Pharmacokinetics of letrozole and effects of its increasing doses on gonadotropins in ewes during the breeding season.

Letrozole is a non-steroidal, third-generation aromatase inhibitor used in humans. Although letrozole is not approved for use in animals, it is used off-label in cases of synchronization and infertility. The aim of this study was to determine the pharmacokinetics of letrozole after a single intravenous administration at three different doses in ewes during the breeding season and its effect on gonadotropins (luteinizing hormone (LH) and follicle-stimulating hormone (FSH)) at the beginning of proestrus. The study was carried out on 24 healthy Merino ewes. Ewes were randomly divided into four groups (n = 6) as control, 0.5, 1, and 2 mg/kg. Plasma concentrations of letrozole were measured using HPLC-UV and were analyzed by non-compartmental analysis. LH and FSH concentrations were measured with a commercial ELISA kit. The terminal elimination half-life (t1/2ʎz ) was significantly prolonged from 11.82 to 18.44 h in parallel with the dose increase. The dose-normalized area under the concentration-time curve (AUC) increased, and total body clearance (ClT ) decreased at the 1 and 2 mg/kg doses (0.05 L/h/kg) compared with the 0.5 mg/kg dose (0.08 L/h/kg). There were no differences in the volume of distribution at steady-state and initial (C0.083h ) plasma concentration values between dose groups. The decreased ClT , prolonged t1/2ʎz, and increased AUC at increasing doses showed the nonlinear kinetic behavior of letrozole. Letrozole significantly reduced LH concentration without affecting FSH concentration at all doses. As a result, letrozole has the potential to be used in synchronization methods and manipulation of the follicular waves due to its effect on LH secretion.

Tissue distribution and correlations of heavy metals in wild birds from Southern Turkey: an ecologically important region on the west Palearctic migration route.

Even if some are essential for biological functions, the accumulation of heavy metals above tolerable physiological limits is potentially toxic to also wild animals. The present study aimed to investigate concentrations of environmentally relevant heavy metals (As, Cd, Cu, Fe, Hg, Mn, Pb, and Zn) in feathers, muscle, heart, kidney, and liver tissues of wild birds (golden eagle [Aquila chrysaetos], sparrowhawk [Accipiter nisus], and white stork [Ciconia ciconia]) from Hatay province, southern Turkey. The metal concentrations of tissues were determined by a validated ICP-OES analysis method after microwave digestion. The concentration differences of metals in species/tissues and the correlations between essential/non-essential metals were determined by statistical analysis. According to the results, Fe (326.87±3.60 mg kg-1) had the highest, and Hg (0.09±0.00 mg kg-1) had the lowest mean concentration in all tissues. Compared to the literature; Cu, Hg, Pb, and Zn concentrations were lower; Cd, Fe, and Mn concentrations were higher. The correlations between As and all essentials; Cd and Cu, Fe; Hg and Cu, Fe, Zn; Pb and all essentials were significantly positive. In the conclusion, while essential Cu, Fe, and Zn are below the threshold value and do not pose a risk, Mn is close to the threshold value. Therefore, periodically monitoring the pollutant concentrations in bioindicators is a key necessity for the early determination of biomagnification trends and prevention of potential toxic stress on wildlife ecology.

Inula viscosa ameliorates acetic acid induced ulcerative colitis in rats.

Increased pro-inflammatory cytokines and oxidative stress contribute to the pathophysiology of ulcerative colitis (UC). Inula viscosa is a plant with antioxidant and anti-inflammatory properties. We investigated the effect of an ethanolic extract of I. viscosa on an experimental UC model created using acetic acid. Rats were divided into four groups of eight: group 1, control; group 2, 3% acetic acid group; group 3, 100 mg/kg sulfasalazine + 3% acetic acid group; group 4, 400 mg/kg I. viscosa + 3% acetic acid. I. viscosa and sulfasalazine were administered by oral gavage and 3% acetic acid was administered per rectum. We found that I. viscosa treatment decreased colon malondialdehyde, tumor necrosis factor-α, interleukin-1 beta and nuclear factor kappa B levels; it increased reduced glutathione, nuclear factor erythroid 2-related factor 2, heme oxygenase-1 and kelch-like ECH-associated protein 1 levels and glutathione peroxidase enzyme activity. Group 1 colon exhibited normal histological structure. Slight inflammatory cell infiltration and edema and insignificant slight erosion in crypts were detected in colon tissues of group 4. We found that I. viscosa reduced oxidative stress and inflammation, which was protective against UC by inducing the Nrf-2/Keap-1/HO-1 pathway in the colon.

Pharmacokinetics and bioavailability of danofloxacin in swan geese (Anser cygnoides) following intravenous, intramuscular, subcutaneous, and oral administrations.

The aim of this study was to determine the pharmacokinetics and bioavailability of danofloxacin in swan geese (Anser cygnoides) after intravenous (IV), intramuscular (IM), subcutaneous (SC), and oral (PO) administrations at 10 mg/kg dose. In this study, eight clinically healthy swan geese were used. The study was performed in four periods according to a crossover design with a 15 days washout period between two administrations. The plasma concentrations of danofloxacin were analyzed using high-performance liquid chromatograph-ultraviolet detection, and pharmacokinetic parameters were estimated by non-compartmental analysis. Following IV administration, terminal elimination half-life (t1/2ʎz ), total clearance, and volume of distribution at steady state were 6.03 h, 0.34 L/h/kg, and 2.71 L/h/kg, respectively. After IM, SC, and PO administration, t1/2ʎz was longer than that after IV administration. The Cmax of danofloxacin following IM, SC, and PO administrations was 3.65, 2.76, and 1.98 µg/mL at 0.63, 1, and 2 h, respectively. The bioavailability following IM, SC, and PO administrations was 87.99, 72.77, and 57.68%, respectively. This information may help in the use of danofloxacin in geese, yet the determination of optimal dosage regimen and pharmacodynamic studies are needed.

Health Risk Assessment of Essential and Toxic Metals in Canned/Pouched Food on Kitten and Adult Cats: an Animal Health Risk Assessment Adaptation Assay.

The main aim of this study was to determine the levels of Al, