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Rosmarinus officinalis L. (Rosemary) is a popular herb with reported effectiveness against diarrhea, anxiety and constipation, albeit with limited pharmacological evidence. The current study was aimed at evaluating the therapeutic potential, possible pharmacological mechanisms of action and active constituents of hydro-ethanolic extract of rosemary (Rs.Cr), as potential anti-diarrheal, laxative and anxiolytic agent. Rs.Cr was analyzed through reverse-phase high pressure liquid chromatography (RP-HPLC). Laxative, antidiarrheal, and anxiolytic activities were assessed using in vivo models. Spasmogenic and spasmolytic mechanisms were studied on isolated guinea pig ileum and rabbit jejunum tissues, respectively. Possible role of diosmetin, one of the active constituents of Rs.Cr was also evaluated. RP-HPLC analysis revealed presence of diosmetin, rutin and apigenin in Rs.Cr. Laxative effect was seen at low doses, which was partially reversed in atropinized mice. The spasmogenic mechanism was mediated by cholinergic and histaminergic receptors stimulation. At higher doses, antidiarrheal activity was evident, with reduction in gastrointestinal motility and secretions using charcoal meal and enteropooling assays, respectively. Rs.Cr also showed dose-dependent anxiolytic effect. The antispasmodic mechanisms were mediated by anti-muscarinic and K+ channel opening-like effect (predominant K ATP -dependent). Diosmetin exhibited antidiarrheal and antispasmodic activities, but spasmogenic effect was not seen. Rosemary leaves have dual antidiarrheal and laxative effects, and as well as anxiolytic activity. In addition, the possible modulation of muscarinic and histaminergic receptors, and K ATP channels show it as potential herb to be explored for irritable bowel syndrome. Diosmetin is possibly one of its constituents that contributes to its antidiarrheal activity. [Display omitted] • Hydro-ethanolic extract of rosemary (Rs.Cr) leaves are enriched in flavonoids including diosmetin, rutin and apigenin. • Rs.Cr exhibits anti diarrheal, laxative activities and anxiolytic activities. • The spasmogenic activity is by stimulation of cholinergic and histaminergic receptors. • The Diosmetin, prominent flavonoid identified in Rs.Cr, also showed anti diarrheal and spasmolytic activities. • Rosemary is a potential herb to be explored for IBS. [ABSTRACT FROM AUTHOR]

A new series of (S)-flurbiprofen derivatives 4a–4p and 5a–5n were synthesized with different aromatic or aliphatic aldehydes and ketones to produce Schiff's bases and their structures were confirmed through HR-ESI-MS, 1H, and 13C-NMR spectroscopy. The α-glucosidase inhibitory activities of the newly synthesized compounds were scrutinized, in which six compounds 5k, 4h, 5h, 4d, 4b, and 5i showed potent inhibition in the range of 0.93 to 10.26 µM, respectively, whereas fifteen compounds 4c, 4g, 4i, 4j, 4l, 4m, 4o, 4p, 5c, 5d, 5j, 5l, 5m, 5n and 1 exhibited significant inhibitory activity with IC50 in range of = 11.42 to 48.39 µM. In addition, compounds 5g, 5f, 4k, 4n, and 4f displayed moderate-to-low activities. The modes of binding of all the active compounds were determined through the molecular docking approach, which revealed that two residues, specifically Glu277 and His351 are important in the stabilization of the active compounds in the active site of α-glucosidase. Furthermore, these compounds block the active site with high binding energies (−7.51 to −3.36 kcal/mol) thereby inhibiting the function of the enzyme. [ABSTRACT FROM AUTHOR]

