Hot Plate Method Research Articles

SYNTHESIS, DOCKING STUDY, AND BIOLOGICAL EVALUATION OF 4-AMINOANTIPYRINE-ISONIAZID DERIVATIVES AS A HYBRID ANTIBACTERIAL AND ANALGESIC AGENTS

Background: 4-aminoantipyrine is one of the pyrazolone derivatives, it has been exposed to a large range of biological activities as an antimicrobial, analgesic, antiviral, anti-inflammatory, and anticancer compound. One of the important derivatives is the hybrid pyrazolone which includes two organic or inorganic drugs attached to give new pharmaceutical agents which may be the same or different activity from the original drugs. Aim: This research aimed to synthesize novel compounds derived from 4-aminoantipyrine and test their biological activity. Methods: Synthesis of 4-aminoantipyrine derivatives, which contain structurally two heterocyclic moieties, pyrazolone with oxadiazole, triazole, or tetrazole rings. The structures of the compounds were identified by 1H-NMR and FT-IR spectroscopy. The in vitro, developed compounds were screened for their analgesic activity and antibacterial activity against medically important gram (+) and gram (-) bacterial strains. Results: The antibacterial evaluation tests showed that some compounds gave good activity and others had no activity. The analgesic activity referred that the synthesized compounds had promising potency. The free binding energy (S) of the compounds with the protein 6B73 were ?4.90 to ?8.76 kcal/mol, whereas free energy (S) with the protein 5C1M gave ?4.94 to ?9.21 kcal/mol. Discussion: Among the tested compounds, it was found that compounds 1a, 4b, and 5a had more potent antibacterial activity. The analgesic activity showed that compounds 1b, 4b, and 5a gave the best activity using hot plate methods compared with the standard drug. On the other hand, compounds 1a, 4b, and 5b gave good activity using the writhing test method. Conclusions: Potent, good, or moderate analgesic and antibacterial agents were synthesized using simple and high-yield chemical reactions. The chemical reactions include the synthesis of hybrid antibacterial and analgesic agents using pyrazolone compounds.

Interaction of meloxicam and phenylbutazone on the level of cyclooxygenase-2 in mice

The reason for the recent study was to inspect the therapeutic efficacy of meloxicam and phenylbutazone alone with their analgesic interaction and their subsequent inhibitory interaction at the level of cyclooxygenase-2 in mice. Meloxicam and phenylbutazone had the analgesic-median effective doses (ED50s) of 15.57 and 119.73 mg/kg, i.p., respectively, given once to mice separately as determined by the up-and-down procedure using a hot plate method. The estimated analgesic ED50s for meloxicam and phenylbutazone combination were at 12.84 and 98.75 mg/kg, i.p., correspondingly when given together at a ratio of 1:1 of their ED50s. The isobolographic analysis reveals that the analgesic interaction between meloxicam and phenylbutazone was antagonistic, as indicated by the interaction index of 1.65. The ELISA technique was used to estimate the cyclooxygenase-2 activity, reflecting that meloxicam or phenylbutazone significantly inhibited the cyclooxygenase-2 activity by 72 and 90%, respectively, compared to the control group. The combination composed of meloxicam and phenylbutazone has a lower limit of inhibition of the cyclooxygenase-2 activity (33%) in comparison to meloxicam or phenylbutazone. Meloxicam and phenylbutazone coadministration were significantly different from the control, meloxicam, and phenylbutazone groups concerning the cyclooxygenase-2 activity in mice. The sum of the data concluded that meloxicam and phenylbutazone have an excellent analgesic efficacy when administered alone. In contrast, the mixture of these two drugs has no benefit because of the antagonistic interaction at cyclooxygenase-2 in mice.

