Safety evaluation and modulatory effects on innate immune system of pyrazoline-derived compounds.

Pyrazolines are compounds that have been studied for their strong biological potential and structure diversity. Several studies demonstrated their biological effectiveness, highlighting their anti-inflammatory potential. This study aimed to evaluate the physicochemical profile, the safety, and the anti-inflammatory effects of four pyrazolines (PH0, PH3, PH4, and PH7).

The anti-inflammatory activity of N-antipyrine-3,4-dichloromaleimide derivatives is due to an immunomodulatory effect on cytokines environment.

Background And Aim: Inflammation is the immune response to a harmful stimulus, and its purpose is to destroy foreign agents so that the affected site can be repair. When uncontrolled or unresolved, inflammation can lead to significant tissue damage. Many classes of compounds are used today as anti-inflammatory drugs.

Anti-inflammatory and anti-hypersensitive effects of the chalcone isocordoin and its semisynthetic derivatives in mice.

Isocordoin (1), a chalcone isolated from different plants, has been found to present a range of interesting biological properties. This study aimed to evaluate the anti-hypersensitive and anti-inflammatory effects of isocordoin (1) and several natural and semisynthetic derivatives (2-10). Initial evaluation of (1), dihydroisocordoin (2) and six semisynthetic derivatives (3-8) in the inhibition of abdominal writhes induced by acetic acid model showed that only isocordoin dimethylether (5) caused more than 70% of inhibition.

Synthetic chalcones as potential tool for acute- and chronic-pain control.

The purpose of this study was to validate the potential anti-hypersensitive activity of two chalcones, (2E)-1-(4-aminophenyl)-3-(4-nitrophenyl)prop-2-en-1-one (ANCh) and N-{4-[(2E)-3-(4-nitrophenyl)prop-2-enoil]phenyl}acetamide (AcANCh), by different models of acute and persistent pain in mice, besides in silico analysis. Molecules computational investigation for prediction of Lipinki's and Veber's rules to determine solubility, % absorption, drug likeness and toxicity liabilities was performed. Male and female C57BL/6 mice (20-30 g, n = 6) were used.

The validation of Calophyllum brasiliense ("guanandi") uses in Brazilian traditional medicine as analgesic by in vivo antinociceptive evaluation and its chemical analysis.

Calophyllum brasiliense is used as anti-inflammatory and analgesic in Brazilian traditional medicine. Thus, the main purpose of this study is to evaluate the antinociceptive effect of the chloroform fraction of C. brasiliense (CFCB) roots and to investigate its main mechanism of action.

Chemical Composition and Antinociceptive Potential of Campomanesia reitziana Fruits.

The methanolic extract from Campomanesia reitziana fruits and the main active principle, identified as 4',6'-dihydroxy-3',5'-dimethyl-2'-methoxy chalcone or dimethyl cardamonin (1), exhibited pronounced antinociceptive effects against two models of pain in mice. Compound 1 caused dose-dependent inhibition of abdominal constrictions, with a calculated ID50 value of 8.1 (6.

Bioactive metabolites from Cnidoscolus souzae and Acmella pilosa.

The bioassay-guided purification of the ethanol extracts of Acmella pilosa and Cnidoscolus souzae, two plants of the native flora of the Yucatan Peninsula used in traditional medicine to treat inflammation and pain, resulted in the identification of rosmarinic acid (1) and caffeic acid (2) as the bioactive metabolites from A. pilosa, and of 7-deoxynimbidiol (4) as the major bioactive metabolite from C. souzae.

The antihypersensitive and antiinflammatory activities of a benzofuranone derivative in different experimental models in mice: the importance of the protein kinase C pathway.

Background: Benzofuranone (BF1) was synthesized and its effects evaluated on mechanical hypersensitivity and paw edema models induced by different agents and on neuropathic pain induced by partial ligation of the sciatic nerve. An attempt was also made to elucidate the mechanism of action.

Methods: Swiss mice were used for the tests.

A magnetic nanogel based on O-carboxymethylchitosan for antitumor drug delivery: synthesis, characterization and in vitro drug release.

