scholarly journals Effects of a BMI1008 mixture on postoperative pain in a rat model of incisional pain

PLoS ONE ◽  
2021 ◽  
Vol 16 (9) ◽  
pp. e0257267
Author(s):  
Geun Joo Choi ◽  
Eun Jin Ahn ◽  
Oh Haeng Lee ◽  
Hyun Kang

Background The purpose of this study was to evaluate the analgesic effect of BMI1008 (a new drug containing lidocaine, methylene blue, dexamethasone and vitamin B complex) and to investigate the analgesic effect of lidocaine and BMI-L (other components of BMI1008 except lidocaine) at different concentrations in a rat model of incisional pain. Methods Male Sprague-Dawley rats (250–300 g) were used for the incisional pain model simulating postoperative pain. After the operation, normal saline, various concentrations of BMI1008, lidocaine with a fixed concentration of BMI-L, and BMI-L with a fixed concentration of lidocaine were injected at the incision site. The preventive analgesic effect was evaluated using BMI1008 administered 30 min before and immediately after the operation. In addition, BMI1008 was compared with positive controls using intraperitoneal ketorolac 30 mg/kg and fentanyl 0.5 μg/kg. The mechanical withdrawal threshold was measured with a von Frey filament. Results The analgesic effect according to the concentration of BMI1008, lidocaine with a fixed concentration of BMI-L, and BMI-L with a fixed concentration of lidocaine showed a concentration-dependent response and statistically significant difference among the groups (P <0.001, P <0.001, and P <0.001, respectively). The analgesic effect according to the time point of administration (before and after the operation) showed no evidence of a statistically significant difference between the groups (P = 0.170). Compared with the positive control groups, the results showed a statistically significant difference between the groups (P = 0.024). Conclusion BMI1008 showed its analgesic effect in a rat model of incisional pain in a concentration-dependent manner. Moreover, BMI-L showed an additive effect on the analgesic effect of lidocaine.

AMB Express ◽  
2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Hend M. Tag ◽  
Amna A. Saddiq ◽  
Monagi Alkinani ◽  
Nashwa Hagagy

AbstractHaloferax sp strain NRS1 (MT967913) was isolated from a solar saltern on the southern coast of the Red Sea, Jeddah, Saudi Arabia. The present study was designed for estimate the potential capacity of the Haloferax sp strain NRS1 to synthesize (silver nanoparticles) AgNPs. Biological activities such as thrombolysis and cytotoxicity of biosynthesized AgNPs were evaluated. The characterization of silver nanoparticles biosynthesized by Haloferax sp (Hfx-AgNPs) was analyzed using UV–vis spectroscopy, transmission electron microscopy (TEM), X-ray diffraction (XRD), and Fourier-transform infrared spectroscopy (FTIR). The dark brown color of the Hfx-AgNPs colloidal showed maximum absorbance at 458 nm. TEM image analysis revealed that the shape of the Hfx-AgNPs was spherical and a size range was 5.77- 73.14 nm. The XRD spectra showed a crystallographic plane of silver nanoparticles, with a crystalline size of 29.28 nm. The prominent FTIR peaks obtained at 3281, 1644 and 1250 cm− 1 identified the Functional groups involved in the reduction of silver ion reduction to AgNPs. Zeta potential results revealed a negative surface charge and stability of Hfx-AgNPs. Colloidal solution of Hfx-AgNPs with concentrations ranging from 3.125 to 100 μg/mL was used to determine its hemolytic activity. Less than 12.5 μg/mL of tested agent showed no hemolysis with high significant decrease compared with positive control, which confirms that Hfx-AgNPs are considered non-hemolytic (non-toxic) agents according to the ISO/TR 7405-1984(f) protocol. Thrombolysis activity of Hfx-AgNPs was observed in a concentration-dependent manner. Further, Hfx-AgNPs may be considered a promising lead compound for the pharmacological industry.


