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Bioavailability and pharmacokinetic studies of eurycomanone from Eurycoma longifolia

Low BS, Ng BH, Choy WP, Yuen KH, Chan KL

Planta Med, 2005 Sep;71(9):803-7.
PMID: 16206032

A validated HPLC analysis of eurycomanone (1), a bioactive quassinoid, in rat plasma following oral and intravenous administration of Eurycoma longifolia Jack extract was developed for pharmacokinetic and bioavailability studies. Relatively high plasma eurycomanone concentrations were detected after an intravenous injection of 10 mg/kg extract F2 containing 1.96 mg/kg of the quassinoid. However, it declined rapidly to zero after 8 h. Its mean elimination rate constant (k(e)), biological half-life (t(1/2)), volume of distribution (V(d)) and clearance (CL) were 0.88 +/- 0.19 h (-1), 1.00 +/- 0.26 h, 0.68 +/- 0.30 L/kg and 0.39 +/- 0.08 L/h/kg, respectively. Following oral administration of eurycomanone, its Cmax and Tmax values were detected as 0.33 +/- 0.03 microg/mL and 4.40 +/- 0.98 h, respectively. The plasma concentration of the quassinoid after oral administration was much lower than after intravenous application in spite of the oral dose being 5 times higher. The results indicate that eurycomanone is poorly bioavailable when given orally. A comparison of the AUC (0-->infinity) obtained orally to that obtained after an intravenous administration (normalized for dose differences) revealed that the absolute bioavailability of the compound was low with 10.5 %. Furthermore, the compound appeared to be well distributed in the extravascular fluids because of its relatively high V(d) value. The poor oral bioavailability was not attributed to instability problems because eurycomanone has been shown to be stable under different pH conditions. Thus, its poor oral bioavailability may be due to poor membrane permeability in view of its low P value and/or high first-pass metabolism.

Matched MeSH terms: Rats, Sprague-Dawley
Polar Quassinoids in Standardized Eurycoma longifolia Extract Formulated into a Lipid-Based Solid Dispersion to Improve Rat Sperm Count

Ma HQ, Ebrahimi F, Low BS, Khan NAK, Chan KL

Phytother Res, 2017 Dec;31(12):1875-1882.
PMID: 28948658 DOI: 10.1002/ptr.5930

Eurycoma longifolia Jack is popularly sought in Southeast Asian countries for traditional remedies to improve sexual performance and fertility. 13α(21)-Epoxyeurycomanone and eurycomanone, two major quassinoids in a root extract (TAF2) were reported to improve rat spermatogenesis and fertility. Unfortunately, these quassinoids possess low bioavailability because of high aqueous solubility and low lipid membrane permeability. Often, other possible barriers may be P-glycoprotein (P-gp) efflux in the gut and presystemic hepatic metabolism. The present study attempted to solve these problems by formulating a lipid-based solid dispersion (TAF2-SD) of optimized mixture of TAF2 and emulsifiers, which was then orally administered to rats prior to sperm count analysis. The TAF2-SD-treated rats showed significantly twofold (p

Matched MeSH terms: Rats, Sprague-Dawley
Comparative ultrastructural hepatic alterations induced by free and liposome-encapsulated mefenamic acid

Jarrar QB, Hakim MN, Cheema MS, Zakaria ZA

Ultrastruct Pathol, 2017 8 23;41(5):335-345.
PMID: 28829237 DOI: 10.1080/01913123.2017.1349850

Mefenamic acid (MFA) is used as an anti-inflammatory, antinociceptive, and antipyretic agent for treatment of a wide range of pathological disorders. While the uncertainty of its safety and the poor oral bioavailability constitute the major limiting factors of its medical use, considerable efforts including liposomal encapsulation are needed to achieve maximum therapeutic advantages. The current work was conducted to investigate the ultrastructural alterations in the liver induced by free MFA and its liposomal preparation. Female Sprague-Dawley rats were treated with daily oral doses of either free MFA or MFA entrapped in Tween 80 inoculated liposomes at the concentration of 80 mg/kg for 28 days. Ultrathin sections were prepared from biopsies taken from the liver of each member of all animals under study and subjected to examination by transmission electron microscopy. The liver of rats that were exposed to liposomal MFA showed more ultrastructural alterations than the rats treated with the free drug. While both groups of rats demonstrated sinusoidal dilatation, Kupffer cell hyperplasia, mitochondrial damage, and nuclear alterations, rats treated with liposome-encapsulated MFA induced an increase in the multiple lysosomes formation, hepatocytic steatosis, and apoptotic activity than free MFA-treated rats. The ultrastructural findings of the present study indicate that the use of liposomal MFA induces more hepatic damage than the use of free MFA.