Investigation of Analgesic Effects of Venlafaxine, Atomoxetine and Trazodone Alone and in Combination in Acute Pain Models of the Rats

Purpose: Poorly controlled pain is linked to several other undesirable outcomes. These outcomes are upsetting to patients, their families, and society as a whole. Although opioids and non-steroidal anti-inflammatory drugs are the cornerstone of the nociceptive pain treatment, the use of these drugs is restricted due to their side effects. Therefore, it is essential to develop new treatment alternatives for pain. Our study aimed to examine the pain relief effectiveness of Venlafaxine, Atomoxetine and Trazodone at 3 different doses alone, and in combination with each other in an acute pain model.
 Material and Methods: The analgesic effectiveness of Venlafaxine, Atomoxetine, and Trazodone at three different doses alone and in combination in an acute pain model in rats was examined using the hot plate and tail flick methods.
 Results: Venlafaxine and Trazodone, Venlafaxine showed dose-dependent analgesic effect when compared to the control. When Venlafaxine at dose of 2 mg/kg were combined with Atomoxetine at doses of 1, 3 and 6 mg/kg, the analgesic effects were significantly increased compared to these drugs alone. When Venlafaxine at dose of 2 mg/kg were combined with trazodone at doses of 4, 12 and 24 mg/kg, the analgesic effects were significantly increased compared to these drugs alone. 
 Conclusion: All in all, our data suggest these combinations may offer a beneficial treatment option for acute pain in future.

Phytochemical characterization, Antioxidant and Analgesic potentials of Aerial Parts of Eruca vesicaria

Our work is based on the phytochemical study, the antioxidant and the analgesic activities of a hydroalcoholic extract of Eruca vesicaria aerial part very used in traditional medicine. The phytochemical screening highlighted the presence of tannins, flavonoids, sterols, flavonoid glucosides, saponins, phenols and alkaloids. The determination of total phenols of hydromethanolic extract by the Folin-ciocalteu method revealed a content equal to 4.63 ± 0.017 mg GAE / g extract. The amount of flavonoids by AlCl3 method achieved a content equal to 2.14 ± 0.025 mg QE/ g extract. The antiradical activities were evaluated by two chemical tests ; DPPH and FRAP. The obtained results showed a high reducing activity. Besides, the acute toxicity and the analgesic activity of the plant extract was evaluated on rats, using a pain model induced by chemical stimuli, hot plate and tail immersion methods. The extract was used at various doses 100, 200 and 300 mg/kg, whereas acetylsalicylic acid was used as the standard drug (200 mg/kg). In the acetic acid-induced model, the plant extracts and the standard drug significantly (p<0.05) reduced the abdominal writhing in rats compared to the control group by increasing the percentage of writhing inhibition in a dose-dependent manner. In the hot plate and the tail immersion models, the plant extracts and the standard drug acetylsalicylic acid demonstrated a good analgesic activity and significantly (p<0.05) increasing the pain reaction time. These results indicate that the E. vesicaria plant has a significant analgesic potential that can act through peripheral and central mechanisms.

Development of Plant Fibre Foam and Study of Its Thermal Insulation Properties

At present, the research and production of green fiber materials that replace plastics are becoming the consistent proposition of all countries that pay attention to environmental protection. In order to improve the thermal insulation properties of forest plant-based foams, which are low-cost and non-polluting, this paper explores the preparation of forest plant-based foams and the determination of their thermal insulation properties. Firstly, based on the three-factor orthogonal experimental method, variables such as the ratio of materials that may affect the foaming rate and the size of the mould were designed, and the influence of these variables on the foaming rate of the material was analysed. Then, for the samples obtained, slices were made and the thermal conductivity of the sample was measured by the hot plate method, and finally, for the measurement results, the influence of the foaming rate on the thermal conductivity was analysed by non-linear regression, and the regression equation between the two. The results show that the size of the mould has the greatest influence on the foaming rate out of all the independent variables influencing the results. At a foaming rate of 19.8%, the thermal conductivity of the material was the lowest and the material had the best thermal insulation effect.

