensive studies within the last half a century have demonstrated the protective action of curcumin in many disorders of the body. Objective: This study evaluated the protective effect of curcumin on dexamethasone-induced spermatogenesis defects in mice. Materials and methods: Thirty-two NMRI mice were randomly divided into 4 groups. The first (control) group received 1 mL/day of distilled water by intraperitoneal (i.p.) injection for 7 days. The second group received 200 mg/kg/day of curcumin (Cur) for 10 days. Third group received 7 mg/kg/day of dexamethasone (Dex) for 7 days. Forth group received 200 mg/kg of curcumin for 10 days after dexamethasone treatment. Testicular histopathology, morphometric analysis, head sperm counting, and immunohistochemistry assessments were performed for evaluation of the dexamethasone and curcumin effects. Results: Expression of Bcl-2 was significantly increased in the curcumin + dexamethasone group compared with dexamethasone-treated animals (p < 0.05). Dexamethasone induced spermatogenesis defects including epithelial vacuolizations, sloughing of germ cells, reduction of seminiferous tubule diameter, reduction in the number of sperm heads and significant maturation arrest (p < 0.001). Curcumin + dexamethasone treatment significantly prevented these changes (p < 0.05). Discussion and conclusion: The results of this study demonstrate that curcumin increases the expression of Bcl-2 protein, an important anti-apoptotic factor, and improves the spermatogenesis defects in dexamethasone treated mice. Curcumin has a potent protective effect against the testicular toxicity and might be clinically useful.

Concepts: Gene, Meiosis, Curcuma, Dexamethasone, Turmeric, Curcumin, Zingiberaceae, Thai cuisine

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Context: Several studies have reported the antioxidant activity and potential therapeutic properties of Punica granatum L. (Lythraceae) fruit. Medicinal properties have also been attributed to other parts of P. granatum tree, which are rich in bioactive phytochemicals. Objective: To explore the phytochemical characteristics, in vitro and in vivo antioxidant and in vivo antigenotoxic potential of P. granatum leaf extract (PLE). Materials and methods: The in vitro antioxidant potential of PLE was assessed by DPPH (1,1-diphenyl-2-picrylhydrazyl), ferric reducing antioxidant power (FRAP). Inhibition of lipid peroxidation (LPO) and the total phenolic content of the samples were also determined. Thirty-six male Swiss albino mice were divided into six groups (six animals each). Group 1 (control) and group 2 mice received vehicle and genotoxin alone, respectively. Groups 3, 4 and 5 were pretreated with PLE (400, 600 and 800 mg/kg body weight, respectively) prior to the administration of genotoxin. Group 6 received highest test dose of PLE. DNA damage in the bone marrow cells, hepatic LPO and antioxidants were recorded. Results: Phytochemical analysis of PLE showed the presence of flavonoids, phenols, phytosterols, tannins and carbohydrates. Aqueous PLE demonstrated free radical scavenging activity, reducing power and inhibition of LPO with the EC(50) values of 10.25, 59.88 and 20.05, respectively. A significant protective effect was observed against cyclophosphamide induced DNA damage and inhibition of hepatic LPO with concomitant increase in reduced glutathione (GSH) glutathione S-transferase (GST), superoxide dismutase (SOD) and catalase (CAT) in mice pretreated with PLE. Discussion and conclusion: PLE demonstrated a significant antioxidant and antigenotoxic potential and hence can be a potential natural source in health and medicine.

Concepts: Nutrition, Antioxidant, Bone marrow, Reactive oxygen species, Superoxide dismutase, Glutathione, Antioxidants, Pomegranate

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Context: During the last few decades, the prevalence of obesity in the western world has dramatically increased with epidemic proportions. Hand in hand with this statistic, the incidences of obesity-linked diseases such as diabetes are increasing with pandemic rate. The search for novel drugs and nutritional intervention approaches for obesity is now of significant importance. Objective: The anti-obesity potential of eriodictyol (ERD) and its close structural analogue, sigmoidin A (SGN), were evaluated. SGN was isolated from Erythrina abyssinica Lam. ex DC. (Fabaceae). Materials and methods: Concentrations between 300 and 0.1 µM of test samples and reference drugs made in three-fold dilutions were tested for enzyme inhibitory effects. The major obesity target, pancreatic lipase, was used to test the anti-obesity potential while the selective effects of the compounds were determined through assessments of effects on α-glucosidase. Results: The inhibitory effect of SGN on pancreatic lipase (IC(50), 4.5 ± 0.87 µM) was 30-times greater than that of ERD (IC(50), 134 ± 19.39 µM) while their effect on α-glucosidase enzyme was comparable (IC(50) value of 62.5 ± 9.47 and 57.5 ± 13.15 µM). The anti-obesity drug, orlistat, inhibited pancreatic lipase with an IC(50) value of 0.3 ± 0.04 µM, while the anti-diabetic drug, acarbose, inhibited α-glucosidase with an IC(50) value of 190.6 ± 16.05 µM. Discussion: Although less active than the standard anti-obesity drug, orlistat, the observed activity indicated that prenylation of the flavonoid skeleton potently enhances anti-lipase activity. Conclusion: Such groups of flavonoids need to be further investigated for their therapeutic and nutritional benefit in combating obesity problems.

