Studies of the Toxicological Potential of Capsinoids, XI: Pharmacokinetic and Tissue Distribution Study of 14C-Dihydrocapsiate and Metabolites in Rats

2010 ◽  
Vol 29 (2_suppl) ◽  
pp. 3S-14S ◽  
Author(s):  
Bruce K. Bernard ◽  
Kazuyuki Ubukata ◽  
Ryuichi Mihara ◽  
Yoshiaki Sato ◽  
Hiroyuki Nemoto
Keyword(s):  
Body Weight ◽  
Plasma Concentration ◽  
Vanillic Acid ◽  
Male Rats ◽  
Vanillyl Alcohol ◽  
Tissue Concentrations ◽  
Distribution Study ◽  
Maximal Plasma ◽  
Tissue Distribution Study ◽  
Kidney Liver

Pharmacokinetics of a single gavage dose of 14C-labeled dihydrocapsiate (10 mg/kg) were investigated in male rats. Maximal plasma concentration was achieved in 40 minutes and exhibited an apparent half-life of 2.4 hours. Excretion of radioactivity in the urine, feces, and expired air was 78.2%, 19.4%, and 0.5% of the dose, respectively. Highest tissue concentrations were achieved in the kidney, liver, and blood; the data indicate that radioactivity accumulation following daily exposure at a dose of 10 mg/kg body weight is unlikely. Radioactivity in the plasma was associated with metabolites and their conjugates, probably vanillyl alcohol, vanillic acid, glucuronide of vanillyl alcohol, sulphate of vanillyl alcohol, and sulphate of vanillic acid. These results suggest dihydrocapsiate is metabolized by hydrolysis in the gut, or esterase or other enzymes in the blood, and the metabolites were rapidly absorbed and converted to their conjugates in the liver and eliminated by the kidneys into the urine.

DYNAMIC STUDY OF POST-NATAL THYROID FUNCTION IN THE RAT

1976 ◽  
Vol 83 (4) ◽  
pp. 752-762 ◽  
Author(s):  
E. Vigouroux
Keyword(s):  
Body Weight ◽  
Plasma Concentration ◽  
Thyroid Function ◽  
Rate Constant ◽  
Turnover Rate ◽  
Single Injection ◽  
Iodine Content ◽  
Adult Females ◽  
Maximal Plasma ◽  
Old Rats

ABSTRACT The thyroid function in development was investigated in post-natal rats. The thyroid iodine content rapidly increased from birth (137 ± 26 ng iodine/mg thyroid) up to day 10 (338 ± 42 ng iodine/mg thyroid) then increased more slowly up to day 30 (425 ± 34 ng iodine/mg thyroid). The maximal plasma concentration of thyroxine was observed on day 16 (56.9 ± 3.5 ng T4/ml) and of iodide on day 10 (110.2 ± 12.6 ng I−/ml). The turnover rate constant of extrathyroidal thyroxine was higher at birth (8.0 ± 2.3 %/h) than at any older age studied (average 6 %/h). Thyroxine secretion by the thyroid was more intense before weaning (37 ng hormonal iodine/h/100 g body weight on days 10 and 20) than after weaning (22 ± 6 ng hormonal iodine/h/100 g body weight in 30 days old rats). The peripheral deiodination rate of thyroxine represented about 90 % thyroxine secretion rate in newborn and 10 days old rats and only 40% in adult females. In pre-weaning rats, after a single injection of both [131I]L-T4 and [125I]Na, extrathyroidal radioactivity disappeared more slowly than in 30 days old rats and adult animals. This suggests that iodide concentrations of extrathyroidal tissues are higher before than after weaning.

Intestinal Absorption, Pharmacokinetics and Tissue Distribution of Gossypol Nanosuspensions

2014 ◽  
Vol 1015 ◽  
pp. 708-712
Author(s):  
Si Tao Yang ◽  
Xue Ying ◽  
Hui Tang ◽  
Jian Chen Wang ◽  
Bing Bing Wu
Keyword(s):  
Plasma Concentration ◽  
Tissue Distribution ◽  
Intestinal Absorption ◽  
Reticuloendothelial System ◽  
Polyphenolic Compounds ◽  
Water Soluble ◽  
High Uptake ◽  
Distribution Study ◽  
Poorly Water Soluble ◽  
Tissue Distribution Study

Gossypol (GP) is a kind of poorly water-soluble polyphenolic compounds. In this study, gossypol nanosuspensions (GP-NS) were prepared. The ability of intestinal absorption was evaluated. The result indicated that GP-NS could be absorbed in whole intestinal sections and permeated across the intestine, the process of gossypol nanosuspensions were not affected by P-gp efflux.The pharmacokinetics and tissue distribution of GP-NS after intravenous administration to mice was studied. GP-NS resulted in a higher plasma concentration and lower clearance.The tissue distribution study indicated that GP-NS showed a high uptake in reticuloendothelial system organs. In conclusion, the nanosuspensions system is a promising approach for gossypol.