Evaluation of analgesic, anti-inflammatory, and antipyretic activities of Ziziphus mauritania Lam leaves in animal models

Ziziphus mauritiana (Rhamnaceae), commonly known as Ziziphus jujuba Mill, is in traditional Chinese medicine enriched with high medicinal values. In Indian and Chinese traditional medicine, a decoction of Ziziphus mauritiana leaves was used to cure insomnia, amnesia, pain, and vertigo. The study aims to determine the analgesic, anti-inflammatory, and antipyretic activities of Ziziphus mauritiana Lam leaves to establish a rationale for their use. We studied analgesic activity by writhing and the hot plate methods in mice, whereas mechanical allodynia in rats. Also, rats were used in carrageenan anti-inflammatory and brewer's yeast-caused pyrexia. MEZ were tested at 250 and 500 mg/kg orally. Molecular docking studies between 3 inflammatory pathway proteins and natural molecules are planned and carried out. CHARMm was used for docking, and the smart minimizer algorithm was used to reduce energy. Acute toxicity testing up to 5000 mg/kg showed no deaths. Both UPLC-Q-TOF-MS/MS analysis and phytochemical analysis supported the presence of flavonoids, terpenoids and saponins. At a dose of 500 mg/kg, MEZ significantly (p<0.001) reduces the perception of pain brought on by thermal, mechanical, and chemical pain models. Paw edema is dramatically reduced at 0, 1, 2, 3, and 4 h after carrageenan injection by MEZ at 500 mg/kg.Similarly, MEZ at 500 mg/kg showed a gradual drop in rectal temperatures from 3 to 9 h. The docking result illustrated that the quercetin and rutin exposed a better binding with inflammatory protein through multiple hydrogen bonds and π interactions. The findings showed that the MEZ has potential analgesic, anti-inflammatory, and antipyretic properties at the levels studied, supporting the traditional use claim.

Water Mediated One-Pot, Stepwise Green Synthesis, Anti-Inflammatory and Analgesic Activities of (3-Amino-1-Phenyl-1H-Benzo[f]Chromen-2-yl) (1H-Indol-3-yl) Methanone Catalysed by L-Proline

Aim: The reactions were carried out by one pot three-component synthesis, 3- cyanoacetylindole (1) on reaction with aromatic aldehydes (2) and β-naphthol (3) in an aqueous medium in the presence of L-proline as a catalyst under reflux for 30 min, resulting in (3-amino-1- phenyl-1H-benzo[f]chromen-2-yl) (1H-indol-3-yl)methanone (4). The method has many advantages like short reaction times, good yields, and simple workup procedure, besides being green in nature. Pharmacological evaluation of title compounds was done for anti-inflammatory and analgesic activities. Anti-inflammatory activity was carried carrageenan-induced paw edema model in which indomethacin was used as standard and analgesic activity was evaluated by eddy's hot plate method using diclofenac as standard drug. Background: Benzopyrans or chromenes are an important class of heterocyclic compounds due to their broad spectrum of biological activity and a wide range of applications in medicinal chemistry. The chromene moiety is found in various natural products with interesting biological properties. Chromenes constitute the basic backbone of various types of polyphenols and are widely found in alkaloids, tocopherols, flavonoids, and anthocyanins. Indoles are omnipresent in various bioactive compounds like alkaloids, agrochemicals, and pharmaceuticals. Objective: The objective of this study is to synthesize one-pot stepwise Green synthesis, antiinflammatory and analgesic activities of 3-amino-1-phenyl-1H-benzo[f]chromen-2-yl) (1H-indol-3- yl) methanones. Methods: The acute anti-inflammatory effect was evaluated by carrageenan-induced mice paw edema (Ma Rachchh et al., 2011). Edema was induced by injecting carrageenan (1% w/v, 0.1 ml) in the right hind paw of mice. The test compounds 1-12, indomethacin (10 mg/kg), and the vehicle were administered orally one hour before injection of carrageenan. Paw volume was measured with a digital plethysmometer at 0, 30, 60, 90, 120 min after injection. Percentage increase =A-B/ A *100 Results: Carrageenan induced paw edema model was used for anti-inflammatory activity in which animals treated with standard (indomethacin) and test compounds showed a significant decrease in the paw edema. Analgesic activity was estimated using Eddy’s hot plate method; animals were treated with standard (diclofenac) and test compounds showed a significant increase in the reaction time. Conclusion: A green, one-pot, step-wise and three-component synthesis of 3-amino-1-phenyl-1Hbenzo[ f]chromen-2-yl) (1H-indol-3-yl) methanone was achieved by using water as a solvent, Lproline as catalyst under reflux conditions. The reactions were carried out in eco-friendly conditions with shorter reaction times, easier workup, and high yields. Anti-inflammatory activity was evaluated by carrageenan-induced paw edema model, where significant anti-inflammatory activity is shown by all the test compounds 4(a-l) compared to standard drug. Analgesic activity was studied by Eddy’s Hot plate method and Test compounds 4e, 4f, 4h, 4i, 4j, 4k, 4l showed significant activities compared to the reference drug.