Matched MeSH terms: Rats, Sprague-Dawley
Fulltext Volumetric changes in the aging rat brain and its impact on cognitive and locomotor functions

Hamezah HS, Durani LW, Ibrahim NF, Yanagisawa D, Kato T, Shiino A, et al.

Exp Gerontol, 2017 12 01;99:69-79.
PMID: 28918364 DOI: 10.1016/j.exger.2017.09.008

Impairments in cognitive and locomotor functions usually occur with advanced age, as do changes in brain volume. This study was conducted to assess changes in brain volume, cognitive and locomotor functions, and oxidative stress levels in middle- to late-aged rats. Forty-four male Sprague-Dawley rats were divided into four groups: 14, 18, 23, and 27months of age. 1H magnetic resonance imaging (MRI) was performed using a 7.0-Tesla MR scanner system. The volumes of the lateral ventricles, medial prefrontal cortex (mPFC), hippocampus, striatum, cerebellum, and whole brain were measured. Open field, object recognition, and Morris water maze tests were conducted to assess cognitive and locomotor functions. Blood was taken for measurements of malondialdehyde (MDA), protein carbonyl content, and antioxidant enzyme activity. The lateral ventricle volumes were larger, whereas the mPFC, hippocampus, and striatum volumes were smaller in 27-month-old rats than in 14-month-old rats. In behavioral tasks, the 27-month-old rats showed less exploratory activity and poorer spatial learning and memory than did the 14-month-old rats. Biochemical measurements likewise showed increased MDA and lower glutathione peroxidase (GPx) activity in the 27-month-old rats. In conclusion, age-related increases in oxidative stress, impairment in cognitive and locomotor functions, and changes in brain volume were observed, with the most marked impairments observed in later age.

Matched MeSH terms: Rats, Sprague-Dawley
Fulltext Anti-atherosclerotic effects of Eurycoma Longifolia (Tongkat Ali) in rats fed on High-fat diet

Fakhria Al-Joufi, Anil K. Saxena, Imad M. Al-Ani, Norlelawati A. Talib, Rafidah H. Mokhtar, Norsidah Ku -Zaifah

International Medical Journal Malaysia, 2017;16(1):83-90.
MyJurnal

Atherosclerosis in cardiovascular disease (CVD) is a growing health problem, especially in developing countries. Hyperlipidemia is known as a dominant risk factor for the development of atherosclerosis. This study was designed to investigate the effects of Eurycoma Longifolia (EL) also known as Malaysian Ginseng/ Tongkat Ali on the testosterone level, biochemical changes of lipid profile and intima media thickness (IMT) in rats fed on high-fat diet. Twenty young, adult male Sprague-Dawley (SD) rats were housed for 12 weeks. After one week of acclimatization, they were randomly divided into four groups of 5 animals each and treated for 12 weeks as follow: Group ND was given only normal diet, group NDEL was given normal diet and EL extracts (15mg/kg) dissolved in distilled water, group HFD was given only high fat diet and group HFDEL was given high fat diet and EL extracts (15mg/kg). Rats which were treated with EL (NDEL and HFDEL) showed a significant increase (p

Matched MeSH terms: Rats, Sprague-Dawley
Microwave as skin permeation enhancer for transdermal drug delivery of chitosan-5-fluorouracil nanoparticles

Nawaz A, Wong TW

Carbohydr Polym, 2017 Feb 10;157:906-919.
PMID: 27988008 DOI: 10.1016/j.carbpol.2016.09.080