The present study attempted to evaluate and rationalize the medicinal use of the methanolic extract of the fruits of Balanites aegyptiaca (B. aegyptiaca) in the treatment of hyperactive gut disorders. The in vivo, castor oil-induced diarrhea model in mice was followed to test its antidiarrheal effect. To test the antispasmodic effect and to explore its pharmacodynamic details, isolated small intestines (ileum) obtained from rats were selected to provide physiological conditions for the ex vivo assays. In the in vivo assays, the orally administered extract of B. aegyptiaca protected mice from diarrheal drops with resultant percent inhibitions of 40% and 80% at the respective doses of 200 mg/kg and 400 mg/kg, while the highest protection (100%) was observed with a positive control drug, loperamide, at 10 mg/kg. In the ileum, B. aegyptiaca produced an antispasmodic effect in a concentration-dependent manner by inhibiting the carbachol (CCh; 1 µM) and high K+ (80 mM)-evoked spasms with resultant EC50 values of 1.44 mg/mL (1.08–1.78) and 1.27 mg/mL (0.98–1.66), respectively. Papaverine, a known phosphodiesterase enzyme (PDE) inhibitor and blocker of Ca++ channels (CCB), also inhibited both CCh and high K+ induced contractions at comparable EC50 values of 8.72 µM (7.92–9.24) and 8.14 µM (7.62–8.84), respectively. Contrary to the extract and papaverine, verapamil showed distinctly higher potency in regard to inhibiting high K+, compared to CCh-evoked spasms that had EC50 values of 0.16 µM (0.13–0.261) and 2.54 µM (2.28–2.92), respectively. The inhibitory effects of B. aegyptiaca on PDE were further confirmed when the pre-incubated extract shifted the isoprenaline-mediated relaxation curves (CRCs) towards the left, similar to papaverine, whereas the CCB-like effect was confirmed when the pre-incubated tissues with B. aegyptiaca caused deflection in the Ca++ CRCs towards the right, constructed in Ca++ free medium with suppression of the maximum response. Thus, this study provides detailed, mechanistic support for the medicinal use of B. aegyptiaca in the treatment of hyperactive gut disorders. [ABSTRACT FROM AUTHOR]

Underwater discharge plasmas are widely acclaimed for their potential applications in wastewater treatment, biomedical sciences, and industry. This article reports on pre- and post-breakdown characteristics of nanosecond pulsed plasma discharge generated in oxygen–water mixture flowing through a quartz capillary tube. In pre-breakdown region of applied voltage range of 4–4.5 kV, medium capacitance varies between 20 and 26 pF. For applied voltage range of 5–9 kV, a plasma discharge was observed during which the prominent current and voltage peaks show 5–10-ns phase difference. Electron number density was estimated using current density and Stark broadening techniques. It was noted that electron number density estimated from current density values ranges from 0.08 $\times \,\,10^{\mathrm {23 {}}}\,\,\text{m}^{-3}$ to 0.18 $\times \,\,10^{23}\,\,\text{m}^{-3}$ , while the electron number density estimated from Stark broadening of Balmer series hydrogen $H_{\alpha }$ and $H_{\beta }{}$ lines was found between 1.26 $\times \,\,10^{23}\,\,\text{m}^{-3}$ –2.69 $\times \,\,10^{23}\,\,\text{m}^{-3}$ and 1.25 $\times \,\,10^{23}\,\,\text{m}^{-3}$ –2.52 $\times \,\,10^{23}\,\,\text{m}^{-3}$ , respectively. The estimated values of plasma coupling parameter were in the range of 0.031–0.21, indicating the generated plasma to be on the margins of noncoupling ideal plasma to nonideal weakly coupled plasma. Effect of oxygen–water mixture flow direction on discharge stability and other plasma parameters was also monitored. It was observed that plasma discharge was more stable with higher electron number density in the direction of fluid flow. [ABSTRACT FROM AUTHOR]

A series of new para-terphenyls derivatives have been efficiently synthesized by a ligand-free heterogeneous Pd/C-catalyzed two-fold Suzuki–Miyaura coupling reaction. Methyl 5-bromo-2-iodobenzoate was selected to react with a variety of different aryl boronic acids (2a-i). Nine new p-terphenyl derivatives (3a–i) were prepared and the structures were confirmed by several analytical techniques including infrared, spectroscopy, 1H and 13C NMR spectroscopy, mass spectrometry, and in the case of compound 3 b, by X-ray diffraction method. The new derivatives were obtained in very good yields (78–91%). This synthetic facile route is envisioned to improve the preparation of p-terphenyl-based natural products. [ABSTRACT FROM AUTHOR]

Evaluation of CA inhibition activity and the identification of the components of the essential oil of Frankenia pulverulenta (FPEO) and Boerhavia elegans (BEEO) were undertaken for the first time in this study. Twenty-five components were identified using Gas Chromatography/Mass Spectrometry (GC/MS) in the FPEO, representing 92.7 % of the total oil. The major components were β-caryophyllene (32.5 %), δ-cadinene (8.4 %), alloaromadendrene (7.1 %), copaene (6.9 %), and ledol (5.3 %). Similarly, the BEEO contained 13 components representing 92.9 % of the total oil with β-caryophyllene (17.1 %) and β-amyrin (13.7 %) as the major components. The results determined that the FPEO was a rich source of sesquiterpene hydrocarbons (69.8 %), while BEEO contains a higher concentration of aliphatic hydrocarbons (46.4 %). The EOS of both plants were further screened for carbonic anhydrase II (CA-II), and antimicrobial activities. Essential oil of F. pulverulenta exhibited significant CA-II activity with 101.5±2.35 % inhibition, while B. elegans essential oil presented promising bactericidal and fungicidal activities against Escherichia coli (Gramnegative bacteria) and Penicillium simplicissimumi. These results indicate that the essential oil of B. elegans can inhibit the growth of Gram-negative bacteria and fungi. In addition, FPEO significantly inhibited CA and might have the potential to be used for the treatment of CA-related diseases. [ABSTRACT FROM AUTHOR]