2017 ◽  
Vol 2 (2) ◽  
pp. 147
Author(s):  
Triswanto Sentat ◽  
Susiyanto Pangestu

Kersen leaf (Muntingia calabura L.) contains tannins, flavonoids and polyphenol compounds allegedly have analgesic effect. The objective was to determine the analgesic effect of ethanol extract of kersen leaves and to determine the most effective analgesic dose. This study was an experimental research. Leaves were extracted with ethanol 70% and the analgesic effect test was divided into 5 groups: negative control treatment (distilled water), positive control (mefenamic acid 2.6mg/kg), kersen leaf ethanol extract first dose (100mg/kg), second dose (200mg/kg) and tthird dose (400mg/kg). Giving treatments by oral, after 30 minutes, the mices were given a pain inductor with 0.5% acetic acid by intra peritonial administration. Analgesic power was calculated by counting the number of writhing in mice for 1 hour. The results showed that the ethanol extract of cherry leaf has analgesic effect. From the calculation of the first dose analgesic power (42.9%), second dose (59.4%) and the third dose 69.9%. Statistical test results kruskal wallis value of p=0.011 (p<0.05) showed a significant difference between all analgesic treatment groups. The conclusion of this study is all of the ethanol extract had analgesic effects on male white mice, whereas a dose of 400mg/kg is the most effective analgesic dose.


2003 ◽  
Vol 94 (5) ◽  
pp. 1813-1820 ◽  
Author(s):  
Shin Terada ◽  
Isao Muraoka ◽  
Izumi Tabata

The purpose of the present investigation was to establish a method for estimating intracellular Ca2+ concentrations ([Ca2+]i) in isolated rat epitrochlearis muscles. Epitrochlearis muscles excised from 4-wk-old male Sprague-Dawley rats were loaded with a fluorescent Ca2+indicator, fura 2-AM, for 60–90 min at 35°C in oxygenated Krebs-Henseleit buffer. After fura 2 loading and subsequent 20-min incubation, the intensities of 500-nm fluorescence, induced by 340- and 380-nm excitation lights (Ftotal340 and Ftotal380), were measured. The fluorescences specific to fura-2 (Ffura 2340 and Ffura 2380) were calculated by subtracting the non-fura 2-specific component from Ftotal340 and Ftotal380, respectively. The ratio of Ffura 2340 to Ffura 2380 was calculated as R, and the change in the ratio from the baseline value (ΔR) was used as an index of the change in [Ca2+]i. In resting muscle, ΔR was stable for 60 min. Incubation for 20 min with caffeine (3–10 mM) significantly increased ΔR in a concentration-dependent manner. Incubation with hypoxic Krebs-Henseleit buffer for 10–60 min significantly elevated ΔR, depending on the duration of the incubation. Incubation with 50 μM N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide for 20 min significantly elevated ΔR ( P < 0.05). No significant increases in ΔR were observed during incubation for 20 min with 2 mM 5-aminoimidazole-4-carboxamide-1-β-d-ribofuranoside or with 2 mU/ml insulin. These results demonstrated that, by using the fura 2-AM fluorescence method, the changes in [Ca2+]i can be monitored in the rat epitrochlearis muscle and suggest that the method can be utilized to observe quantitative information regarding [Ca2+]i that may be involved in contraction- and hypoxia-stimulated glucose transport activity in skeletal muscle.


Author(s):  
Santosh Fattepur ◽  
Kiran Chanabasappa Nilugal ◽  
Ranya Rajendran ◽  
Fadli Asmani ◽  
Eddy Yusuf