This study investigated transdermal drug delivery mechanisms of chitosan nanoparticles with the synergistic action of microwave in skin modification. Chitosan nanoparticles, with free or conjugated 5-fluorouracil, were prepared by nanospray-drying technique. Their transdermal drug delivery profiles across untreated and microwave-treated skins (2450MHz 5min, 5+5min; 3985MHz 5min) were examined. Both constituent materials of nanoparticles and drug encapsulation were required to succeed transdermal drug delivery. The drug transport was mediated via nanoparticles carrying drug across the skin and/or diffusion of earlier released drug molecules from skin surfaces. The drug/nanoparticles transport was facilitated through constituent nanoparticles and microwave fluidizing protein/lipid domains of epidermis and dermis (OH, NH, CH, CN) and dermal trans-to-gauche lipid conformational changes. The microwave induced marked changes to the skin ceramide content homogeneity. The chitosan nanoparticles largely affected the palmitic acid and keratin domains. Combined microwave and nanotechnologies synergize transdermal drug delivery.

Matched MeSH terms: Rats, Sprague-Dawley
Fulltext Vitamin E improved bone strength and bone minerals in male rats given alcohol

Zakaria S, Mat-Husain SZ, Ying-Hwey K, Xin-Kai K, Mohd-Badawi A, Abd-Ghani NA, et al.

Iran J Basic Med Sci, 2017 Dec;20(12):1360-1367.
PMID: 29238472 DOI: 10.22038/IJBMS.2017.9610

Objectives: Alcohol consumption induces oxidative stress on bone, which in turn increases the risk of osteoporosis. This study determined the effects of vitamin E on bone strength and bone mineral content in alcohol-induced osteoporotic rats.
Materials and Methods: Three months old Sprague Dawley male rats were randomly divided into 5 groups: (I) control group; (II) alcohol (3g/kg) + normal saline; (III) alcohol (3g/kg) + olive oil; (IV) alcohol (3g/kg) + alpha-tocopherol (60mg/kg) and (V) alcohol (3g/kg) + palm vitamin E (60mg/kg). The treatment lasted for three months. Following sacrifice, the right tibia was subjected to bone biomechanical test while the lumbar (fourth and fifth lumbar) and left tibia bones were harvested for bone mineral measurement.
Results: Alcohol caused reduction in bone biomechanical parameters (maximum force, ultimate stress, yield stress and Young's modulus) and bone minerals (bone calcium and magnesium) compared to control group (P<0.05). Palm vitamin E was able to improve bone biomechanical parameters by increasing the maximum force, ultimate stress and Young's modulus (P<0.05) while alpha-tocopherol was not able to. Both alpha-tocopherol and palm vitamin E were able to significantly increase tibia calcium and magnesium content while only alpha-tocopherol caused significant increase in lumbar calcium content (P<0.05).
Conclusion: Both palm vitamin E and alpha-tocopherol improved bone mineral content which was reduced by alcohol. However, only palm vitamin E was able to improve bone strength in alcohol treated rats.

Matched MeSH terms: Rats, Sprague-Dawley
Fulltext Short-term consumption of Gelam honey reduces Triglyceride level

Samat, S., Mohd Nor, N., Hussein, F. N., Eshak, Z., Ismail, W. I. W.

International Food Research Journal, 2017;24(4):1519-1524.
MyJurnal

The study was carried out to evaluate short-term administration of Gelam honey. A single oral
administration of the honey at a dose of 5000 mg/kg body weight on male Sprague Dawley rats
(test group) for 14 days did not produce any signs of toxicity, behavioral changes, mortality, changes on gross appearance or histopathological changes of internal organs. The examinations
of signs, animal behavior and health monitoring showed no abnormalities in the test group as
compared to the rats unfed with the honey (control group). The test group had progressive increased both body weight and in the meal pattern analysis. However, triglycerides level was found significantly decreased in the test group. It suggested that the honey might have a decent effect in controlling the blood triglyceride level. Polyphenol contents in the honey may play the role to reduce the trigyceride level. Biochemical test for aspartate aminotransferase (AST), alanine transaminase (ALT), urea, creatinine, cholesterol and glucose of rats in the test group were in the normal range compared to the control. There were no significant changes in the absolute and relative organ weight between the two groups. As a conclusion, tested dose of Gelam honey is safe and has medical potential. Meanwhile, lethal dose (LD50) of the honey was found to be greater than 5000 mg/kg body weight. Long period of Gelam honey consumption should be conducted to observe and confirm those effects.