Abstract Background The aqueous-methanolic extract of Amaranthus spinosus (A. spinosus Linn.,) whole plant, was studied for its laxative, spasmolytic and bronchodilator activities to validate some of its medicinal uses. Methods The crude extract of A. spinosus was studied in-vivo for bronchodilator and laxative activities and in-vitro using isolated tissue preparations which were mounted in tissue baths assembly containing physiological salt solutions, maintained at 37°C and aerated with carbogen, to assess the spasmolytic effect and to find out the possible underlying mechanisms. Results In the in-vivo experiments in mice, the administration of A. spinosus increased fecal output at doses of 100 and 300 mg/kg showing laxative activity. It also inhibited carbachol-induced bronchospasm in anesthetized rats at 1, 3, 10 and 30 mg/kg indicative of bronchodilator activity. When tested on isolated gut preparations, the plant extract showed a concentration-dependent (0.01-10.0 mg/ml) spasmogenic effect in spontaneously contracting rabbit jejunum and guinea-pig ileum. The spasmogenic effect was partially blocked in tissues pretreated with atropine (0.1 μM). When tested on K+ (80 mM)-induced sustained contractions in isolated rabbit jejunum, the plant extract caused complete relaxation and also produced a shift in the Ca++ concentration-response curves (CRCs) towards right, similar to diltiazem. In rabbit trachea, the plant extract completely inhibited K+ (80 mM) and carbachol (CCh, 1 μM)-induced contractions at 1 mg/ml but pretreatment of tissue with propranolol (1 μM), caused around 10 fold shift in the inhibitory CRCs of the plant extract constructed against CCh-induced contraction. The plant extract (up to 0.3 mg/ml) also increased both force and rate of spontaneous contractions of isolated guinea-pig atria, followed by relaxation at higher concentration (1.0-5.0 mg/ml). The cardio-stimulant effect was abolished in the presence of propranolol, similar to that of isoprenaline. Activity-directed fractionation revealed that the spasmolytic component(s) was separated in the organic fraction, whereas the spasmogenic component was concentrated in the aqueous fraction. Conclusion These results indicate that A. spinosus possesses laxative activity partially mediated through cholinergic action. The spasmolytic effect was mediated through calcium channel blocking (CCB), while bronchodilator activity through a combination of β-adrenergic and CCB pathways, which may explain the traditional uses of A. spinosus in gut and airways disorders.

In the current investigation, the chemical composition of the essential oils (EOs) from the stem and leaves of Acridocarpus orientalis A. Juss. were evaluated by gas chromatography (GC) and gas-chromatography-mass spectrometry (GC-MS). The main volatile constituents identified in the essential oil of stem were rich in methyl 8-pimaren-18-oate (43.8 %), octacosane (5.8 %), heptacosane (4.6 %) and hexacosane (4.1 %), methyl dehydroabietate (3.9 %) and methyl pimar-8(14)-en-18-oate (3.6 %), while tetracosane (16.6 %), heptacosane (16.4 %), docosane (13.9 %), hentriacontane (13.5 %), heneicosane (10.9 %) and α-pinene (7.7 %) were abundant in the EO of leaves. Both essential oils, screened against urease, α-glucosidase and carbonic anhydrase II (CA-II) enzyme inhibitory activities, were found active against CA-II and inactive against urease and α-glucosidase enzymes. The leaves of AO were found more active only against CA-II enzyme having IC50 values of 45.6 ± 1.0 μg/mL than stem (156.3 ± 1.5 μg/mL). The results determined that the EO of leaves could be a promising target for anti-cancer treatment. This is the first report, up to the best of the author's knowledge, on the chemical composition and CA-II activity of this essential oil. [ABSTRACT FROM AUTHOR]