Concepts: Nutrition, Enzyme, Diabetes mellitus, Obesity, Anti-diabetic drug, Flavonoid, Lipase, Pancreatic lipase

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Context: Lycopene is a carotenoid found in tomato, watermelon, pink grapefruit, and guava in high concentration. Dietary intake of lycopene has been proposed to inversely correlate with the risk of cancer. It has also been reported to provide protection against cellular damage caused by reactive oxygen species, which makes it worthwhile to study the effect of lycopene on liver damage in rat model. Objective: In this study, we report the effect of lycopene on 7,12-dimethylbenz[a]-anthracene (DMBA)-induced expression of Bax, Bcl-2, caspases, and oxidative stres biomarkers in the liver. Materials and methods: Lycopene was administered orally at 20 mg/kg body weight for 20 weeks followed by the intraperitoneal injection of DMBA (50 mg/kg body weight) on day 1 and day 30 of the experiment. Control rats received vehicle (olive oil) or DMBA alone. Rats were sacrificed after completion of the treatment. Results: We observed that the levels of Bax, caspase-3, and caspase-9 decreased to 44, 67, and 43%, respectively, and Bcl-2 increased by 80% in DMBA-treated rats. Lycopene reversed the changes in the respective groups, and decreased the level of Bcl-2 to 25%, while increasing the Bax to 42% when compared to DMBA control. Lycopene increased the expression of caspase-3 (82.09%) and caspase-9 (58.96%), and attenuated the level of hepatic malondialdehyde (41%) and 8-isoprostane (40%) when compared to the respective controls. Glutathione (GSH) decreased significantly in DMBA group (15.89%), but reached the normal level in lycopene-treated animals. Hepatic lycopene concentration in treated rats was 8.2 nmol/g tissue. Conclusion: The study reports that lycopene counteracts the hepatic response to DMBA by altering the expression of Bax, Bcl-2, caspases, and oxidative stress biomarkers in animal model.

Concepts: Antioxidant, Apoptosis, Oxidative stress, Oxidative phosphorylation, Reactive oxygen species, Hydrogen peroxide, Glutathione, Lycopene

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Context: Safe and effective antioxidants are regarded as a cornerstone for the prevention and treatment of several types of disorders. Objective: The present study aimed to investigate the antioxidant and anti-glycation properties of branchlet and fruit oils of Cupressus sempervirens L. var. horizontalis (Mill.) Gord. (Cupressaceae). Materials and methods: Essential oils were extracted from the branchlets and fruits of C. sempervirens var. horizontalis using the steam distillation method. A gas chromatography-mass spectrometry method was employed for the compositional analysis of essential oils. In order to evaluate antioxidant activities of oils at different concentrations (180, 220 and 260 μg mL(-1)), linoleic acid peroxidation test and peroxyl radical mediated hemolysis of red blood cells (RBC) assay were used. Linoleic acid peroxidation was monitored for 4 h and determined during each hour of incubation. Antiglycation effects of oils at 200, 400 and 600 μg mL(-1) were assessed using hemoglobin and insulin glycation assays. Results: Overall, 10 volatile components were identified, amounting for 88.2 and 93.2% of branchlet and fruit oils, respectively. α-Pinene and δ-3-carene were major components of both branchlet (46.2 and 22.7%) and fruit (59.2 and 14.9%) oils. Hemoglobin glycation was inhibited by both branchlet (44.8, 62.6 and 54.0% at 200, 400 and 600 μg mL(-1), respectively) and fruit (41.0, 62.8 and 48.5%) oils. As for the insulin glycation, inhibitory rates were 66.1, 69.2 and 73.8% for branchlet oil, and 80.0, 76.9 and 81.5% for fruit oil (at 200, 400 and 600 μg mL(-1), respectively). RBC hemolysis was also inhibited by both branchlet (49.9, 38.5 and 15.0% at 180, 220 and 260 μg mL(-1), respectively) and fruit (45.9, 38.6 and 25.0%) oil. Finally, the oils mitigated linoleic acid peroxidation which was peaked after 4 h for both branchlet (39.5, 35.6 and 53.4% at 180, 220 and 260 μg mL(-1), respectively) and fruit (47.5, 58.6 and 59.8%) oil. Conclusions: The present findings suggest that essential oils obtained from the branchlets and fruits of C. sempervirens var. horizontalis possess antioxidant and, in particular, antiglycation properties. These activities may find implication in the prevention of diabetic and cardiovascular complications. However, further investigations are required to justify the traditional medical applications of the plant.

