Lysionotin exerts antinociceptive effects in various models of nociception induction.

Background: Lysionotin, a natural flavonoid extracted from Maxim (Gesneriaceae), has several pharmacological effects including anti-bacterial, anti-hypertensive and anti-inflammatory effects. However, its analgesic effect has not been investigated. This study aimed to assess the antinociceptive activity of lysionotin using chemically and thermally induced nociception in a mouse model.

New Treatment for Type 2 Diabetes Mellitus Using a Novel Bipyrazole Compound.

2',3,3,5'-Tetramethyl-4'-nitro-2'H-1,3'-bipyrazole (TMNB) is a novel bipyrazole compound with unknown therapeutic potential in diabetes mellitus. This study aims to investigate the anti-diabetic effects of TMNB in a high-fat diet and streptozotocin-(HFD/STZ)-induced rat model of type 2 diabetes mellitus (T2D). Rats were fed HFD, followed by a single low dose of STZ (40 mg/kg).

Understanding the Mechanism Underlie the Antidiabetic Activity of Oleuropein Using Approach.

Background: Oleuropein, the main constituent of olive fruit and leaves, has been reported to protect against insulin resistance and diabetes. While many experimental investigations have examined the mechanisms by which oleuropein improves insulin resistance and diabetes, much of these investigations have been carried out in either muscle cell lines or models two scenarios with many drawbacks. Accordingly, to simplify identification of mechanisms by which oleuropein regulates specific cellular processes, we resort, in the present study, to isolated muscle preparation which enables better metabolic milieu control and permit more detailed analyses.

Co-overexpression of CD36 and FABPpm increases fatty acid transport additively, not synergistically, within muscle.

We aimed to determine the combined effects of overexpressing plasma membrane fatty acid binding protein (FABPpm) and fatty acid translocase (CD36) on skeletal muscle fatty acid transport to establish if these transport proteins function collaboratively. Electrotransfection with either FABPpm or CD36 increased their protein content at the plasma membrane (+75% and +64%), increased fatty acid transport rates by +24% for FABPpm and +62% for CD36, resulting in a calculated transport efficiency of ∼0.019 and ∼0.

Effect of chronic spinal cord injury's severity on sperm parameters in rat: correlation with locomotion deficits.

Objectives: Infertility is one of the major concerns for male patients following spinal cord injury (SCI). Although the severity of the injury has a large impact on extent of infertility, the effect of exact injury extent (with specific affected spinal tracts) on fertility is not studied yet.

Materials And Methods: In the present study, sperm parameters, locomotion scores, and hormonal changes were evaluated following dorsal one third SCI (1/3 SCI), dorsal two third SCI (2/3 SCI), and complete spinal cord transection (TX) at T8 spinal level in male rats.

Severing the ventral funiculus in chronic spinal cord injury has the most deteriorating effect on spermatogenesis in rats.

Sexual dysfunction, following spinal cord injury (SCI), is highly dependent on the extent of injury. SCI disrupts the supraspinal innervation of the reproductive organs; resulting in structural and functional deficits. Relating the extent of SCI to these changes could eventually improve diagnoses and treatment planning of sexual dysfunction following SCI.

Eugenol ameliorates insulin resistance, oxidative stress and inflammation in high fat-diet/streptozotocin-induced diabetic rat.

Background: Eugenol, a phenolic compound present in many plant essential oils, demonstrated anti-diabetic activity but the underlying mechanisms are not fully understood. The aim of the present study was to examine the anti-diabetic, anti-oxidative and the anti-inflammatory effect of eugenol in high-fat-diet (HFD) and streptozotocin (STZ)-induced diabetic rats. Additionally, the effect of eugenol on the insulin sensitivity and on skeletal muscle protein contents of glucose transporter-4 (GLUT4) and AMP-activated protein kinase (AMPK) was investigated.

Antitumor Action of Amygdalin on Human Breast Cancer Cells by Selective Sensitization to Oxidative Stress.

The treatment of MCF-7 and T47D human breast cancer cell lines with amygdalin was able to reduce the growth of both cells, in concentration and time-dependent manners. The potency of this inhibition against MCF-7 and T47D cells produced IC values of 39 and 45 mM, respectively. To investigate the correlation of this inhibition with oxidative stress, an amygdalin treatment of both cell lines was capable of inducing the generation of malondialdehyde (MDA) and oxidized glutathione levels.

Beneficial effects of oleuropein on glucose uptake and on parameters relevant to the normal homeostatic mechanisms of glucose regulation in rat skeletal muscle.

Oleuropein, the main constituents of leaves and fruits of the olive tree, has been demonstrated to exert various therapeutic and pharmacological properties including antidiabetic effect. However, the effectiveness of oleuropein on glucose homeostasis in intact rat skeletal muscle ex vivo has never been explored. Therefore, our current study was carried out to investigate and confirm the beneficial effect of oleuropein (1.

Preventive effect of oleate on palmitate-induced insulin resistance in skeletal muscle and its mechanism of action.