Green synthesis and Characterization of Zinc Nanoparticles using Herbal plant Extracts with their Influence on some Bacterial Infection

The nanoparticles of ZnO biosynthesis have distinctive features. many researchers have noted it cute to research in diverse research disciplines due to modern medical applications. different NPS have been estimated for their potential usage in which zinc oxide (ZnO) nps have confirmed to be a viable replacement for treating environmental pollutants, due to their excellent capacity to absorbed rays of UV. The purchase seeds of Trigonella foenum-graecum, clove buds, and leaves of the Salvia officinalis plant from the local market and extracted by hot plate methods. the purpose of the current study was the green synthesis of ZnO nanoparticles (NPS) from the different above extracts followed by a comprehensive characterization and assessment of their biological potential. no-NPS synthesized as such was subjected to characterization employment standard techniques such as particle size and tem. highly stable crystalline NPS with sizes between 32.6 and 142.7 nm were obtained from different plants. These Nps revealed a wide range of biological applications showing antioxidant, moderate α-amylase inhibitors, antibacterial and cytotoxic powers. in addition to the percentage of s. epidermidis and k. pneumonia isolated from human and children was recorded mean (40 and 60.4 %) respectively. The highest antibacterial activity (17±0.10 mm and 18±0.09) was shown by seed salvia Officinalis-mediated ZnO NPS against k and s. epidermidis respectively. on the other aspect the result obtained from using silymarin and the mediated zinc nanoparticles showed limited zone inhibition (15 ± 0.09, 15 ± 0.15, and 8 ± 0.02, 8 ± 0.02) respectively. Among all of the NPS synthesized and used, the effect of seed extract-mediated NPS was found to be most promising for future applications.

Analysis of the Thermal Conductivity of a Bio-Based Composite Made of Hemp Shives and a Magnesium Binder

The evolution of bio-based composites in the building industry is strongly linked with the growing demand for sustainable development, which is relevant nowadays. Hemp shives are a large group of organic residues that are obtained in the process of oil extraction as well as straw processing. These residues could be utilized along with a binder as constituents in the manufacture of bio-based building composites. This study is focused on the impact of density and relative humidity on the effective thermal conductivity of hemp shive-based bio-composites with a magnesium binder. For this reason, a series of samples with variable densities was manufactured and subjected to conditioning in a climatic chamber at a constant temperature and different relative humidity settings. As soon as samples were stabilized, the guarded hot plate method was applied to determine their thermal conductivities. Before each measurement, great care was taken during sample preparation to ensure minimum moisture loss during long-lasting measurements. The results showed that an increase in sample density from 200 kg/m3 to 600 kg/m3 corresponded to up to a three-fold higher composite thermal conductivity. In the case of sample conditioning, a change in relative humidity from a very low value to 90% also resulted in almost 60% average higher thermal conductivity.

Evaluation of the Antinociceptive Action of Simvastatin in Mice.