Matched MeSH terms: Rats, Sprague-Dawley
Microwaved bacterial cellulose-based hydrogel microparticles for the healing of partial thickness burn wounds

Pandey M, Mohamad N, Low WL, Martin C, Mohd Amin MC

Drug Deliv Transl Res, 2017 02;7(1):89-99.
PMID: 27815776 DOI: 10.1007/s13346-016-0341-8

Burn wound management is a complex process because the damage may extend as far as the dermis which has an acknowledged slow rate of regeneration. This study investigates the feasibility of using hydrogel microparticles composed of bacterial cellulose and polyacrylamide as a dressing material for coverage of partial-thickness burn wounds. The microparticulate carrier structure and surface morphology were investigated by Fourier transform infrared, X-ray diffraction, elemental analysis, and scanning electron microscopy. The cytotoxicity profile of the microparticles showed cytocompatibility with L929 cells. Dermal irritation test demonstrated that the hydrogel was non-irritant to the skin and had a significant effect on wound contraction compared to the untreated group. Moreover, histological examination of in vivo burn healing samples revealed that the hydrogel treatment enhanced epithelialization and accelerated fibroblast proliferation with wound repair and intact skin achieved by the end of the study. Both the in vitro and in vivo results proved the biocompatibility and efficacy of hydrogel microparticles as a wound dressing material.

Matched MeSH terms: Rats, Sprague-Dawley
Fulltext Edible bird's nest impact on rats' uterine histomorphology, expressions of genes of growth factors and proliferating cell nuclear antigen, and oxidative stress level

Albishtue AA, Yimer N, Zakaria MZA, Haron AW, Yusoff R, Assi MA, et al.

Vet World, 2018 Jan;11(1):71-79.
PMID: 29479160 DOI: 10.14202/vetworld.2018.71-79

Aim: This study aimed to evaluate the effect of edible bird's nest (EBN) supplementation on the uteri of rats based on analyses of the morphological and histomorphometric changes, and expressions of epidermal growth factor (EGF) and its receptor (REGF) genes, vascular endothelial growth factor (VEGF), proliferating cell nuclear antigen (PCNA), and steroid receptors.
Materials and Methods: Twenty-four: Sprague Dawley rats were equally distributed into the following four groups: G1 (control), G2, G3, and G4 represented the groups treated with EBN at graded concentrations of 0, 30, 60, and 120 mg/kg body weight (BW) per day for 8 weeks, respectively. During the experimental period, the BW of each rat was recorded weekly. At the proestrus stage of estrous cycle, blood samples were collected from the hearts of anesthetized rats that were later sacrificed. The uteri were removed for histological and immunohistochemical analyses.
Results: The EBN-treated groups showed an increase in the weights and lengths of uteri as compared to the control. Results showed that relative to G1 and G2, G3 and G4 exhibited proliferation in their uterine luminal and glandular epithelia and uterine glands, and up-regulated expressions of EGF, REGF, VEGF, PCNA, and progesterone receptor, and estrogen receptor in their uteri. The EBN increased the antioxidant (AO) and total AO capacities and reduced the oxidative stress (OS) levels in non-pregnant rats.
Conclusion: Findings of this study revealed that EBN promotes proliferation of the uterine structures as evidenced by the upregulation of the expressions of steroid receptors, EGF, REGF, VEGF, and PCNA in the uterus and increased in the plasma concentrations of AO and reduced levels of OS.

Matched MeSH terms: Rats, Sprague-Dawley
Protective effect of curcumin on experimentally induced arthritic rats: detailed histopathological study of the joints and white blood cell count