In the last decade the prevalence of diabetes has escalated globally and it is estimated that the number of diabetic people will increase to 642 million by 2040. Although numerous classes of pharmaceutical drugs are available to treat Type ll diabetes, they manifest certain side effects. PTP1B has attracted significant interest as an important therapeutic agent and has been validated to target diabetes and obesity. Fungi, in general, produce secondary metabolites with some amazing chemical and structural diversity and are recognized to be a valuable source for therapeutic molecules. In this review, the focus is on describing the PTP1B effects and their potential as anti-diabetic agents for the various metabolites isolated from fungi. [ABSTRACT FROM AUTHOR]

Background: This study investigated the anticancer potential of the medicinal herb, Cleome droserifolia (CD), a local plant of the Arabian Peninsula. C. droserifolia is traditionally known for its rubefacient, anti-diabetic, anti-oxidant, and anti-inflammatory properties. Methods: Organic fractions of the aerial parts of Cleome droserifolia harvested from the Arabian Peninsula were tested in human breast and cervical cancer cell lines for their anticancer potential. This was accomplished by using biochemical and cellular assays, including MTT, caspase Glo, western blot, and annexin V/propidium iodide-based flow cytometry analyses. Results: Test of the dichloromethane fraction of the methanolic extract of C. droserifolia, (CDD) revealed potent cytotoxic activity (from 70 to 90%) against several human cancer cell lines, including MCF-7, MDA-MB-231, and HeLa. Further characterization of the CDD fraction in MCF-7 cells revealed that it could activate the enzymatic activity of various caspases in a statistically significant manner, and induce cleavage of both caspase 7 and poly ADB ribose polymerase (PARP) proteins, but not the ethyl acetate fraction. Test of the ability of CDD to induce early signs of apoptosis was validated by annexin V/propidium iodide assay using FACS analysis. Induction of apoptosis was completely reversed by the classic pan inhibitor of apoptosis, Z-VAD-FMK, reducing early apoptosis from 29.7 to 0.6%, confirming that CDD could induce caspase-dependent apoptosis. Conclusions: Altogether, our results reveal that C. droserifolia is a valuable medicinal plant with bioactive molecules that can induce apoptosis in human cancer cells. Thus, this plant should be explored further for its potential as an anticancer natural therapy as well as the isolation of novel molecules with anticancer properties. [ABSTRACT FROM AUTHOR]

In this article, we prepared efficient ZnO@MoS2 composites through hydrothermal and solvothermal method for photocatalytic hydrogen evolution. The structural, morphological, surface area and optical properties were investigated using transmission electron microscopy (HR-TEM), X-ray diffractometer (XRD), Brunauer Emmett Teller (BET), UV–visible (UV-vis) absorption and Photoluminescence (PL) emission spectroscopy. The incorporating effect of MoS2 on the photocatalytic performance of ZnO photocatalyst has been studied. The PL emission spectra of prepared composites elucidate that recombination of electron/hole pairs is greatly suppressed owing to the incorporation of MoS2 sheet-like nanostructures. The composite sample (3wt % of MoS2 in ZnO) showed the excellent photocatalytic efficiency when compared to pure photocatalyst. The considerable increase in the efficiency of nanocomposites may be accredited to extended absorption region, favorable band structure, and effective separation of charge carriers, large surface area and the reactive active sites provided by layered structure of MoS2. This study demonstrates that prepared composites could be promising and efficient photocatalysts for the evolution of hydrogen through water-splitting under visible light illumination. [ABSTRACT FROM AUTHOR]

Among medicinal plants, Acridocarpus orientalis (AO) possesses a remarkable anti-cancer potential, possibly because of its anti-oxidant property. In this study, the leaf and stem extracts from AO were assessed to find the bioactive compound with selective anti-cancer properties. The MTT viability and live and dead assays revealed that around 80% and 98% of 4T1 cells survival were declined after 48 h incubation with leaf and stem extracts, respectively. The leaf extract increased stem cell proliferation by 20% whereas the stem extract inhibited around 22% of stem cells proliferation after 48 h treatment. The live and dead assay of MSCs confirmed that 40% of the MSCs died when treated with AO stem extract. On the other hand, there were no dead cells after two days of treatment with the leaf extract. Followed by the induction of cell cycle arrest in G0/G1-phase, the real-time PCR demonstrated apoptosis properties in 4T1 cells through overexpression of Bax and down-regulation of BCL2 genes. Interestingly, within the pure compounds isolated from AO leaf extract, Morin was responsible for the inhibition of 4T1 cells proliferation as well as MSCs expansion, predicting to play an essential role in the treatment of cancer. The promising in vitro anti-cancer and stem cell-inductive properties of morin isolated from AO extract may provide a great potential to produce selective herbal derived drugs. [ABSTRACT FROM AUTHOR]