This paper studied the synthesis, characterization and use of the magnetic chitosan nanogel for carrying meleimidic compounds. The hydrogel polymer was prepared using O-carboxymethylchitosan, which was crosslinked with epichlorohydrin for subsequent incorporation of iron oxide magnetic nanoparticles. The characterization revealed that the magnetic material comprises about 10% of the hydrogel.

Chemical composition and antinociceptive, anti-inflammatory and antiviral activities of Gallesia gorazema (Phytolaccaceae), a potential candidate for novel anti-herpetic phytomedicines.

Ethnopharmacological Relevance: In traditional medicine, teas made from leaves and bark of Gallesia gorazema are used as antispasmodic, anthelmintic, antihemorrhagic and febrifuge agents. Crude leaves of this plant are also employed as a remedy in the treatment of abscesses, orchitis, gonorrhea and for rheumatic pain relief. this study investigates the presumed antinociceptive and anti-inflammatory activities of leaves and roots Gallesia gorazema (Phytolaccaceae) extracts.

Osteogenic potential of a chalcone in a critical-size defect in rat calvaria bone.

Background: This study describes the bone formation stimulated by the application of a type of chalcone to critical-size defects in rat calvarial bone.

Material And Methods: Sixty female Wistar rats were divided into 6 groups of 10 animals per group: control (no treatment), vehicle (vaseline) and the chalcone (1-phenyl-3-(4-chlorophenyl)-2-propen-1-one) suspended in vaseline at 10%. A critical-size defect of 5 mm was prepared using a trephine in the calvarial bone, after which the treatment was applied, in a single dose, according to the experimental group.

Anti-hyperalgesic activity of corilagin, a tannin isolated from Phyllanthus niruri L. (Euphorbiaceae).

Ethnopharmacological Relevance: Corilagin (β-1-O-galloyl-3,6-(R)-hexahydroxydiphenoyl-D-glucose) is a tannin isolated from Phyllanthus niruri (Euphorbiaceae). This plant is well known for their therapeutic purposes to treat several diseases associated with dolorous process and are used in several ethno-medicines in tropical and subtropical countries.

Aim Of The Study: This study was designed to evaluate the anti-hyperalgesic activity of corilagin using chemically and thermally based nociception models in mice.

Benzofuranones as potential antinociceptive agents: structure-activity relationships.

This work evaluates the antinociceptive properties of benzofuranones using chemically induced models of pain and the hot plate test. All the compounds exhibited significant antinociceptive activity, with 3-[2-(4-chlorophenyl)-2-oxoetil]-2-benzofuran-1(3H)-one (3d) being the most active. According to the application of the Topliss method, the 2π-π(2) parameter was the preponderant one, indicating that the hydrophobicity (π) seems to be more involved in the antinociceptive activity.

New antinociceptive agents related to dihydrosphingosine.

The main objective of this study was to evaluate the antinociceptive activity of three ethylenediamine derivatives and three β-aminoethanol lipidic derivatives structurally related to dihydrosphingosine. These derivatives were selected on the basis of previous results from in vitro and in vivo anti-inflammatory studies. For all of the assayed compounds, an intraperitoneal dose of 3 mg/kg caused pronounced pain inhibition as measured by the acetic acid-induced writhing model in mice.

Synthesis and biological evaluation of N-antipyrine-4-substituted amino-3-chloromaleimide derivatives.

This paper describes the synthesis of new cyclic imides obtained by reaction with N-antipyrine-3,4-dichloromaleimides and different aromatic amines. The analgesic activity of the synthesized compounds was initially investigated against the writhing test in mice, followed by analysis of the most promising compounds in this model and in the formalin-induced model. The results indicate that the compounds containing the electron-withdrawing substituents in the para position of the substitute ring exerted more potent analgesic activity in mice, being much more potent than the prototype N-antipyrine-3,4-dichloromaleimide and some reference drugs.

N-antipyrine-3, 4-dichloromaleimide, an effective cyclic imide for the treatment of chronic pain: the role of the glutamatergic system.