Kamarudin TA, Othman F, Mohd Ramli ES, Md Isa N, Das S

EXCLI J, 2012;11:226-36.
PMID: 27366139

Curcuma longa (turmeric) rhizomes contains curcumin, an active compound which possesses anti-inflammatory effects. Collagen-induced arthritis (CIA) is an accepted experimental animal model of rheumatoid arthritis. The present study aimed to observe the histological changes in the joints of experimental arthritic rats treated with curcumin. Twenty four male Sprague-Dawley (approximately 7 weeks-old) rats were randomly divided into four groups. Three groups were immunized with 150 µg collagen. All rats with established CIA, with arthritis scores exceeding 1, were orally treated with betamethasone (0.5 mg/ml/kg body weight), curcumin (110 mg/ml/kg body weight) or olive oil (1.0 ml/kg body weight) daily, for two weeks. One remaining group was kept as normal control. Treatment with 110 mg/ml/kg curcumin showed significant mean differences in the average white blood cell (WBC) count (p<0.05), cell infiltration, bone and cartilage erosion scores (p<0.05) compared to the olive oil treated group. Pannus formation scores showed that curcumin supplementation successfully suppressed the pannus formation process that occurred in the articular cartilage of the CIA joints. The mean difference for histological scores for the curcumin group was insignificant compared to the betamethasone treated group. It is concluded that supplementation of curcumin has protective effect on the histopathological and degenerative changes in the joints of CIA rats which was at par with betamethasone.

Matched MeSH terms: Rats, Sprague-Dawley
Fulltext 1H NMR-based Investigation of Metabolic Response to Electro-Acupuncture Stimulation

Lin C, Wei Z, Cheng KK, Xu J, Shen G, She C, et al.

Sci Rep, 2017 07 28;7(1):6820.
PMID: 28754994 DOI: 10.1038/s41598-017-07306-5

Acupuncture is a traditional Chinese medicine therapy that has been found useful for treating various diseases. The treatments involve the insertion of fine needles at acupoints along specific meridians (meridian specificity). This study aims to investigate the metabolic basis of meridian specificity using proton nuclear magnetic resonance (1H NMR)-based metabolomics. Electro-acupuncture (EA) stimulations were performed at acupoints of either Stomach Meridian of Foot-Yangming (SMFY) or Gallbladder Meridian of Foot-Shaoyang (GMFS) in healthy male Sprague Dawley (SD) rats. 1H-NMR spectra datasets of serum, urine, cortex, and stomach tissue extracts from the rats were analysed by multivariate statistical analysis to investigate metabolic perturbations due to EA treatments at different meridians. EA treatment on either the SMFY or GMFS acupoints induced significant variations in 31 metabolites, e.g., amino acids, organic acids, choline esters and glucose. Moreover, a few meridian-specific metabolic changes were found for EA stimulations on the SMFY or GMFS acupoints. Our study demonstrated significant metabolic differences in response to EA stimulations on acupoints of SMFY and GMFS meridians. These results validate the hypothesis that meridian specificity in acupuncture is detectable in the metabolome and demonstrate the feasibility and effectiveness of a metabolomics approach in understanding the mechanism of acupuncture.

Matched MeSH terms: Rats, Sprague-Dawley
5-Fluorouracil ethosomes - skin deposition and melanoma permeation synergism with microwave

Khan NR, Wong TW

Artif Cells Nanomed Biotechnol, 2018;46(sup1):568-577.
PMID: 29378453 DOI: 10.1080/21691401.2018.1431650

This study focuses on the use of ethosome and microwave technologies to facilitate skin penetration and/or deposition of 5-fluorouracil in vitro and in vivo. Low ethanol ethosomes were designed and processed by mechanical dispersion technique and had their size, zeta potential, morphology, drug content and encapsulation efficiency characterized. The skin was pre-treated with microwave at 2450 MHz for 2.5 min with ethosomes applied topically and subjected to in vitro and in vivo skin drug permeation as well as retention evaluation. The drug and/or ethosomes cytotoxicity, uptake and intracellular trafficking by SKMEL-28 melanoma cell culture were evaluated. Pre-treatment of skin by microwave promoted significant drug deposition in skin from ethosomes in vitro while keeping the level of drug permeation unaffected. Similar observations were obtained in vivo with reduced drug permeation into blood. Combination ethosome and microwave technologies enhanced intracellular localization of ethosomes through fluidization of cell membrane lipidic components as well as facilitating endocytosis by means of clathrin, macropinocytosis and in particularly lipid rafts pathways. The synergistic use of microwave and ethosomes opens a new horizon for skin malignant melanoma treatment.

Matched MeSH terms: Rats, Sprague-Dawley
Synthesis of Novel Derivatives of Quinazoline Schiff base Compound Promotes Epithelial Wound Healing

Bagheri E, Saremi K, Hajiaghaalipour F, Faraj FL, Ali HM, Abdulla MA, et al.

