Notes

Considering Simple Internet Connects regarding Risk Models for Scientific Employ: Initial Review Research.
Tumor necrosis factor alpha (TNFα) is a relevant clinical target for the treatment of chronic inflammatory diseases. Currently, only few small molecules are known as direct inhibitors of TNFα. To date, none of these molecules has shown both an efficient activity and a low toxicity to be considered for clinical trials. The SPD304 is considered as a reference of direct inhibitors of TNFα because of its well demonstrated mechanism (He et al., 2005). Herein, we provide new insights regarding the drug profile, selectivity and absorption, distribution, metabolism, excretion and toxicity (ADMET) considerations of SPD304 to evaluate its potential as a hit for the structure-based design of novel TNFα inhibitors. ELISA experiments confirmed the inhibition of TNFα/TNF receptor 1 binding (IC50 = 12 μM). Cellular-based assays highlighted the cytotoxicity of SPD304, as well as its ability to inhibit TNFα signaling pathways at non-cytotoxic concentrations. A surface acoustic wave (SAW) experiment highlighted only one binding site with a dissociation constant of 6.1 ± 4.7 nM. SPD304 inhibited the binding of the cytokines like interleukins (IL)-4 and IL-13 to their receptors and showed no direct inhibition on proteins involved in the TNFα pathway. Finally, the thermodynamic solubility and Caco-2 cells permeability of SPD304 were experimentally evaluated and ADMET in silico predictions are also discussed. The physicochemical, pharmacological and ADMET studies of SPD304 have shown that is not an ideal hit for a drug optimization program based on its chemical structure.
Information collected from local traditional healers reported that Eremomastax speciosa (Hochst.) Cufod. has for a long time been used to manage gastric ulcers in many regions of Cameroon and beyond. This traditional use is supported by numerous studies. However, efficacy of this plant has never been tested in case of chronic gastric ulcers associating Helicobacter pylori infection.

This study was designed to investigate curative effects of the aqueous extract of E. speciosa leaves (AEESL) against chronic gastric ulcers associated to Helicobacter pylori infection.

Two experimental methods of chronic gastric ulcers, involving H. pylori infection, were performed using Wistar rats, namely acetic acid-induced ulcers and "unhealed ulcers". E. speciosa extract was tested at three doses (100; 200; 400mg/kg) and at the end of experiments, some in vivo antioxidant parameters were measured, bacterial load in stomach tissue calculated and histopathological examinations performed.

E. speciosa reduced ulcer index sed monotherapy able to efficiently replace/supplement standard antiulcer tri/quadritherapy.
Nowadays, gastrointestinal motility disorders (GMD) have reduced the quality of people's daily life worldwide, but there is still a lack of effective western medicine treatment. Fructus aurantii (FA), a representative regulating-qi herbal medicine, has been widely used to treat GMD in China for thousands of years, but it is not clear that which specific components contribute to the efficacy.

The efficacy differences of various fractions of FA on normal mice and GMD rats were compared, so as to find out the main effective fraction of FA, and to screen the main regulating-qi components based on spectrum-effect relationship and multivariate statistical analysis.

The fingerprints of different fractions of FA were established and main compounds were identified with UHPLC-Q-TOF/MS technique. The promoting gastrointestinal motility activities of FA were evaluated by defecation test, gastric emptying and intestinal propulsion test in mice, and further investigated according to the biochemical analysis of 5-HT, SP, MLT, GAS and VIP in GMD rats' plasma. One-way ANOVA was used to find out the difference of efficacy. The active components were screened through spectrum-effect relationship with PCA-X, Pearson bivariate correlation analysis and OPLS analysis.

Ethyl acetate fraction is the main active fraction, and nine compounds are the major regulating-qi components. The developed spectrum-effect analysis can be used for the screening of bioactive components in natural products with high accuracy and reliability.
Ethyl acetate fraction is the main active fraction, and nine compounds are the major regulating-qi components. The developed spectrum-effect analysis can be used for the screening of bioactive components in natural products with high accuracy and reliability.
Prunella vulgaris L. (P. vulgaris) is a medicinal plant belonging to the Labiatae family, and its dried spikes is called as Xiakucao in China, which is a common traditional Chinese medicine with the activities of clearing the liver and expelling fire, improving eyesight, dispersing nodules and detumescence. Modern pharmacological studies have proved that P. vulgaris has various pharmacological activities such as immunomodulatory, antiviral, antibacterial and anti-insomnia activities.

P. vulgaris have been reported to have anti-insomnia effects. Nevertheless, the pharmacodynamic substance basis of this anti-insomnia effect is still unclear. The aim of this study was to identify the active components responsible for evoking the anti-insomnia effect of P. vulgaris and to evaluate its anti-insomnia effect.

In this study, we proposed a method combined with pharmacodynamic experiments, extraction and enrichment of chemical components, and the plasma pharmacochemistry to screen out the anti-insomnia componentsactive ingredients responsible for evoking the anti-insomnia effect of P. vulgaris. The three compounds of P. Guanidine vulgaris may help develop one or more drugs to prevent or treat insomnia. Further investigations are recommended to define the mechanism of the anti-insomnia activity of P. vulgaris.
Cissus quadrangularis L. is a perennial herb of the Vitaceae family and is utilized comprehensively as a medicinal herb in most tropical regions by various names. This herb is documented to possess a wide-ranging ethnomedicinal uses in malaria, fever, epilepsy, gout, piles, skin diseases, colic, etc. AIM OF THE REVIEW A organized summary of the botany, traditional uses, phytochemistry, pharmacology, toxicology, available marketed formulations and filed patents were presented to explore the future therapeutic potential and scientific potential of this herb.

For a review of the literature, various databases were searched, including PubMed, EMBASE, and Scopus etc. From, total 408 records of this herb, we have screened 155 articles consist of desired information and available as full text. Present manuscript is structured from comprehensive information on this herb from screened 155 records. Plant taxonomy was confirmed to the database "The Plant List".

Phytochemical assessment as a whole indicated the presence of flavonoids, triterpenoids, alkaloids, saponins, iridoids, stilbenes, vitamins, steroids, and glycosides.
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