Reproductive toxicity and tissue concentrations of lindane in adult male rats

1996 ◽  
Vol 15 (5) ◽  
pp. 406-410 ◽  
Author(s):  
PR Dalsenter ◽  
AS Faqi ◽  
J. Webb ◽  
H-J. Merker ◽  
I. Chahoud
Keyword(s):  
Electron Microscopy ◽  
Body Weight ◽  
Adipose Tissue ◽  
Sertoli Cells ◽  
Reproductive Toxicity ◽  
Complete Loss ◽  
Male Rats ◽  
Histological Investigation ◽  
Tissue Concentrations ◽  
Different Tissues

1 The effects of lindane on the reproductive system and its concentration in different tissues were investigated. Groups were dosed orally with 6 mg lindane/kg for 5 days or with a single dose of 30 mg/kg body weight. 2 The results indicate that the number (mio) of sperma tids counted in the testes of both treated groups 2 weeks after treatment were significantly reduced compared to the control rats. Effects on the number of sperms were observed in both treated groups, but significant differences were only revealed on those with 30 mg/kg. 3 The concentration (μg/g tissue) of lindane in adipose tissue, liver, brain and testis was determined 24 h and 2 weeks after the last treatment. Lindane was detected in the testis of both groups 24 h and 2 weeks after the last treatment. 4 Histological investigation by electron microscopy revealed a pronounced ballooning of Sertoli cells accompanied by fragmentation or complete loss of organelles. 5 According to the result obtained, it is evident that lindane passes through the testis and exerts its toxic effect.

Pharmacokinetics and Tissue Distribution Study of Ferruginol in Wistar Rat by High-performance Liquid Chromatography

2018 ◽  
Vol 15 (1) ◽  
pp. 67-73 ◽  
Author(s):  
Guiyun Cao ◽  
Suqiao Han ◽  
Keke Li ◽  
Li Shen ◽  
Xiaohong Wang ◽  
...  
Keyword(s):  
Tissue Distribution ◽  
Mobile Phase ◽  
High Performance ◽  
Wistar Rat ◽  
Freezing And Thawing ◽  
Promising Candidate ◽  
Distribution Study ◽  
Substance Loss ◽  
Tissue Distribution Study ◽  
The Brain

Background: Ferruginol (FRGN) exhibits a broad range of pharmacological properties which make it a promising candidate for chemoprevention. However, little is known about its absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties. Methods: A rapid, sensitive and specific HPLC-DAD method was established to quantify FRGN in the plasma and tissues of Wistar rats. After extraction of FRGN with ethyl acetate (EtOAc), chromatographic separation was performed on a YMC ODS C18 column (250 × 4.6 mm I.D., 5 µm) with a mobile phase consisting of methanol-water (92:8, v/v) at a flow rate of 0.9 mL/min. Detection was conducted with a wavelength of 273 nm at 25 °C. Results: The calibration curves for FRGN were linear in the concentration range of 0.5-20 µg/mL for plasma, 0.5-10 µg/mL for heart, liver, spleen, lung, kidney, stomach, intestine, brain and muscle. After three cycles of freezing and thawing, the concentration variations were within ± 7% of nominal concentrations, indicating no significant substance loss during repeated thawing and freezing. The assay was applied to pharmacokinetic and tissue distribution study in rats. Results suggested that lung, heart, liver, spleen and kidney were the major distribution tissues of FRGN in rats, and FRGN could permeate the blood-brain barrier to distribute in the brain of rats. Conclusion: The information provided by this research is very useful for gaining knowledge of the pharmacokinetic process and tissue distribution of FRGN.

Effect of Opuntia dejecta (Salm-Dyck) flowers in liver of fructose-fed rats: Biochemicals, enzymatic and histological studies

2021 ◽  
pp. 096032712110134
Author(s):  
O Zouaoui ◽  
K Adouni ◽  
A Jelled ◽  
A Thouri ◽  
A Ben Chrifa ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Antioxidant Activity ◽  
Body Weight ◽  
Diabetes Type 2 ◽  
Male Rats ◽  
Control Group ◽  
Standard Drug ◽  
High Fructose ◽  
Group A ◽  
Histological Architecture

Phytochemical composition and antioxidant activity of flowers decoction at post-flowering stage (F3D) of Opuntia dejecta were determined. The obtained findings demonstrate that F3D has a marked antioxidant activity in all tested assays. Furthermore, the present study was designed to test the protective activity of F3D against induced Diabetes type 2 (DT2) in male rats. Those metabolic syndromes were induced by a high-fructose diet (HFD) (10% fructose solution) for a period of 20 weeks. F3D was administered orally (100 and 300 mg/kg body weight) daily for the last 4 weeks. Metformin (150 mg/kg body weight) was used as a standard drug and administrated orally for the last 4 weeks. The results showed a significant increase in blood glucose, triglycerides and hepatic markers (ALAT, ASAT and ALK-P) in HFD group. A significant increase in hepatic TBARS and a significant decrease in SOD, CAT and GPX were observed in fructose fed rats compared to control group. Administration of F3D showed a protective effect in biochemical and oxidative stress parameters measured in this study. Also, oral administration of F3D restored the histological architecture of rat liver in comparison with rats fed HFD. In conclusion, F3D attenuated hepatic oxidative stress in fructose-fed rats.