Objective: Hyperlipidemia is one of the risk factors that contribute to the prevalence of coronary heart diseases and antihyperlipidemic agents, such as statin, was used to treat hyperlipidemia as a current therapy. Boesenbergia pandurata has not been exploited for antihyperlipidemic effect. Hence, this study aims to screen for the antihyperlipidemic activity of methanolic extracts of B. pandurata rhizomes (BPR extracts) in hypercholesterolemia-induced Sprague-Dawley rats.Methods: BPR extracts were prepared using the maceration method with 1500 ml of 80% methanol at room temperature for about 7 days. A toxicity study was carried out based on OECD guidelines. Hypercholesterolemia was induced by 6% lard oil, 2% of cheese, and egg yolks. Two different doses of BPR extracts, 200 and 400 mg/kg, were used to screen for antihyperlipidemic effect. Histopathological study was carried out in the liver. The results were evaluated for the statistically significant difference by using the one-way ANOVA followed by post hoc Dunnett test.Results: No mortality was witnessed even till 2 g/kg. Only 400 mg/kg of BPR extracts statistically reduced in total cholesterol (p<0.05), low-density lipoprotein-cholesterol (p<0.05) and an increase in high-density lipoprotein-cholesterol (p<0.05) when compared to the positive control. BPR extracts (400 mg/kg) showed less enlargement of lipid droplets as compared to positive control.Conclusion: BPR extracts can be a promising medicinal plant for treating hyperlipidemia in underdeveloped countries.


2020 ◽  
Vol 42 (4) ◽  
pp. 564-564
Author(s):  
Ju liu Ju liu ◽  
Jun Li Jun Li ◽  
Jian tao Shi Jian tao Shi ◽  
Jie Li Jie Li ◽  
Xue chen Hao Xue chen Hao ◽  
...  

A series of novel 4-phenylaminobenzofuro[2,3-d]pyrimidine derivatives had been prepared and assessed for their in vitro antiproliferative activities against three lung cancer cell lines (A549, H460 and H1975). The bioassay results showed most of the designed compounds exhibited potential antiproliferation activities. Among them, compound 8f exhibited remarkable inhibitory activity against A549 and H460 cell lines with IC50 value of 2.54 μM and 2.68 μM, respectively, which was comparable to that of the positive control sorafenib (IC50 = 2.69 μM for A549 and 3.71 μM for H460). AO/EB staining suggests that compound 8f could induce apoptosis in A549 cells. Furthermore, cell cycle analyses show that compound 8f increased G0/G1 A549 cells arrest in a concentration-dependent manner. The preliminary structure-activity relationships (SARs) studies indicated that mono-electron-withdrawing groups (mono-EWGs) on the phenyl ring are positive on the antitumor activity.


1999 ◽  
Vol 37 (4) ◽  
pp. 704 ◽  
Author(s):  
Soo Seog Park ◽  
Dong Eon Moon ◽  
Oh Kyoung Kwon ◽  
Yeon Jang ◽  
Eun Chung Cho ◽  
...  

2017 ◽  
Vol 16 (1) ◽  
pp. 167-167
Author(s):  
M.S. Berke ◽  
Klas S.P. Abelson

Abstract Aims This study investigated the effects of buprenorphine treatment on pain and welfare parameters and model specific parameters in a rat model of monoarthritis to eliminate unnecessary pain from this model. Methods 32 male Sprague Dawley rats were divided into four groups: (1) A negative control without arthritis receiving no analgesia. (2) A positive monoarthritic control group receiving no analgesia, but subcutaneous saline injections twice a day. (3) A positive control with monoarthritis receiving subcutaneous carprofen once a day and saline once a day. (4) A group with monoarthritis receiving subcutaneous buprenorphine twice a day. Monoarthritis was induced with an injection of 0.02 ml Complete Freund’s Adjuvant intra-articularly in the left tibiotarsal joint. Treatment with analgesia was initiated at day 15 and the rats were euthanized at day 23. Results The induced monoarthritis elicited a pronounced acute inflammation. Several parameters such as bodyweight, mobility, stance, joint-stiffness and lameness scores were affected. A marked mechanical hyperalgesia in the tarsal area was observed by Electronic Von Frey testing, but no severe compromise of the animal welfare was seen at any time. Signs of chronic development began to appear from day 10 after the monoarthritic induction. No significant change in serum cytokines and faecal corticosterone measurements was found after administration of buprenorphine. A minor decrease in body weight was seen, and a higher pain tolerance to mechanical stimuli was observed, indicating pain alleviation. The histological examination confirmed monoarthritic development in all monoarthritic rats and revealed periarticular lesions suggesting diffusion of adjuvant from intra-articular injection site to the periphery. Conclusions The study demonstrated that buprenorphine has an analgesic effect in the adjuvant induced monoarthritic rat model, without obvious interference with the development of arthritis.