Curr Pharm Des, 2018;24(13):1395-1404.
PMID: 29384057 DOI: 10.2174/1381612824666180130124308

Quinazoline is an aromatic bicyclic compound exhibiting several pharmaceutical and biological activities. This study was conducted to investigate the potential wound healing properties of Synthetic Quinazoline Compound (SQC) on experimental rats. The toxicity of SQC was determined by MTT cell proliferation assay. The healing effect of SQC was assessed by in vitro wound healing scratch assay on the skin fibroblast cells (BJ-5ta) and in vivo wound healing experiment of low and high dose of SQC on adult Sprague-Dawley rats compared with negative (gum acacia) and positive control (Intrasite-gel). Hematoxylin and Eosin (H&E), Masson's Trichrome (MT) staining and immunohistochemistry analysis were performed to evaluate the histopathological alterations and proteins expression of Bax and Hsp70 on the wound tissue after 10 days. In addition, levels of antioxidant enzymes (catalase, glutathione peroxidase and superoxide dismutase), and malondialdehyde (MDA) were measured in wound tissue homogenates. The SQC significantly enhanced BJ-5ta cell proliferation and accelerated the percentage of wound closure, with less scarring, increased fibroblast and collagen fibers and less inflammatory cells compared with the negative control. The compound also increases endogenous enzymes and decline lipid peroxidation in wound homogenate.

Matched MeSH terms: Rats, Sprague-Dawley
Intraocular pressure lowering effect and structure-activity relationship of imidazo[1,2-a]benzimidazole and pyrimido[1,2-a]benzimidazole compounds in ocular normotensive rats: Insight on possible link with hypotensive activity

Marcus AJ, Iezhitsa I, Agarwal R, Vassiliev P, Spasov A, Zhukovskaya O, et al.

Eur J Pharm Sci, 2018 Mar 01;114:245-254.
PMID: 29274441 DOI: 10.1016/j.ejps.2017.12.015

In an effort to find new ocular hypotensive drug candidates, a total of 27 condensed benzimidazoles based compounds were screened. This study was done in normotensive rats and rebound tonometry was used to estimate IOP. All compounds were topically applied as a single drop, unilaterally, at 3 different concentrations (0.1%, 0.2% and 0.4%). The contralateral eye was instilled with vehicle and served as control. The IOP reduction was measured up to 6h. It was observed that with a single topical instillation, compounds RU 551, RU 555, RU839 (pyrimido[1,2-a]benzimidazole derivatives), and RU 615 (imidazo[1,2-a]benzimidazole derivative) showed significant IOP lowering activities in ocular normotensive rats. All other compounds showed none, weak and inconsistent IOP lowering effect. The relationship between ability of IOP lowering and hypotensive activities was studied. According to the pharmacophore analysis, the class of pyrimido[1,2-a]benzimidazole is more promising than the class of imidazo[1,2-a]benzimidazole as a source of compounds with high IOP lowering activity. Pharmacophore analysis also showed that the critical features of high IOP lowering activity are methoxyphenyl and [phenyl]alkyl fragments, and non-conjugated six-membered heterocyclic ring.

Matched MeSH terms: Rats, Sprague-Dawley
Citrus leaf extract reduces blood pressure and vascular damage in repeatedly heated palm oil diet-Induced hypertensive rats

Siti HN, Kamisah Y, Nur Iliyani MI, Mohamed S, Jaarin K

Biomed Pharmacother, 2017 Mar;87:451-460.
PMID: 28068636 DOI: 10.1016/j.biopha.2016.12.075

Prolonged consumption of repeatedly heated vegetable oil increases blood pressure. This study aimed to determine the effects of Citrus leaf extract, (CLE) on blood pressure, blood pressure-regulating enzymes and mediators, as well as aortic histomorphometry in heated palm oil induced-hypertension. Male Sprague Dawley rats (n=56) were divided into seven groups; control group was given normal diet and the other groups were fed with palm oil-enriched diet (15% w/w) either fresh (FPO), five-time-heated (5HPO) or ten-time-heated (10HPO) with or without CLE (0.15%, w/w) supplementation. CLE supplementation reduced the heated oil-raising effect of blood pressure, plasma TBARS, thromboxane and angiotensin-1 converting enzyme in 5HPO but not in 10HPO group. CLE increased serum heme oxygenase-1 in both 5HPO and 10HPO groups. CLE supplementation reduced the increase in aortic intima-media thickness, intima-media area and circumferential wall tension in 5HPO group but not in 10HPO group. These findings suggested that CLE supplementation reduces the blood pressure-raising effects of 5HPO and vascular damage, possibly through its antioxidant effect by modulating vasoactive mediators and blood pressure-regulating enzymes.

