ABSTRACT
Dermatophytosis is a contagious fungal disease among animal communities. The major concerns of dermatophytosis are cost of treatment, difficulty of control, and the public health consequences. The objective of the present study was to compare the clinical efficacy of Sumaq and Neem extract cream with that of traditional treatments, eniloconazole and glycerine iodine, on dermatophytosis in Arabian horses. For this purpose, 37 Arabian horses with dermatophytosis had been used. Fungal isolation and identification for each horse were carried out by standard microbiological procedures. Sumaq (Rhus coriaria Linn.) and Neem (Azadirachta indica) seed extracts were selected based on in vitro effectiveness. Horses were randomly allocated into four groups. The first group (n = 8) was treated with glycerine iodine 10% daily for 7 days. The second group (n = 10) was treated using eniloconazole 10% emulsified concentrate four times with 2 days interval. The third group (n = 11) was treated with Neem seeds extract (20% cream) daily for 10 days, and the fourth group (n = 8) was treated with Sumaq extract (5% cream) daily for 10 days. Clinical and mycological evaluations were assessed at 0, 7, 14, 21, and 28 days post-treatment. The Sumaq and eniloconazole were more effective on clinical index score after 7 days of treatment followed by Neem seed 20% cream. At 28 days post-treatment, a complete healing was obtained by Sumaq 5% cream and eniloconazole (median clinical sum score = zero) followed by Neem (median clinical sum score = 1.5). Moreover, Dermatophytes spp. was isolated only from two horses, one from Neem group and the other from glycerin iodine group. The present results indicate that Sumaq 5% and Neem seed extract are effective alternative treatment for dermatophytosis in Arabian horses.
Subject(s)
Azadirachta , Horse Diseases , Plant Extracts , Rhus , Tinea , Animals , Glycerol , Horse Diseases/drug therapy , Horses , Iodine/therapeutic use , Phytotherapy/veterinary , Plant Extracts/therapeutic use , Seeds , Tinea/drug therapy , Tinea/veterinaryABSTRACT
Acute lung injury (ALI) is a universal cause of respiratory failure and death especially after sepsis. The current study evaluates the protective efficacy of acylated catalpol diglycoside (ACD), a plant iridoid glycoside, against lipopolysaccharides (LPS)-induced ALI in rats. ACD prevented LPS-induced elevations in total and differential cell counts and total protein content in bronchoalveolar lavage fluid, lung malondialdehyde content, and serum lactate dehydrogenase activity. Moreover, ACD significantly increased lung glutathione and superoxide dismutase and improved lung histopathology with significant reduction in lung tumor necrosis factor-α (TNF-α) content mediated mainly via inhibition of TNF-α messenger RNA (mRNA) expression. In addition, ACD significantly reduced lung total nitrate concentration content through downregulation of inducible nitric oxide synthase (iNOS) mRNA expression, negating the excessive undesired vasodilatation characteristic to sepsis. In conclusion, the reduction of oxidative stress, amelioration of inflammatory cytokines expression, and antagonism of sepsis associated-excessive vasodilatation are main contributors in ACD's protective effect in LPS-induced ALI in rats.
Subject(s)
Acute Lung Injury/prevention & control , Anti-Inflammatory Agents, Non-Steroidal/therapeutic use , Antioxidants/therapeutic use , Lung/drug effects , Nitric Oxide Synthase Type II/antagonists & inhibitors , Tumor Necrosis Factor-alpha/antagonists & inhibitors , Acute Lung Injury/chemically induced , Acute Lung Injury/metabolism , Acute Lung Injury/pathology , Acylation , Administration, Inhalation , Aerosols , Animals , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Anti-Inflammatory Agents, Non-Steroidal/isolation & purification , Antioxidants/chemistry , Antioxidants/isolation & purification , Biomarkers/metabolism , Gene Expression Regulation/drug effects , Lipid Peroxidation/drug effects , Lipopolysaccharides/administration & dosage , Lipopolysaccharides/toxicity , Lung/immunology , Lung/metabolism , Lung/pathology , Molecular Structure , Nitric Oxide Synthase Type II/genetics , Nitric Oxide Synthase Type II/metabolism , Oxidative Stress/drug effects , Random Allocation , Rats , Rats, Sprague-Dawley , Tumor Necrosis Factor-alpha/genetics , Tumor Necrosis Factor-alpha/metabolismABSTRACT
The cross talk between the over expression of oxygen-free radicals is known as reactive oxygen species (ROS) that is associated with the excessive telomerase activity (TA). Telomerase activity is an invariable finding where human telomerase (hTERT) has been implicated in tumor oxidative stress and redox-mediated malignancy. The hTERT over expression is a novel tumor marker and is promising as a novel class of therapeutic weapons to fight against cancer. A new series of phenylene diamines were designed, synthesized, and evaluated for their in vitro antioxidant as an indicator of inhibiting the oxidative stress tumor. Compounds 3b and 7b proved to be the most active antioxidants with high percentage ABTS inhibition ranged from 89.40% to 88.59% respectively. Molecular modeling studies indicated that the crest configuration of phenylene diamine nucleus with substitutions of trimethoxy benzamido functional proved to be crucial for enhancing the free radical scavenging activity. Molecular modeling exploration indicated the proper binding selectivity of the 3b and 7b to the 3KYL pocket with promising hTERT inhibitors as a hallmark of cancer.
