137 research outputs found

    Intriguing diverse chemistry and unique molecular mechanisms: new medicines with diverse pharmacological activities from cephalopods ink

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    The ink that cephalopods secrete to hide and frighten the enemies contains a treasury rich in bioactive diverse compounds like DOPA, melanin, melanin synthase, tyrosinase, angiotensin converting enzyme, catecholamines, oligopeptides, polyphenols, flavonoids, alkaloids, polysaccharides, fatty acids and minerals. These groups of the aforementioned compounds have promising unique in-vitro and in-vivo biological activities like antioxidant activity, anti-inflammatory, vasopressin, anti-Parkinson, anti-cancer, anticoagulant, antimicrobial, anti-retroviral, anti-ulcerogenic and immune boosting activities. Cephalopods ink can be offered in its raw state or after separation and purification of its chemical constituents for use as natural medicine to treat many diverse diseases

    Unveiling the chemical profiling and remarkable modulation of carbohydrate metabolism by costus root, Dolomiaea costus (Falc.) in streptozotocin (STZ)-induced diabetic rats

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    Ethnopharmacological relevance: Dolomiaea costus (Falc.), formerly Saussurea costus (Falc.) Lipsch., an ayurvedic medicinal plant, has long been recognized and utilized in diverse indigenous systems of medicine for its multifaceted therapeutic properties, including anti-inflammatory, carminative, expectorant, antiarthritic, antiseptic, aphrodisiac, anodyne, and antidiabetic effects. Aim of the study: The potential and underlying mechanisms of D. costus root as an antidiabetic agent were investigated in this study. Additionally, the quantification of phenolic and flavonoid compounds, which dominate the extracts, was of particular interest in order to elucidate their contribution to the observed effects. Materials and methods: High-performance liquid chromatography/electrospray ionization tandem mass spectrometry (HPLC-ESI-MS/MS) was employed to analyze the chemical constituents in D. costus root aqueous extract (DCA) and D. costus root ethanolic extract (DCE). Furthermore, the inhibitory potentials of DCE and its respective fractions as well as DCA against α-amylase, α-glucosidase, and lipase enzymes were assessed. Subsequently, the efficacy of DCA and DCE extracts was evaluated using an established streptozotocin (STZ)-induced diabetic animal model; this involved administering the extracts at doses of 200 and 400 mg/kg bwt. and comparing them with a positive control (glibenclamide (Glib.) at 0.6 mg/kg bwt.). After induction of diabetes (except for negative control), all animals received the treatments orally for 21 days consecutively, followed by the collection of rat serum to assess various parameters including, glycemic and lipid profiles, liver and kidney functions, antioxidant activity, glycolysis, and gluconeogenesis pathways. Results: The results of HPLC-ESI-MS/MS revealed that isochlorogenic acid A (8393.64 μg/g) and chlorogenic acid (6532.65 μg/g) were the predominant compounds in DCE and DCA, respectively. Both extracts exhibited notable antidiabetic properties, as evidenced by their ability to regulate blood glycemic and lipid profiles (glucose, insulin, HBA1C; HDL, TC, TGs), liver enzymes (ALT, ALP, AST), kidney function (urea, creatinine, uric acid), oxidative stress biomarkers (MDA), antioxidant enzymes (CAT, GSH, SOD), as well as glycolysis (glucokinase) and gluconeogenesis (G-6-P, FBP1) pathways. Conclusions: Furthermore, the administration of D. costus extracts significantly mitigated STZ-induced diabetic hyperglycemia. These results can be attributed, at least partially, to the presence of several polyphenolic compounds with potent antioxidant and anti-inflammatory activities

    Dolomiaea costus: an untapped mine of sesquiterpene lactones with wide magnificent biological activities