Introduction: Statins are well-established agents for dyslipidemia and have successfully been used for the prevention of coronary artery diseases for a long time; this is attributed not only to their lipid-lowering action but also to their pleiotropic actions. Recently many pleiotropic actions of statins have been explored, but very few studies were done to explore statins' antinociceptive action; therefore, the current study was planned to evaluate the antinociceptive activity of Simvastatin in different pain models in mice.Materials and Methods: Antinociceptive activity of Simvastatin was evaluated by using Eddy's hot plate method (central analgesic model), acetic acid-induced writhing method (peripheral analgesic model), and biphasic formalin-induced paw licking method. Twenty-four mice were divided into four groups (n = 6 in each): Vehicle control group, simvastatin 5mg/kg, simvastatin 20mg/kg, and positive control group.Results: In the hot plate method, as compared to the vehicle control group, Simvastatin 20mg/kg group showed a significant rise in the reaction time to the corresponding time interval (p<0.001). While the simvastatin 5mg/kg group did not show any significant analgesic activity in the hot plate test. In the acetic acid writhing method, both test groups show a significant delay in the onset of writhing and a decrease in the number of writhes as compared to the vehicle control group (P<0.001). While in the formalin test, both groups show dose-dependent analgesic activity in both the early and late phases.Conclusion: Simvastatin exhibits analgesic activity in both central as well as peripheral models of analgesia, but central analgesia shows only at higher concentrations. Similarly, it inhibits inflammatory pain more predominantly than neurogenic, and hence simvastatin can be used in inflammatory conditions like rheumatoid arthritis and osteoarthritis particularly when there is coexisting dyslipidemia.

Acute Oral Toxicity Studies and Evaluation of Central Analgesic Activity of Various extracts of Leaves of &lt;i&gt;Rhizophora apiculata&lt;/i&gt;

The present study aimed to determine the acute toxicity and screening of central analgesic activity of various extracts of Rhizophora apiculata leaves. The animals (Mice) were divided into control (no drug) and extract-treated groups (n=5), which were treated with diethyl ether, ethyl alcohol, and aqueous extract of R. apiculata leaves in various doses for specific regulatory needs. The groups which were given the highest safe doses were observed for 14 days. Then, blood samples were collected from high dose treated live mice through the retro-orbital route and were analysed for haematological, biochemical, and histopathological study. Evaluation of central analgesic activity was carried out by using tail immersion and hot plate methods. No considerable alterations were observed in body weight and organ-to-body weight index with the administration of extracts. An increase in albumin, globulin, total protein content and high-density lipoproteins, white blood cells, mean corpuscular volume, and eosinophils were observed. And a decrease in low-density lipoproteins, very low-density lipoproteins, triglycerides, and red blood cells were observed. Lymphocyte and monocyte levels were also reduced. The results also showed that the ethyl alcohol and aqueous extracts have elevated the time taken to flick response in the tail immersion test, and reduced the number of jumps, paw lick responses in the hot plate method. It was concluded that the diethyl ether and ethanolic extracts were found to be safe, which falls under non-toxic chemicals (LD50&gt;2000 smg/kg) whereas the aqueous extract was found safe up to 550 mg/kg beyond which, it was shown mortality. Ethyl alcohol and aqueous extracts were also proved to have analgesic activity.

Analgesic Effects of Vilazodone, Indatraline, and Talsupram in a Rat Model of Neuropathic Pain.

Drugs that inhibit the reuptake of serotonin, norepinephrine, and/or dopamine are widely used for treating depressive disorders and have emerged as effective drugs for neuropathic pain. They have no substantial anti-nociceptive effects but are considered, with gabapentin/pregabalin, first-line drugs for neuropathic pain. In this study, three different antidepressant agents were used in different doses to investigate their anti-hyperalgesic effects in rat models of neuropathic pain using hot plate and tail flick methods. They have different mechanisms of action; vilazodone hydrochloride is a selective serotonin inhibitor and a 5-HT1A partial agonist; talsupram hydrochloride is a selective noradrenaline inhibitor, and it has a high affinity for noradrenaline transporter (NET), whereas indatraline hydrochloride is a triple reuptake inhibitor that inhibits transporters for 5-HT (SERT), dopamine (DAT), and NET. All the drugs used in the experiment were found to have an anti-hyperalgesic effect in both tests compared to the sham group. When anti-hyperalgesic effects of the three agents were compared to each other, it was found that talsupram hydrochloride was significantly more effective than the two other drugs in hot plate test. However, there was no statistically significant difference in the tail flick test. Indatraline hydrochloride was more effective than vilazodone hydrochloride at the same doses in the tail flick test. Our data suggest that three drugs are effective analgesics in rat models of neuropathic pain and inhibition of noradrenaline reuptake represents the cornerstone of analgesic mechanisms of effective antidepressants.