Concepts: Red blood cell, Antioxidant, Distillation, Essential oil, Oil, Juniper, Cupressus sempervirens, Cupressaceae

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Abstract Context: Muntingia calabura L. (Muntingiaceae) is a native plant species of the American continent and is widely cultivated in warm areas in Asia, including Malaysia. The plant is traditionally used to relieve pain from gastric ulcers. Objective: This study was designed to determine the antiulcer activity of a methanol extract of M. calabura leaves (MEMC) and the possible mechanisms of action involved. Materials and methods: An acute toxicity study was conducted using a single oral dose of 2000 mg/kg MEMC. The antiulcer activity of MEMC was evaluated in absolute ethanol- and indomethacin-induced gastric ulcer rat models. MEMC was administered orally (dose range 25-500 mg/kg) to rats fasted for 24 h. The animals were pretreated with N(G)-nitro-l-arginine methyl esters (l-NAME) or N-ethylmaleimide (NEM) prior to MEMC treatment to assess the possible involvement of endogenous nitric oxide (NO) and nonprotein sulfhydryl (NP-SH) compounds in the gastroprotective effect of MEMC. Results: As the administered dose did not cause toxicity in the rats, the oral median lethal dose (LD50) of MEMC was >2000 mg/kg in rats. MEMC exerted significant (p < 0.001) gastroprotective activity in the ethanol- and indomethacin-induced ulcer models dose-dependently. Histological evaluation supported the observed antiulcer activity of MEMC. l-NAME and NEM pretreatment significantly (p < 0.05) reversed and abolished the gastroprotective effect of MEMC, respectively. Discussion and conclusion: The results obtained indicate that MEMC has significant antiulcer activity that might involve the participation of endogenous NO and NP-SH compounds. These findings provide new pharmacological information regarding the potential use of M. calabura.

Concepts: Stomach, Toxicology, Peptic ulcer, Acute toxicity, Median lethal dose, Muntingia, Certain safety factor, Sodium nitrite

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Abstract Context: The search for new sources of natural antioxidants from plant material may have beneficial therapeutic potential for those diseases associated with oxidative stress. The medicinal plant Haplophyllum tuberculatum (Forsskal) A. Juss. (Rutaceae) contains phenolic compounds as main phytochemicals; however, there are no reports on its antioxidant properties. Objective: To evaluate antioxidant and cytoprotective potential of ethanol extract of Haplophyllum tuberculatum aerial parts. Materials and methods: Total phenol content was determined using Folin-Ciocalteu reagent; antiradical activity was measured using ORAC assay and the analysis of the major polyphenols was carried out using a HPLC-MS method. The antioxidant and cytoprotective effect were also investigated by the MTT assay and DCFH-DA method. The human astrocytoma U373-MG cell line was pretreated with ethanol extract (from 0.025 to 250 µg/mL) for 24 h, prior to 1 mM H2O2 exposure (30 min). Results and conclusion: Total phenol content was 46.2 mg gallic acid/g sample and ORAC value was 1.283 µmol TE/mg sample. Chemical constituents were methoxyflavones, flavonols (mainly quercetin derivatives), cinnamic acids and benzoic acids. In cell system model of oxidative stress, pretreatments with ethanol extract at the concentrations of 2.5, 0.25 and 0.025 µg/mL significantly attenuated H2O2-induced loss in viability by 13.5, 17 and 20.5%, respectively. Furthermore, these ethanol extract concentrations markedly inhibited intracellular ROS production with IC50 0.026 µg/mL. These findings demonstrate the beneficial properties of ethanol extract of Haplophyllum tuberculatum aerial parts, rich in phenolic compounds, as antioxidant and radical scavenger ameliorating ROS-related processes and diseases such as several neurodegenerative disorders.

Concepts: Antioxidant, Oxidative stress, Catechin, Quercetin, Resveratrol, Phenols, Polyphenol antioxidant, Oxygen radical absorbance capacity