ABSTRACT
A new stilbene, 2',3,4',5,5'-pentahydroxy-cis-stilbene (1), along with 13 known compounds, resveratrol (2), oxyresveratrol (3), norartocarpetin (4), kuwanon C (5), morusin (6), cudraflavone A (7), kuwanon G (8), albafurane C (9), mulberrofuran G (10), 3-O-acetyl-α-amyrin (11), 3-O-acetyl-ß-amyrin (12) ursolic acid-3-O-acetate (13) and uvaol (14), were isolated from the barks of Morus nigra. Compounds 2, 8, 10, 12 and 14 are reported for the first time from this plant. The isolated compounds were elucidated by means of 1D and 2D NMR, UV, IR and MS, as well as by comparison with the literature data. The isolated compounds and the different extracts were evaluated for their potential antioxidant activity using 2,2'-azino-bis-(3-ethylbenzthiazoline-6-sulfonic acid)(+) radical-scavenging capacity assay and compared with ascorbic acid. The new stilbene (1) exhibited remarkable antioxidant capacity with IC50 of 4.69 µM.
Subject(s)
Antioxidants/isolation & purification , Antioxidants/pharmacology , Flavonoids/isolation & purification , Flavonoids/pharmacology , Morus/chemistry , Stilbenes/isolation & purification , Stilbenes/pharmacology , Antioxidants/chemistry , Benzofurans , Benzothiazoles/pharmacology , Egypt , Flavonoids/chemistry , Molecular Structure , Nuclear Magnetic Resonance, Biomolecular , Plant Bark/chemistry , Plant Extracts , Resveratrol , Stilbenes/chemistry , Sulfonic Acids/pharmacology , TerpenesABSTRACT
Dysmenorrhea is a common cause of sickness absenteeism from both classes and work. This study investigated the effect of aromatherapy massage on a group of nursing students who are suffering of primary dysmenorrhea. A randomized blind clinical trial of crossover design was used. In the first treatment phase, group 1 (n = 48) received aromatherapy abdominal massage once daily for seven days prior to menstruation using the essential oils (cinnamon, clove, rose, and lavender in a base of almond oil). Group 2 (n = 47) received the same intervention but with placebo oil (almond oil). In the second treatment phase, the two groups switched to alternate regimen. Level and duration of pain and the amount of menstrual bleeding were evaluated at the baseline and after each treatment phase. During both treatment phases, the level and duration of menstrual pain and the amount of menstrual bleeding were significantly lower in the aromatherapy group than in the placebo group. These results suggests that aromatherapy is effective in alleviating menstrual pain, its duration and excessive menstrual bleeding. Aromatherapy can be provided as a nonpharmacological pain relief measure and as a part of nursing care given to girls suffering of dysmenorrhea, or excessive menstrual bleeding.
ABSTRACT
A new series of phenylcarbamoylbenzoic acid analogs were designed, synthesized, and evaluated for their in vitro antioxidant activity, aiming to find a lead for the treatment of oxidative stress. The target compounds were prepared by substituting the core phenylcarbamoylbenzoic acid moiety with certain functionalities via simple and efficient synthetic strategies. A molecular modeling study was performed to evaluate the recognition of target compounds at the 3MNG binding pocket. The docking data revealed that compounds 8c and 9a selectively bind to the crucial amino acid residues in the active site of 3MNG. The in vitro antioxidant activity was determined by ABTS antioxidant assay. Compounds 8c, 9a, and 9b showed high antioxidant activity and are thus promising as potent antioxidant leads.