Experimental evaluation on analgesic activity of Erandamoola (Ricinus communis) collected in three different seasons wsr to Dravya Samgrahana Kaala

About: Dravya samgrahana kaala is an important scientific documentation mentioned in Ayurveda where there will be change in activity and phytochemical profile of plants in different seasons. Erandamoola (Ricinus communis) is an important medicinal plant where roots are particularly indicated as analgesic. As per Dravya samgrahana vidhi roots are to be collected in Hemanth-Shishira or Greeshma rutu or Pravarat rutu. Hence with this background study has been planned to evaluate analgesic activity of the Erandamoola (Ricinus cumunis) collected in Greeshma (EMG) and Pravrutritu (EMP) and Shishiraritu (EMS) using Eddy’s Hot plate method, in swiss albino mice. Materials and Methods: Roots of matured plant will be collected in three different seasons, shade dried, powdered and used for the study. Swiss Albino mice were randomly grouped into 3 groups of six animals each. Group I served as control, Group II serve as standard with administration of Tramadol whereas Group III (EMG), Group IV (EMP) and Group V (EMS) serve as the test group with administration of 200 mg/kg body weight (Erandmoola collected in Greeshma (EMG), Pravrut ritu (EMP) and Shishira ritu (EMS) respectively. Results: Erandamoola collected in greeshma and pravrut ritus show almost similar pain threshold with a slight increase in values than drug collected in greeshma ritu. Conclusion: Thus Erandamoola (Ricinus communis) can be efficiently used as an analgesic, simulatneously season or Samgrahana kaala is having a definite role on drug activity.

Basolateral amygdala cannabinoid CB1 receptors mediate the antinociceptive activity of harmaline in adolescent male mice

Evidence suggests a clear role for the amygdala endocannabinoid system in pain processing. Harmaline has been also known as the main nociceptive agent extracted from the Peganum harmala plant. In this study, the role of basolateral amygdala (BLA) cannabinoid CB1 receptors in pain sensitivity of harmaline-treated mice were assessed using tail-flick and hot plate methods in adolescent male NMRI mice. Intraperitoneal administration of two higher doses of harmaline (6 and 8 mg/kg) increased tail-flick latency, suggesting an antinociceptive activity. The same result was observed for the higher dose of harmaline in the hot plate test. Intra-BLA microinjection of CB1 receptor agonist ACPA (1 and 1.5 ng/mouse) or (1.5 ng/mouse) enhanced the ineffective dose-response of harmaline on pain threshold in the tail-flick or hot plate tests, respectively. Microinjection of two higher doses of CB1 receptor antagonist AM251 (0.5 and 1 ng/mouse) attenuated the antinociceptive activity of harmaline (8 ng/mouse) in both tail-flick and hot plate tests. Meanwhile, ACPA and AM251 did not alter latency to withdraw from the noxious stimulus in both tests, by themselves. It should be noted that the analgesic dose of the drugs alone or in combination did not affect locomotor activity. The obtained results highlight that BLA CB1 receptors mediate the antinociceptive activity of harmaline.

Evaluation of Analgesic Activity of Thymoquinone the Major Constituent of Nigella sativa Seeds in Mice