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    Dolomiaea costus (Falc.) Kasana & A.K. Pandey Family Asteraceae, formerly known as Saussurea costus (Falc.) Lipsch contains a rich treasury of diverse bioactive compounds such as monoterpenes, sesquiterpenes, triterpenes, sterols, cardenolides, flavonoids, coumarins, lignans, phenylpropanoids and alkaloids. The sesquiterpene lactones, costunolide and dehydrocostuslactone in D. costus, possess unique promising in vitro and in vivo biological activities for the prevention and cure of diverse ailments like Parkinson’s disease, oxidative stress, hyperpigmentation, ulcerative colitis, breast cancer, hepatocellular carcinoma, colon cancer, prostate cancer, ovarian cancer, leukemia, stomach cancer, prostate cancer, lung cancer, osteosarcoma, neuroblastoma, allergy, type 2 diabetes, hepatotoxicity, bronchitis, pulmonary fibrosis, thrombosis and various microbial infections. Costunolide and dehydrocostuslactone are potential drug candidates that could lead to the development of new medications for a variety of difficult-to-treat diseases

    inhibitors: A safeguard against hypertension, respiratory distress syndrome, and chronic kidney diseases

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    Hypertension is a serious concern as it is one of the causes of kideny failure and pulmonary fibrosis. An important therapeutic strategy for treating chronic hypertension is to inhibit the angiotensin converting enzyme (ACE). ACE inhibition reduces kidney damage, pulmonary artery pressure, and high blood pressure. Due to their high efficacy and low risk of side effects, natural renin-angiotensin system inhibitors have drawn increasing attention over the past decades. Alkaloids, amino acids, anthocyanidins, flavonoids, glucosinolates, isoflavonoids, phenolic acids, polyphenolics, and triterpenoids are among the bioactive metabolites pocessing an impressive ACE inhibitory activity. Many herbs including Rosmarinus officinalis, Hibiscus sabdariffa, Curcuma longa, Rauwolfia serpentina, Emblica officinalis, Cynara scolymus, Punica granatum, Mucuna pruriens, Capsicum annuum, and Moringa olifera were found having ACE inhibitory activities comparable to captopril and enalpril. These enticing natural ACE inhibitors deserve to be a safeguard medicine against hypertension, respiratory distress syndrome, and chronic kidney diseases. More clinical trials are required before new natural compounds and herbs can be used to treat chronic hypertension and its ramifications, such as respiratory distress syndrome and kidney failure

    A new firewall in the fight against breast cancer: in-vitro and in-silico studies correlating chemistry to apoptotic activity of Otostegia fruticosa

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    Breast cancer is the most devastating disease for women. There is a great demand for new sources to treat this disease. Medicinal plants are an indispensable source of bioactive compounds with wide range of pharmacological activities. In-vitro cytotoxic activity of Otostegia fruticosa methanolic extract against human breast cancer was studied using MCF-7 cell line. The extract showed mildly potent activity (IC50 1⁄4 51 ± 9.836 mg/mL) in comparison to the standard anticancer doxorubicin (IC50 1⁄4 7.467 ± 1.05 mg/mL). Potential compounds responsible for activity have been identified using Molecular Operating Environment (MOE) module on the major compounds detected by HPLC-MS/MS technique against estrogen alpha receptor (ERaþ: PDB ID 2JF9). 3,5-di-O-dicaffeoylquinic acid, hyperoside and rutin showed similar binding and antagonistic interaction with the estrogen alpha receptor as tamoxifen in several poses. The retrieved results confirm that we can add this plant to a powerful arsenal that combats this insidious disease

    A new arsenal of polyphenols to make Parkinson's disease extinct: HPLC-MS/MS profiling, very interesting MAO-B inhibitory activity and antioxidant activity of Otostegia fruticosa

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    Fifteen compounds belong to phenolic acids, derivatives of phenolic acids, iridoids, xanthones and flavonoids were characterized in the methanolic extract of Otostegia fruticosa leaves using HPLC-MS/MS. Extract has been also investigated for its MAO-B inhibitory activity, antioxidant activity, total phenolic and total flavonoid content. The extract exhibited interesting MAO-B inhibitory activity (IC50; 2.24 ± 0.08) compared to the reference compound selegiline (0.55 ± 0.02 mg/mL). It also showed a potent antioxidant activity proven in both DPPH and ORAC assay methods. The extract showed an IC50 of 3.64 ± 1.22 mg/mL in the DPPH test which was significantly lower than that of the standard ascorbic acid which attained an IC50 of 18.3 ± 1.41 mg/mL. Moreover, in the oxygen radical absorbance capacity assay (ORAC) the extract showed a decline in the IC50 to 3.48 ± 1.16 mg/mL as compared to the standard Trolox which exhibited an IC50 of 27.0 ± 13.41

    Review: Beneficial Health Effects of Olive Leaves Extracts

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    The olive leaves are well known for many useful pharmacological effects. Olive leaves extracts have anti-microbial, anti-inflammatory, anti-oxidant anti-hypertensive, anti-hypercholestermic, anti-hyperglycemic, anti-thrombotic, diuretic and anti-tumor properties. In this review article, we have showed huge collective medical activities of olive leaves extracts that can be applied for treating variety of health problems. Keywords: Olive leaves extracts, Polyphenols, Oleuropein, Oleuropeosides, Health benefits.