Subject(s)
Antioxidants/pharmacology , Benzoates/pharmacology , Models, Molecular , Oxidative Stress/drug effects , Amino Acids/chemistry , Antioxidants/chemical synthesis , Antioxidants/chemistry , Benzoates/chemical synthesis , Benzoates/chemistry , Drug Design , Humans , Molecular Docking Simulation , Structure-Activity RelationshipABSTRACT
This study aimed to evaluate the effect of betulinic acid (BA) on acute lung damage induced by bacterial endotoxin (lipopolysaccharide, LPS) in male Sprague-Dawley rats and explore its possible mechanisms. Oral administration of 25 (mg/kg) BA started 7 days before LPS or saline nasal installation. Twenty-four hours after LPS or saline installation, samples of lung tissues were collected for determination of level of lipid peroxidation (MDA), reduced glutathione (GSH), superoxide dismutase (SOD), and expression of tumor necrosis-α (TNF-α), transforming growth factor-ß1 (TGF-ß1) and inducible nitric oxide synthase (iNOS). Histopathology was done to examine pathological changes in lungs. Wet/dry (W/D) ratio and capillary protein leakage were also determined. Bronchoalveolar lavage (BAL) fluid was carried out for quantification of airway cellular inflammation and nitrate/nitrite (NOx) level. In comparison to BAL fluid samples from control animals, LPS-stimulated animals exhibited a higher count of the inflammatory cells and increased NOx levels. Lungs from LPS-treated animals showed increased lipid peroxidation, altered activities of antioxidant enzymes (GSH and SOD) and increased expression of TNF-α, TGF-ß1 and iNOS in comparison to lungs from control animals. LPS installation-induced pulmonary edema, manifested by significant increase in lung W/D ratio and Evans blue extravasation in lung tissue. This was supported by the histopathological examination which revealed markedly inflamed lung in LPS-treated animals. Treatment with BA was found to significantly attenuate all these alterations. The present results suggest that BA is endowed with antiinflammatory and antioxidant properties that protect the lung against the deleterious actions of LPS.
Subject(s)
Neutrophil Infiltration/drug effects , Pneumonia/drug therapy , Triterpenes/therapeutic use , Acute Lung Injury/immunology , Analysis of Variance , Animals , Bronchoalveolar Lavage Fluid/chemistry , Free Radical Scavengers/analysis , Glutathione/analysis , Lipid Peroxidation/drug effects , Lipopolysaccharides/immunology , Lung/chemistry , Lung/pathology , Male , Nitric Oxide/analysis , Nitric Oxide Synthase Type II/analysis , Pentacyclic Triterpenes , Pneumonia/chemically induced , Pulmonary Edema/chemically induced , Rats , Rats, Sprague-Dawley , Superoxide Dismutase/analysis , Transforming Growth Factor beta1/analysis , Triterpenes/pharmacology , Tumor Necrosis Factor-alpha/analysis , Betulinic AcidABSTRACT
Echinacea species are used for beneficial effects on immune function, and various prevalent phytochemicals have immunomodulatory effects. Using a commercial E. purpurea (L.) Moench product, we have evaluated the myelopoietic effect on bone marrow of rats treated with various extracts and correlated this with their chemical class composition. Granulocyte/macrophage-colony forming cells (GM-CFCs) from femurs of female Sprague-Dawley rats were assessed at 24 h after 7 daily oral treatments. A 75% ethanolic extract at 50 mg dried weight (derived from 227 mg aerial parts) per kg body weight increased GM-CFCs by 70% but at 100 mg/kg was without effect. Ethanolic extracts from aerial parts of E. angustifolia DC. var. angustifolia and E. purpurea from the USDA North Central Regional Plant Introduction Station increased GM-CFCs by 3- and 2-fold, respectively, at 200 mg/kg (~1400 mg/kg plant material). Extract from another USDA E. angustifolia was inactive. Proton and APT NMR, MS, and TLC indicated alkylamides and caffeic-acid derivatives (CADs) present in ethanolic extracts of both the commercial and USDA-derived material. Cichoric and caftaric acids were prominent in both E. purpurea ethanolic extracts but absent in E. angustifolia. Aqueous extract of the commercial material exhibited polysaccharide and CAD signatures and was without effect on GM-CFCs. A methanol-CHCl3 fraction of commercial source, also inactive, was almost exclusively 1:4 nonanoic: decanoic acids, which were also abundant in commercial ethanolic extract but absent from USDA material. In conclusion, we have demonstrated an ethanolextractable myelostimulatory activity in Echinacea aerial parts that, when obtained from commercial herbal supplements, may be antagonized by medium-chain fatty acids presumably derived from a non-plant additive.