Drugs commonly used in modern medicine for suppression of pain and fever provide only symptomatic relief and long-term use of these drugs is associated with serious adverse effects. Recently, some evidences suggest that Nigella sativa inhibit eicosanoid generation in leukocytes and lipid peroxidation. They are reported to inhibit both cycloxygenase and 5-lipooxygenase pathways of arachidonic acid metabolism. The present study was aimed to evaluate the analgesic activity of pure compound, thymoquinone the major constituent of Nigella sativa seeds in mice. The analgesic activity was determined by hot plate, tail immersion, tail flick method and acetic acid induced writhing test in mice. Thymoquinone (10, 20, 30 mg/kg, body weight) and Aspirin (20mg/kg) made as suspensions prepared in 1% carboxy methyl cellulose and were fed to mice intraperitoneally. In tail flick method thymoquinone exhibited maximum analgesic effect at a dose of 30mg/kg after 120 min as compared to control and standard. Maximum analgesic effect was noted at a dose of 10 mg/kg after 120 min. the poor analgesic effect of thymoquinone at a dose of (20 and 30 mg/kg) as compared to control and standard drug by hot plate method. However with writhing test the thymoquinone showed maximum protection at a dose of 30 mg/kg (98.23%). The thymoquinone have minimum effect showed at dose of 10 mg/kg (69.72%) and 20 mg/kg (42.26%) as compared to standard and control. But in tail immersion method thymoquinone exhibited maximum activity after 120 min at a dose of 20 mg/kg as compared to control and standard drug while at a dose of 30 mg/kg the compound did not showed any further enhancement in analgesic activity. It is concluded from the present study that thymoquinone the major constituent of Nigella sativa possesses potent analgesic activity in mice.&#x0D; Keywords: Thymoquinone, Nigella sativa, Hot plate, Tail immersion, Tail flick method, Acetic acid induced writhing test

Thermal conductivity of 3D printed concrete with recycled fine aggregate composite phase change materials

In this study, a novel shape-stabilization phase change materials (PCM) for 3D printed concrete have been generated by impregnating paraffin into the recycled fine aggregates. Based on both steady state hot plate method and transient hotwire method, the impact of printing parameters, including printing layers, path, extrusion rate and materials on thermal conductivity of the 3D printed concrete was investigated. The relationship among thermal conductivity, dry density and porosity of the 3D printed concrete was analyzed. The results showed that recycled fine aggregates can be successfully used as a support material for paraffin. The melting temperature and latent heat is 36.52 °C and 40.65 J/g, respectively. The thermal conductivity of 3D printed concrete was significantly influenced by the multi-layer structure and with thermal anisotropy. Under the same size, density class or mix design, the thermal conductivity of the 3D printed concrete can reach up to 31.04% lower than that of mould cast concrete. The results also indicate that impregnating paraffin into the recycled fine aggregate can improve its thermal properties so as to upgrade the overall performance of 3D printed concrete.

Pain Allaying Epalrestat-Loaded Lipid Nanoformulation for the Diabetic Neuropathic Pain Interventions: Design, Development, and Animal Study.

Diabetic peripheral neuropathy is the most common complication of diabetes mellitus. Epalrestat, an aldose reductase inhibitor, has been approved for clinical therapy for diabetic peripheral neuropathic pain. In the present study, solid lipid-based nanoparticles are used for oral administration of epalrestat (E-SLN) and evaluated against diabetic neuropathic pain in a rat model. Experimental diabetes in rats was induced by a single dose of streptozotocin (STZ) administration. The therapeutic efficiency of Epalrestat nanoparticles (0.25, 0.50, 1, and 5 mg/kg) in diabetic rats was studied. STZinduced diabetic rats were treated with different doses of E-SLN for 8 weeks. The nanoparticles were orally administered at a single dose in rats, and the various parameters related to peripheral neuropathy were evaluated and compared with the bare drug. The blood glucose level was estimated by standard glucometer, HbA1c, triglycerides, total cholesterol, and liver function test (ALT and AST) were analyzed by blood samples collected from retro-orbital plexus. Oxidative stress markers and Na+K+ATPase, TNF-α, and IL-1β levels were measured in the homogenate of sciatic nerves. Behavioral tests were also performed by the hot plate method and tail-flick method. E-SLN synthesized by the micro-emulsification method was 281 ± 60 nm in size, and encapsulation efficacy was found to be 88 ± 2%. Optimized E-SLN were characterized and found to be optimum in size, spherical shape, decent encapsulation efficiency, stable at acidic gastric pH, and suitable for oral delivery. E-SLNs did not significantly reverse the STZ-induced elevated blood glucose level (FBS and PPBS), HbA1c, triglycerides, and total cholesterol but significantly improved TNF-α, IL-1β, and increased Na+K+ATPase levels, oxidative stress marker and ALT, AST in the treated rat group as compared with the diabetic group. Doses of E-SLN, i.e. 0.5, 1.0, 2.5, and 5 mg/kg, significantly increased the tail-flick latency time and hot plate response time in a dose-dependent manner compared with the diabetic group. Thus, it is suggested that E-SLN were equally effective and less hepatotoxic compared with the standard treatment of epalrestat. To the best of our knowledge, we, for the first time, propose the orally deliverable E-SLN that ameliorates STZ-induced diabetes neuropathic pain effectively as compared with conventional epalrestat.