The bronchodilator effects of Roflumilast "a selective phosphodiesterase type-4 (PDE4)" inhibitor studied in this experimental protocol. The spiral strips of isolated guinea-pig tracheal chains mounted in organ bath and maintained in Krebs solution ventilated with carbogen at 32 °C and in Ca++ restricted krebs solution. PDE inhibitory activity was evaluated by recording dose response curves using inhibitory effect of isoprenaline on CCh induced contractions. For confirmation of PDE inhibition the intracellular cAMP levels were also estimated. Roflumilast resulted a sharp inhibition in contractile responses of carbachol (CCh, 1 µM) and K+ (80 mM) and the results were almost similar to verapamil. In Ca++ restricted Krebs solution, a rightward shift in the Ca++ response curves observed in the tracheal chain strips which were pretreated with Roflumilast (0.001–0.003 mg/mL) and the maximum response was suppressed, similarly as with verapamil. PDE inhibitory effect of Roflumilast evaluated by recording dose-dependent (0.03–0.1 mg/mL) responses, the isoprenaline-induced inhibitory dose response curves shifted leftward similar to papaverine (PDE inhibitor). Pretreatment with Roflumilast exhibited elevated intracellular cAMP levels in tracheal strips. Findings of the experiment conclude bronchodilatory influence of Roflumilast via PDE and Ca++ channel inhibition. Results of current experiment offers comprehensive mechanistic background of Roflumilast in future as therapeutic bronchodilator for hyperactive bronchial airway diseases. [ABSTRACT FROM AUTHOR]

A new a bisflavan-3-ol, boerhavianane (1), was isolated from Boerhavia elegans L. The structure of the flavanol dimer was elucidated by detailed spectroscopic analysis including 1H, 13C NMR, COSY, HMQC, HMBC, and ESI-MS. Boerhavianane (1) was evaluated for its anticancer activity and demonstrated a significant reduction in the viability of breast cancer cells in a concentration-dependent manner with an IC50 value of 38.48 μg/mL. Moreover, boerhavianane (1) was also screened for DPPH antioxidant activity and acetyl cholinesterase, xanthine oxidase, urease, and α-glucosidase enzyme inhibition activities. Preliminary results showed that it exhibited significant inhibition (81.0 ± 2.0%) against urease enzyme, whereas for DPPH radical scavenging it showed moderate activity (75.0 ± 1.5%). [ABSTRACT FROM AUTHOR]

Otostegia fruticosa , a plant belonging to the family Lamiaceae, is endemic to Ethiopia. In Ethiopian traditional medicine, O. fruticosa has been used for the treatment of several respiratory-related disorders. The present study was designed to evaluate the bronchodilatory and antimicrobial activities of O. fruticosa leaves crude extract (Of.Cr). Ex-vivo experiments were conducted on guinea-pig trachea provided with physiological oxygenated buffer solution using emkaBath setup. The crude extract was analyzed by gas chromatography-mass spectrometry. Of.Cr, showed the presence of terpenes, fragrance components, saponins, and higher fatty acids. Of.Cr when tested on contracted tracheal chains with carbamylcholine (CCh, 1 µM) and high K+ (80 mM) produced relaxation by showing higher potency against CCh with incomplete inhibition of high K+. Dicyclomine, used as a positive control, also showed selectively higher potency to inhibit CCh when compared with its effect against K+. In the anticholinergic curves, Of.Cr at 1 mg/mL deflected CCh-induced concentration–response curves (CRCs) competitively to the right like dicyclomine (0.03 µM) and atropine whereas a higher dose of Of.Cr (3 mg/mL) produced a non-parallel shift in the CCh curves like a higher dose of dicyclomine (0.1 µM). In the calcium channel inhibitory assay, Of.Cr at 3 & 5 mg/mL, deflected CRCs of Ca++ to the right like verapamil, used as positive control. Of.Cr, at concentrations (1–3 mg/mL) increases cAMP levels in isolated tracheal homogenates, similar to positive control phosphodiesterase inhibitor (papaverine). When tested for antibacterial activity against standard and clinical strains, Of.Cr was found more active (MIC 475 µg/ml) against S. aureus (NCTC 6571), while the maximum inhibition (MIC 625 µg/ml) was observed by the extract when tested against MRSA. These results determine the mechanistic pathways of the observed bronchodilatory effect of Otostegia fruticosa with a combination of anticholinergic and dual inhibition of phosphodiesterase and voltage-gated Ca++ channels. [ABSTRACT FROM AUTHOR]