Potential anti-toxic effect of d-ribose-l-cysteine supplement on the reproductive functions of male rats administered cyclophosphamide

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Gabriel O. Oludare ◽  
Gbenga O. Afolayan ◽  
Ganbotei G. Semidara
Keyword(s):  
Body Weight ◽  
Single Dose ◽  
Sperm Motility ◽  
Sperm Count ◽  
Male Rats ◽  
Oxidative Enzymes ◽  
Protective Effects ◽  
Testosterone Levels ◽  
Group I ◽  
Antioxidant Defence System

Abstract Objectives This study aimed to access the protective effects of d-ribose-l-cysteine (DRLC) on cyclophosphamide (CPA) induced gonadal toxicity in male rats. Methods Forty-eight male Sprague-Dawley rats were divided into six groups of eight rats each. Group I the control, received distilled water (10 ml/kg), Group II received a single dose of CPA 100 mg/kg body weight intraperitoneally (i.p), Groups III and IV received a single dose of CPA at 100 mg/kg (i.p) and then were treated with DRLC at 200 mg/kg bodyweight (b.w) and 400 mg/kg b.w for 10 days, respectively. Rats in Groups V and VI received DRLC at 200 and 400 mg/kg b.w for 10 days, respectively. DRLC was administered orally. Results Results showed that CPA increased percentage of abnormal sperm cells and reduced body weight, sperm count, sperm motility, follicle-stimulating hormone (FSH), luteinizing hormone (LH) and testosterone levels (p<0.05). CPA also induced oxidative stress as indicated by the increased malondialdehyde (MDA) content and reduced activities of the oxidative enzymes measured (p<0.05). Liver enzymes were elevated while the blood cells production was decreased in the rats administered CPA. DRLC supplementation enhanced the antioxidant defence system as indicated in the reduced MDA levels and increased activities of the antioxidant enzymes when compared with CPA (p<0.05). Bodyweight, sperm count, sperm motility, FSH, and testosterone levels were increased in the CPA + DRLC II group compared with CPA (p<0.05). Conclusions The results of this present study showed that DRLC has a potential protective effect on CPA-induced gonadotoxicity.

scholarly journals Chinese Herbal Medicine Alleviates Thyroidectomy-Induced Cardiopulmonary Exercise Dysfunction in Rats

2020 ◽  
Vol 2020 ◽  
pp. 1-8 ◽  
Author(s):  
Tai-Yuan Chuang ◽  
Chia-Ying Lien ◽  
Chih-Hsiang Hsu ◽  
Chen-Wen Lu ◽  
Chung-Hsin Wu
Keyword(s):  
Blood Flow ◽  
Body Weight ◽  
Negative Control ◽  
The Body ◽  
Male Rats ◽  
Free Triiodothyronine ◽  
Cardiopulmonary Exercise ◽  
Chinese Herbal ◽  
Subcutaneous Blood Flow ◽  
Tsh Levels

Hypothyroidism frequently causes cardiopulmonary dysfunction, such as heart failure and respiratory and metabolic deficiencies. This study investigated the effects of Chinese herbal formula B307 on thyroidectomy-induced cardiopulmonary exercise dysfunction in rats. Twenty male rats were equally divided into four groups: negative control with sham treatment, positive control with oral B307 treatment only, thyroidectomy treatment only, and thyroidectomy with B307 posttreatment groups. The feeding dose of B307 was 50 mg/kg per day for 14 days. We examined and then compared the thyroid-stimulating hormone (TSH), free triiodothyronine (T3), free thyroxine (T4), and reactive oxygen species (ROS) from the blood of these four groups. Also, we compared the body weight, neck subcutaneous blood flow, cardiac ejection function, cardiopulmonary exercise function of oxygen consumption (VO2), carbon dioxide production (VCO2), and respiratory quotient (RQ = VCO2/VO2) among the four groups. Our results indicated that thyroidectomized rats had significantly decreased body weight, neck subcutaneous blood flow, cardiac ejection function, serum T3 and T4, and VO2 and VCO2, but had significantly increased ROS and TSH levels and RQ values compared with sham rats (P<0.01–0.05). In addition, thyroidectomized rats receiving oral B307 treatment had significantly increased body weight, neck subcutaneous blood flow, cardiac ejection function, and VO2, but significantly decreased ROS and TSH levels and VCO2 and RQ values compared with thyroidectomized rats (P<0.01–0.05). We suggest that the B307 could be a protective and beneficial alternative treatment for thyroidectomy-induced cardiopulmonary exercise dysfunction.

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