Subject(s)
Amides/pharmacology , Caffeic Acids/pharmacology , Echinacea/chemistry , Myelopoiesis/immunology , Plant Extracts/pharmacology , Administration, Oral , Amides/chemistry , Amides/isolation & purification , Animals , Bone Marrow/drug effects , Bone Marrow/metabolism , Caffeic Acids/chemistry , Caffeic Acids/isolation & purification , Chromatography, High Pressure Liquid , Colony-Forming Units Assay , Female , Granulocytes/drug effects , Granulocytes/metabolism , Macrophages/drug effects , Macrophages/metabolism , Magnetic Resonance Spectroscopy , Mass Spectrometry , Medicine, Traditional , Myelopoiesis/drug effects , Plant Components, Aerial/chemistry , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Plants, Medicinal/chemistry , Rats , Rats, Sprague-DawleyABSTRACT
The two major Nicotiana tabacum tobacco cembranoids, (1 S,2 E,4 R,6 R,7 E,11 E)-2,7,11-cembratriene-4,6-diol (1) and its C-4 epimer, exhibit a wide range of interesting biological activities. Although the tumorigenesis inhibition activity of tobacco cembranoids have been known since the mid 1980's, only a limited number of investigations have targeted their optimization and structure-activity relationship. This study reports the isolation of the new (1 S,2 E,4 S,6 E,8 S,11 E)-2,6,11-cembratriene-8- O-methyl-4,8-diol (3) and the known (1 S,2 E,4 R,6 R,7 E,11 E)-2,7,11-cembratriene-4- O-methyl-4,6-diol (2) from fresh N. tabacum leaves. Cembranoid 2 showed good anti-migratory activity against prostate cancer cell lines, and was therefore subjected to microbial transformation and semisynthetic optimization studies. Biotransformation of 2 using the fungal strains Cunninghamella NRRL 5695 and Mucor ramannianus ATCC 9628 afforded new ( 4 and 5) and known ( 6 and 7) metabolites. Semisynthetic esterification, oxidation, epoxidation, and reaction with Lawesson's reagent afforded the new products 8- 14. Cembranoid 2 and its epoxidation product 9 showed potent anti-migratory activities against the highly metastatic human prostate cancer cell lines PC-3M-CT+ (spheroid disaggregation assay) and PC-3 (wound-healing assay).
Subject(s)
Diterpenes/chemistry , Diterpenes/pharmacology , Nicotiana/chemistry , Plant Extracts/chemistry , Plant Extracts/pharmacology , Cell Line, Tumor , Cell Movement/drug effects , Cunninghamella/metabolism , Diterpenes/chemical synthesis , Diterpenes/isolation & purification , Humans , Magnetic Resonance Spectroscopy , Male , Mucor/metabolism , Plant Extracts/isolation & purification , Plant Leaves/chemistry , Prostatic Neoplasms/pathology , Spheroids, Cellular , Structure-Activity RelationshipABSTRACT
Tobacco cembranoids were reported to inhibit tumorigenesis. Biocatalysis of (1S,2E,4R,6R,7E,11E)-2,7,11-cembratriene-4,6-diol (1) using the symbiotic Bacillus sp. NC5, Bacillus sp. NK8, and Bacillus sp. NK7, isolated from the Red Sea sponge Negombata magnifica, afforded two new and four known hydroxylated metabolites 3-8. The use of symbiotic marine bacteria as biocatalysts for bioactive natural product scaffolds is very rare. Cembranoid 1 carbamate analogs 9-11 were prepared by its reaction with corresponding isocyanates. Cembranoid 1 and its bioconversion and carabamate products show anti-invasive activity against the human highly metastatic prostate PC-3M cancer cell line at 10-50 nM doses in Matrigel assay.