Insulin resistance in skeletal muscle is a feature associated with exposure to an excess of saturated fatty acids such as palmitate. Oleic acid has been shown to blunt palmitate-induced insulin resistance in muscle cells. However, there is no literature available regarding the effect of oleic acid on palmitate-induced insulin resistance in intact muscle.

Inhibitory Effect of Thymoquinone on Testosterone-Induced Benign Prostatic Hyperplasia in Wistar Rats.

This study addresses the possible protective effects of thymoquinone (TQ) against the development of experimentally-induced benign prostatic hyperplasia (BPH) in Wistar rats. Eighteen adult male rats were divided into three groups; the negative control group (n = 6) received vehicle, and two groups received subcutaneous testosterone injection (3 mg/kg). Animals receiving testosterone were randomized to untreated BPH group (n = 6) and BPH + TQ treated group (n = 6, 50 mg/kg orally for 14 days).

Skeletal muscle fatty acid oxidation is not directly associated with AMPK or ACC2 phosphorylation.

Rescue of palmitate-induced insulin resistance has been linked with improvements in fatty acid oxidation, but importantly, not always with concurrently altered AMPK or ACC2 phosphorylation. Therefore, we examined the interrelationships among AMPK, ACC2, and fatty acid oxidation under 12 controlled conditions in isolated muscle. Incubation of soleus muscle (0-12 h) did not alter fatty acid oxidation, but did increase AMPK and ACC2 phosphorylation (24%-30%).

Thujone, a component of medicinal herbs, rescues palmitate-induced insulin resistance in skeletal muscle.

Thujone is thought to be the main constituent of medicinal herbs that have antidiabetic properties. Therefore, we examined whether thujone ameliorated palmitate-induced insulin resistance in skeletal muscle. Soleus muscles were incubated for < or =12 h without or with palmitate (2 mM).

Restoring AS160 phosphorylation rescues skeletal muscle insulin resistance and fatty acid oxidation while not reducing intramuscular lipids.

We examined whether AICAR or leptin rapidly rescued skeletal muscle insulin resistance via increased palmitate oxidation, reductions in intramuscular lipids, and/or restoration of insulin-stimulated AS60 phosphorylation. Incubation with palmitate (2 mM, 0-18 h) induced insulin resistance in soleus muscle. From 12-18 h, palmitate was removed or AICAR or leptin was provided while 2 mM palmitate was maintained.

Greater transport efficiencies of the membrane fatty acid transporters FAT/CD36 and FATP4 compared with FABPpm and FATP1 and differential effects on fatty acid esterification and oxidation in rat skeletal muscle.

In selected mammalian tissues, long chain fatty acid transporters (FABPpm, FAT/CD36, FATP1, and FATP4) are co-expressed. There is controversy as to whether they all function as membrane-bound transporters and whether they channel fatty acids to oxidation and/or esterification. Among skeletal muscles, the protein expression of FABPpm, FAT/CD36, and FATP4, but not FATP1, correlated highly with the capacities for oxidative metabolism (r>or=0.

Two phases of palmitate-induced insulin resistance in skeletal muscle: impaired GLUT4 translocation is followed by a reduced GLUT4 intrinsic activity.

We examined, in soleus muscle, the effects of prolonged palmitate exposure (0, 6, 12, 18 h) on insulin-stimulated glucose transport, intramuscular lipid accumulation and oxidation, activation of selected insulin-signaling proteins, and the insulin-stimulated translocation of GLUT4. Insulin-stimulated glucose transport was progressively reduced after 6 h (-33%), 12 h (-66%), and 18 h (-89%) of palmitate exposure. These decrements were closely associated with concurrent reductions in palmitate oxidation at 6 h (-40%), 12 h (-60%), and 18 h (-67%).

Fatty acid binding protein facilitates sarcolemmal fatty acid transport but not mitochondrial oxidation in rat and human skeletal muscle.

The transport of long-chain fatty acids (LCFAs) across mitochondrial membranes is regulated by carnitine palmitoyltransferase I (CPTI) activity. However, it appears that additional fatty acid transport proteins, such as fatty acid translocase (FAT)/CD36, influence not only LCFA transport across the plasma membrane, but also LCFA transport into mitochondria. Plasma membrane-associated fatty acid binding protein (FABPpm) is also known to be involved in sacrolemmal LCFA transport, and it is also present on the mitochondria.

Viability of the isolated soleus muscle during long-term incubation.

Skeletal muscle metabolism has been examined in perfused hindlimb muscles and in isolated muscle preparations. While long-term viability of the fast-twitch epitrochlearis has been documented with respect to glucose transport, it appears that long-term incubated soleus muscles are less stable when incubated ex vivo for many hours. Therefore, in the present study, we have examined whether the isolated soleus muscle remains metabolically viable for up to 18 h with respect to maintaining ATP and phosphocreatine (PCr) concentrations, carbohydrate and fatty-acid metabolism, insulin signalling, and protein expression.