Matched MeSH terms: Rats, Sprague-Dawley
Fulltext The effects of Cicletanine, a new antihypertensive agent on insulin release in rat isolated pancreas by the perfusion technique

Mashori GR, Tariq AR, Shahimi MM, Suhaimi H

Singapore Med J, 1996 Jun;37(3):278-81.
PMID: 8942229

Treatment of hypertension has reduced the incidence of stroke, heart failure and renal failure. However, the incidence of coronary heart disease is not reduced to the same degree. Many of the drugs advocated as first-line drugs in the step-wise therapy have been shown to cause carbohydrate intolerance and it is an independent risk factor in the development of coronary heart disease. It is thus important to identify the antihypertensive drugs that may cause deterioration in glucose tolerance. Cicletanine, the first derivative of the furopyridines, is a new class of antihypertensive agents. It acts directly on vascular endothelium cells by increasing prostacyclin synthesis. It also decreases intracytosolic calcium levels in smooth muscles. The purpose of this study is to evaluate the effects of Cicletanine on insulin release in rat isolated pancreas by the perfusion technique adapted from Loubatieres and co-workers (1972). Doses used were based on therapeutic peak plasma concentration. Diazoxide was used as a positive control ie a known insulin suppressant. Cicletanine at 1/10 and equivalent therapeutic concentrations (0.5 microgram/mL and 5.0 micrograms/mL) did not suppress insulin release. However, at concentration exceeding 10X its therapeutic levels (50 micrograms/mL) it begins to suppress insulin release. In conclusion, Cicletanine did not inhibit insulin release at concentrations within the therapeutic range.

Matched MeSH terms: Rats, Sprague-Dawley
Fulltext The Potential Chemopreventive Effect of Andrographis paniculata on 1,2-Dimethylhydrazine and High-Fat-Diet-Induced Colorectal Cancer in Sprague Dawley Rats

Subarmaniam T, Mahmad Rusli RN, Perumal KV, Yong YK, Hadizah S, Othman F, et al.

Int J Mol Sci, 2023 Mar 09;24(6).
PMID: 36982300 DOI: 10.3390/ijms24065224

Colorectal cancer (CRC) is responsible for a notable rise in the overall mortality rate. Obesity is found to be one of the main factors behind CRC development. Andrographis paniculata is a herbaceous plant famous for its medicinal properties, particularly in Southeast Asia for its anti-cancer properties. This study examines the chemopreventive impact of A. paniculata ethanolic extract (APEE) against a high-fat diet and 1,2-dimethylhydrazine-induced colon cancer in Sprague Dawley rats. Sprague Dawley rats were administered 1,2-dimethylhydrazine (40 mg/kg, i.p. once a week for 10 weeks) and a high-fat diet (HFD) for 20 weeks to induce colorectal cancer. APEE was administered at 125 mg/kg, 250 mg/kg, and 500 mg/kg for 20 weeks. At the end of the experiment, blood serum and organs were collected. DMH/HFD-induced rats had abnormal crypts and more aberrant crypt foci (ACF). APEE at a dose of 500 mg/kg improved the dysplastic state of the colon tissue and caused a 32% reduction in the total ACF. HFD increased adipocyte cell size, while 500 mg/kg APEE reduced it. HFD and DMH/HFD rats had elevated serum insulin and leptin levels. Moreover, UHPLC-QTOF-MS analysis revealed that APEE was rich in anti-cancer phytochemicals. This finding suggests that APEE has anti-cancer potential against HFD/DMH-induced CRC and anti-adipogenic and anti-obesity properties.