Background: In recent years, cyclic imides have attracted the attention of the scientific community because of their promising therapeutic potential. Studies with the compound N-antipyrine-3,4-dichloromaleimide (NA-3,4-DCM) also demonstrated an antinociceptive effect in formalin or capsaicin models of nociception, and that it reduced acetic acid-induced abdominal writhing in mice.

Methods: In this study, we examined the effects of NA-3,4-DCM on mechanical hypernociception in persistent pain-like behavioral models in mice.

Antinociceptive properties of caffeic acid derivatives in mice.

Ten ester derivatives from caffeic acid were synthesized, and their antinociceptive properties are evaluated in mice. The most active compound, dodecyl ester derivative, exhibited potent and dose-related activity against the writhing test, with a calculated ID(50) value of 15.1 (11.

Antinociceptive activity of a new benzofuranone derived from a chalcone.

Chalcones represent an important group of natural or synthetic compounds with a variety of biological activities including antinociceptive and anti-inflammatory ones. The aim of this work was the synthesis of a new benzofuranone compound and evaluation of its antinociceptive potential in mice. The new benzofuranone 4 was synthesized from chalcone 3.

Antinociceptive activity and preliminary structure-activity relationship of chalcone-like compounds.

Chalcones belong to a class of alpha,beta,-unsaturated aromatic ketones which occur abundantly in nature, especially in plants. They are promising and interesting compounds due to their vast applications in pharmaceuticals, agriculture and industry. Several studies have shown that these compounds exert important biological activities in different experimental models.

Antiproliferative effects of a series of cyclic imides on primary endothelial cells and a leukemia cell line.

The present study describes the cytotoxic properties of a series of 15 cyclic imides observed against different endothelial cells and K562 leukemic cells. Initially, eight structurally unrelated compounds were evaluated against cultured bone marrow endothelial cells (BMEC) and human umbilical vein endothelial cells (HUVEC). Only two imides showed cytotoxic activity at 10 microM.

Synthesis of new 1-phenyl-3-{4-[(2E)-3-phenylprop-2-enoyl]phenyl}-thiourea and urea derivatives with anti-nociceptive activity.

Chalcones or 1,3-diaryl-2-propen-1-ones are known to be useful for treating pain, inflammation, and certain diseases although their uses have not been scientifically verified. Due to the limitations of opioid and NSAID therapy, there is a continuing search for new analgesics. A series of novel new 1-phenyl-3-{4-[(2E)-3-phenylprop-2-enoyl]phenyl}-thiourea and urea derivatives were synthesized and evaluated against writhing test in mice, following the aromatic substitution pattern proposed by Topliss.

Phytochemical and antinociceptive properties of Matayba elaeagnoides Radlk. barks.

A mixture of triterpenes named lupeol (1), alpha-amyrin (2), beta-amyrin (3), and beta-sitosterol (4) has been isolated from the hexane fraction of Matayba elaeagnoides. In addition, scopoletin (5), umbelliferone (6), 3beta-O-D-glycopyranosyl-sitosterol (7) and betulin (8) were isolated from the chloroform fraction. All the structures were identified by spectroscopic techniques in accordance with literature data.

4'-Acetamidochalcone derivatives as potential antinociceptive agents.

Nine acetamidochalcones were synthesized and evaluated as antinociceptive agents using the mice writhing test. Given intraperitoneally all the compounds were more effective than the two reference analgesic drugs (acetylsalicylic acid and acetaminophen) used for comparison. N-{4-[(2E)-3-(4-nitrophenyl)prop-2-enoyl]phenyl}acetamide (6) was the most effective compound and was therefore selected for more detailed studies.

Seasonal and biological variations of Epidendrum mosenii: quantification of 24-methylenecycloartanol using gas chromatography.

Epidendrum mosenii is a Brazilian medicinal plant, traditionally used to treat infective and dolorous processes. The present article reports a comparative study of the chemical and pharmacological aspects of different parts and seasons of this plant. The results demonstrate that 24-methylenecycloartanol (1), one of the main active principles present in this plant, is located practically in all the parts and during all seasons, but it is much more concentrated in the stems when collected in spring and summer.