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Abstract Context. Cymbopogon winterianus Jowitt ex Bor (Poaceae), known as citronella grass, is an aromatic herbaceous plant and the essential oil extracted from this grass is used in cosmetics, perfumes, hygiene and cleanliness products worldwide. Objective: This study investigated the composition and molluscicidal and larvicidal activities of the essential oil of C. winterianus cultivated in North Brazil. Materials and methods: The oil was obtained by hydrodistillation, analyzed by gas chromatography (GC) and GC-mass spectrometry and then its molluscicidal and larvicidal activities against snails (Biomphalaria glabrata) and hatched larvae of Artemia salina, respectively, were evaluated at concentrations from 10 to 1000 mg/L. Results: The main constituents of oil were citronellal (26.5%), geraniol (16.2%), elemol (14.5%) and citronellol (7.3%). The molluscicidal test revealed significant lethal concentration (LC) values (LC90 = 97.0 mg/L, LC50 = 54.0 mg/L and LC20 = 22.0 mg/L), indicating the presence of molluscicidal compounds in the oil. In addition, the oil showed moderate larvicidal activity (LC50 = 181.0 mg/L) against the larvae of A. salina, which could justify its use in the aquatic environment without affecting other living organisms. Discussion and conclusion: The results suggest that the oil of C. winterianus could be an effective alternative to control schistosomiasis, with an average margin of safety to other living organisms that coexist with snails.

Concepts: DNA, Plant, Crustacean, Gas chromatography, Citronella oil, Citronellol, Cymbopogon, Biomphalaria

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Abstract Context: Citronellal is a monoterpene present in the oil of many species, including Cymbopogon winterianus Jowitt (Poaceae). Objective: The present study investigated the effect of citronellal on inflammatory nociception induced by different stimuli and examined the involvement of the NO-cGMP-ATP-sensitive K(+) channel pathway. Materials and methods: We used male Swiss mice (n = 6 per group) that were treated intraperitoneally with citronellal (25, 50 or 100 mg/kg) 0.5 h after the subplantar injection of 20 μl of carrageenan (CG; 300 µg/paw), tumor necrosis factor-α (TNF-α; 100 pg/paw), prostaglandin E2 (PGE2; 100 ng/paw) or dopamine (DA; 30 μg/paw). The mechanical nociception was evaluated at 0.5, 1, 2 and 3 h after the injection of the agents, using a digital analgesimeter (von Frey). The effects of citronellal were also evaluated in the presence of L-NAME (30 mg/kg) or glibenclamide (5 mg/kg). Results: At all times, citronellal in all doses inhibited the development of mechanical nociception induced by CG (p < 0.001 and p < 0.01) and TNF-α (p < 0.001, p < 0.01, and p < 0.05). The citronellal was able to increase the pain threshold in the DA test (p < 0.001, p < 0.01, and p < 0.05) and in the PGE2 test at all times (p < 0.001 and p < 0.05). L-NAME and glibenclamide reversed the antinociceptive effects of the citronellal at higher doses in the PGE2 test. Discussion and conclusion: These data suggest that citronellal attenuated mechanical nociception, mediated in part by the NO-cGMP--ATP-sensitive K(+) channel pathway.

Concepts: Time, Pain, Prostaglandin E2, Prostaglandin, Citronella oil, Citronellol, Cymbopogon, Citronellal

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Abstract Context: Centella asiatica (L.) Urban (Apiaceae), a valuable herb described in Ayurveda, is used in the indigenous system of medicine as a tonic to treat skin diseases. Objective: Centella asiatica methanol extract and its ethyl acetate, n-butanol and aqueous fraction, were subjected for the evaluation of skin care potential through the in vitro hyaluronidase, elastase and matrix metalloproteinase-1 (MMP-1) inhibitory assay. Materials and methods: The C. asiatica plant was extracted with methanol and fractionated with ethyl acetate, n-butanol and water. The enzymatic activities were evaluated using ursolic acid and oleanolic acid as standards. Isolate molecule asiaticoside was quantified in the crude extract and fractions through high-performance liquid chromatography (HPLC) and structural was characterized by liquid chromatography-mass spectroscopy (LC-MS) and (1)H nuclear magnetic resonance (NMR). Isolated compound was also evaluated for in vitro enzyme assays. Results: Extract exhibited anti-hyaluronidase and anti-elastase activity with IC50 of 19.27 ± 0.37 and 14.54 ± 0.39 µg/mL, respectively, as compared to ursolic acid. Centella asiatica n-butanol fraction (CAnB) and isolated compound showed significant hyaluronidase (IC50 = 27.00 ± 0.43 and 18.63 ± 0.33 µg/mL) and elastase (IC50 = 29.15 ± 0.31 and 19.45 ± 0.25 µg/mL) inhibitory activities, respectively, and also showed significant MMP-1 inhibition (p < 0.05 and p < 0.01). Discussion and conclusion: n-Butanol fraction was found to be most effective among the all fractions from which asiaticoside was isolated and further quantified by HPLC. This work concludes that the asiaticoside from C. asiatica may be a prospective agent for skin care.

Concepts: Nuclear magnetic resonance, Chromatography, High performance liquid chromatography, Acetic acid, Column chromatography, Enzyme assay, Ursolic acid, Oleanolic acid