    Unacylated ghrelin enhances satellite cell function and relieves the dystrophic phenotype in Duchenne muscular dystrophy mdx model

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    Muscle regeneration depends on satellite cells, quiescent precursors that, in consequence of injury or in pathological states such as muscular dystrophies, activate, proliferate, and differentiate to repair the damaged tissue. A subset of satellite cells undergoes self-renewal, thus preserving the satellite cell pool and its regenerative potential. Unacylated ghrelin (UnAG) is a circulating hormone that protects muscle from atrophy, promotes myoblast differentiation, and enhances ischemia-induced muscle regeneration. Here we show that UnAG increases satellite cell activity and stimulates Par polarity complex/p38-mediated asymmetric division, fostering both satellite cell self-renewal and myoblast differentiation. Because of those activities on different steps of muscle regeneration, we hypothesized a beneficial effect of UnAG in mdx dystrophic mice, in which the absence of dystrophin leads to chronic muscle degeneration, defective muscle regeneration, fibrosis, and, at later stages of the pathology, satellite cell pool exhaustion. Upregulation of UnAG levels in mdx mice reduces muscle degeneration, improves muscle function, and increases dystrophin-null satellite cell self-renewal, maintaining the satellite cell pool. Our results suggest that UnAG has significant therapeutic potential for preserving the muscles in dystrophies. This article is protected by copyright. All rights reserved

    Bioactive Cytotoxic Agents and Chemokine Production Inhibitors in LPS-Induced Raw264.7 Macrophage Cell Line from Flowers of Crepis Senecioides

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    Crepis senecioides is one of the endemic plant species found in Libya. The ethanol extract (E) of the flowers was partitioned on silica gel column with dichloromethane affording four compounds. Their structures were elucidated by the physicochemical and spectral data as germanicol acetate (1), 3`,3``butyl, 8`,8``carboxy) di-octyl phethalate (2), taraxasterol (3) and β-sitosterol (4). effect of the tested samples 1 and 2 on the viability of RAW macrophage 264.7 were studied. anti-cancer activity was tested on several human cell lines. Anti-inflammatory effect was also screened. Compound 1 had promising cellular cytotoxicity with IC50 60.26µg/mL on HepG2. Compound 2 had a talented cellular cytotoxicity with IC50 50.18 µg/mL on PC3. Both 1 and 2 exerted alike cytotoxicity with IC50 µg/mL 78.53, 78.14 on PC3 and MCF-7 carcinoma cell lines respectively. The treatment of LPS-stimulated macrophage with 2 led to a highly significant inhibition 45.05% in the nitrite concentration in LPS-stimulated macrophage. Compound 1 had a promising cellular cytotoxicity on HepG2, while 2 exhibited an inhibition on chemokine expression in LPS-induced RAW 264.7 macrophages and had talented cellular cytotoxicity on PC3. Keywords: Crepis senecioide;, Asteraceae; Anti-inflammatory; cytotoxic effect; terpenoids; phethalate derivative

    Metagenomic analysis of fungal taxa inhabiting Mecca region, Saudi Arabia

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    AbstractThe data presented contains the sequences of fungal Internal Transcribed Spacer (ITS) and 18S rRNA gene from a metagenome of the Mecca region, Saudi Arabia. Sequences were amplified using fungal specific primers, which amplified the amplicon aligned between the 18S and 28S rRNA genes. A total of 460 fungal species belonging to 133 genera, 58 families, 33 orders, 13 classes and 4 phyla were identified in four contrasting locations. The raw sequencing data used to perform this analysis along with FASTQ file are located in the NCBI Sequence Read Archive (SRA) under accession numbers: SRR3150823, SRR3144873, SRR3150825 and SRR3150846
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