2019 ◽  
Vol 10 (8) ◽  
pp. 883-892
Author(s):  
L.C. Lew ◽  
Y.Y. Hor ◽  
M.H. Jaafar ◽  
A.S.Y. Lau ◽  
J.S. Ong ◽  
...  

This study aimed to evaluate the anti-ageing effects of different strains of lactobacilli putative probiotics on an ageing rat model as induced by D-galactose and a high fat diet. Male Sprague-Dawley rats were fed with high fat diet (54% kcal fat) and injected with D-galactose daily for 12 weeks to induce ageing. The effects of putative probiotic strains on age-related impairment such as telomere length, plasma lipid peroxidation, hepatic 5’adenosine monophosphate-activated protein kinase (AMPK) expression, as well as endurance performance were evaluated. Administration of statin, Lactobacillus plantarum DR7 (LP-DR7), Lactobacillus fermentum DR9 (LF-DR9), and Lactobacillus reuteri 8513d (LR-8513d) significantly reduced the shortening of telomere and increased the expression of AMPK subunit-α1 (P<0.05). Plasma lipid peroxidation was lower (P<0.05) in groups administered with statin and LF-DR9 as compared to the control. AMPK subunit-α2 was elevated in rats administered with LP-DR7 as compared to the control (P<0.05). Using an in vivo ageing rat model, the current study has illustrated the potentials of lactobacilli putative probiotics in alleviation of age-related impairment in a strain-dependent manner.


2011 ◽  
Vol 345 ◽  
pp. 393-398 ◽  
Author(s):  
Zhi Wang ◽  
Wen Hui Fu ◽  
Xiang Yang Lu ◽  
Guang Xian Cai

This paper focuses on the effect of the venom of the scorpion Buthus martensii on the proliferation of human cervical carcinoma Hela cell line and the related molecular mechanism. MTT test showed that the scorpion venom inhibited proliferation of Hela cells in time-dependent and concentration-dependent manner with 50% inhibitory concentration (IC50) of 34.5 μg/mL(48 h). By using flow cytometry, it was found that the scorpion venom could induce apoptosis and necrosis in Hela cells. RT-PCR and Western blot indicated there were obviously up-regulated in the expressions of p21 protein but the expression of p21 mRNA showed no significant difference in the Hela cell by the scorpion venom. These results suggest that the possible mechanism of the scorpion venom is to activate the expressions of p21 protein and to cause Hela cell apoptosis.


2017 ◽  
Vol 2017 ◽  
pp. 1-11 ◽  
Author(s):  
Mengjiao Chen ◽  
Peijun Ding ◽  
Lili Yang ◽  
Xufeng He ◽  
Chunjie Gao ◽  
...  

To evaluate the anti-inflammatory activities of QRQS against AD and the inhibitory molecular mechanisms of IL-33/ST2 signal transduction, BALB/c mice were divided into six groups (normal control, OVA control, low-dose of QRQS, middle-dose of QRQS, high-dose of QRQS, and cetirizine) and epicutaneously exposed to ovalbumin or PBS for 3 weeks and treated with QRQS for 2 weeks. Skin biopsies and blood samples were obtained for histological study, antibody analysis, and RNA isolation. HaCaT cells, stimulated by TNF-α and IFN-γ, were treated with QRQS to evaluate mRNA and protein expression by RT-PCR and ELISA. QRQS decreased both epidermal and dermal thickness, alleviated dermatitis, and reduced IL-33 and ST2 positive cell numbers. The concentration of specific IgE, IgG, IgG1, and IgG2a antibodies in serum and the expression of IL-33, ST2, IL-1RAcP, IL-4, and IL-13 mRNA in the skin were suppressed. No significant difference exists in TNF-α or IFN-γ. QRQS decreased IL-33 mRNA and protein secretion in HaCaT cells exposed to TNF-α and IFN-γ in a time- and concentration-dependent manner. QRQS regulates related molecule expression of ovalbumin-induced dermatitis involved in the IL-33/ST2 signaling axis in the treatment of acute AD.


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