Preliminary phytochemical and analgesic activity extract of Kigelia pinnata leaf

Kigelia pinnata Linn. (Balam Kheera) belongs to the family of Bignoniaceae and is commonly called the "sausage" tree because of its hugs fruits. The present research was conducted to investigate the analgesic activity of different extracts of leaves of Kigelia pinnata. Preliminary phytochemical investigations were performed by chemical tests. In the preliminary phytochemical test, the leaves extract showed the presence of phytosterols, alkaloids, glycosides, flavonoids, saponins, tannins, and phenolic compounds. An acute toxicity study was performed according to OECD guidelines. The analgesic activity was conducted by Hot Plate Method and Tail Immersion Test on adult Swiss albino mice. In Acute Toxicity Study, oral administration of extract was found safe at a dose of 2,000 mg/kg, p.o. and produced no signs of toxicity. The methanolic extract was found to be significant in Analgesic activity.

Pharmacological Potential of Avicennia alba Leaf Extract: An Experimental Analysis Focusing on Antidiabetic, Anti-inflammatory, Analgesic, and Antidiarrheal Activity.

Avicennia alba is a mangrove plant that is extensively used to treat severe health issues. This focus of this study was to investigate the antidiabetic, anti-inflammatory, analgesic, and antidiarrheal activities of methanolic extract of A. alba leaves in Swiss albino mouse model. The antidiabetic, anti-inflammatory, analgesic, and antidiarrheal activities of the leaf extract were performed using alloxan-monohydrate, carrageenan-induced paw edema, acetic acid-induced writhing test and the hot plate method, and castor oil-induced method, respectively. The extract was used at doses ranging from 200 to 500 mg/kg to conduct the investigation. Leaf extract at 400 and 500 mg/kg showed potent antidiabetic activity in alloxan-induced diabetic mice. Advanced research is needed to control blood glucose levels and carrageenan paw edema-based anti-inflammatory effects. Both tests showed statistically significant result in a dose-dependent manner. The maximum dose (500 mg/kg) demonstrated potent analgesic activity in both writhing test and hot plate method. The plant extract also showed significant antidiarrheal activity at 400 and 500 mg/kg in experimental mice. However, more research is needed to explore the possible mechanisms and isolate the compounds associated with these bioactivities from the leaf extract of A. alba.

Anti-inflammatory and analgesic activities of imidazolyl triazolo hydroxamic acid derivatives

Hydroxamic acids are directly related with cancer and its progression. Long term exposure with inflammatory responses, dysplasia develops which leads to cancer. Metastasis of cancer and expression of transient potential receptor ankyrin-1 are known to cause severe pain. Here, we explored the possibility of developing newer hydroxamic acid derivatives as anti-inflammatory and analgesic agent. Animals were administered with 100 mg/kg dose of the synthesized imidazolyl triazolo hydroxamic acid derivatives (FP1-FP12) and 50 mg/kg dose of standard diclofenac sodium. Carrageenan induced rat paw edema and Eddy’s hot plate methods were considered for anti-inflammatory and analgesic activities. Among all the synthesized molecules, FP10 and FP4 were the most effective anti-inflammatory and analgesic agent, respectively. The activity profile of remaining molecules as anti-inflammatory agents was as follows: FP4>FP9> FP8> FP2 and as analgesic activity profile was FP10>FP3>FP8 >FP11 >FP2 > FP12. Presence of ethyl- benzyl and furan groups in linker portion of the structure minimized both the anti-inflammatory and analgesic activities. Results have shown that compounds with electron releasing groups considerably enhance both anti-inflammatory and analgesic activities.