Matched MeSH terms: Rats, Sprague-Dawley
Fulltext Elateriospermum tapos Yoghurt as a Therapeutic Intervention for Obesity-Associated Cognitive Impairments and Anxiety-like Behaviour in a High Fat Diet Maternal Obese Rat Model

Naomi R, Teoh SH, Rusli RNM, Embong H, Bahari H, Kumar J

Nutrients, 2023 May 15;15(10).
PMID: 37242195 DOI: 10.3390/nu15102312

Maternal obesity can be considered an intergenerational cycle and is also an important indicator of cognitive impairments. It is thought that using natural products is the best and safest way to combat maternal obesity and associated complications. Recent studies have shown that Elateriospermum tapos (E. tapos) contains bioactive compounds with anti-obesity effects, and yoghurt is a convenient medium for supplementing obese maternal rats with E. tapos extract. Thus, the aim of this study is to investigate the impact of E. tapos in yoghurt on maternally obese rats' cognitive function supplemented with a high-fat diet (HFD). In this study, 48 female Sprague-Dawley rats were used. The rats were fed HFD for a period of 16 weeks to induce obesity, after which they were allowed to mate. Upon confirmation of pregnancy, obese rats were given varying doses of E. tapos (5, 50, and 500 mg/kg) in yoghurt until postnatal (PND) day 21. On PND 21, the dams' body mass index (BMI), Lee index, abdominal circumference, oxidative status, and metabolic profile were measured. The behavioral tests (open field, place, and object recognition) were conducted on PND 21 to access memory. The results show that the 50 and 500 mg/kg E. tapos in yoghurt supplemented groups had similar BMI, Lee index, abdominal circumference, lipid profile, FBG, insulin, FRAP, and GSH levels, as well as a similar recognition index, in comparison with the control group supplemented with saline. In conclusion, the results of this study indicate that the newly formulated E. tapos in yogurt can act as an anti-obesity agent in maternal obesity, alleviate anxiety, and enhance hippocampal-dependent memory.

Matched MeSH terms: Rats, Sprague-Dawley
Fulltext Enrichment of Eucalyptus oil nanoemulsion by micellar nanotechnology: transdermal analgesic activity using hot plate test in rats' assay

Aziz ZAA, Nasir HM, Ahmad A, Setapar SHM, Ahmad H, Noor MHM, et al.

Sci Rep, 2019 Sep 23;9(1):13678.
PMID: 31548590 DOI: 10.1038/s41598-019-50134-y

Eucalyptus globulus is an aromatic medicinal plant which known for its 1,8-cineole main pharmacological constituent exhibits as natural analgesic agent. Eucalyptus globulus-loaded micellar nanoparticle was developed via spontaneous emulsification technique and further evaluation for its analgesic efficacy study, in vivo analgesic activity assay in rats. The nanoemulsion system containing Eucalyptus-micelles was optimized at different surfactant types (Tween 40, 60 and 80) and concentrations (3.0, 6.0, 9.0, 12.0, 15.0, and 18.0 wt. %). These formulations were characterized by thermodynamically stability, viscosity, micelles particle size, pH, and morphology structure. The spontaneous emulsification technique offered a greener micelles formation in nanoemulsion system by slowly titrated of organic phase, containing Eucalyptus globulus (active compound), grape seed oil (carrier oil) and hydrophilic surfactant into aqueous phase, and continuously stirred for 30 min to form a homogeneity solution. The characterizations evaluation revealed an optimized formulation with Tween 40 surfactant type at 9.0 wt. % of surfactant concentration promoted the most thermodynamic stability, smaller micelles particle size (d = 17.13 ± 0.035 nm) formed with spherical shape morphological structure, and suitable in viscosity (≈2.3 cP) and pH value (6.57) for transdermal purpose. The in vivo analgesic activity assay of optimized emulsion showed that the transdermal administration of micellar nanoparticle of Eucalyptus globulus on fore and hind limb of rats, possessed the central and peripheral analgesic effects by prolonged the rats pain responses towards the heat stimulus after being put on top of hot plate (55 °C), with longest time responses, 40.75 s at 60 min after treatment administration. Thus, this study demonstrated that micellar nanoparticle of Eucalyptus globulus formed in nanoemulsion system could be promising as an efficient transdermal nanocarrier for the analgesic therapy alternative.

Matched MeSH terms: Rats, Sprague-Dawley

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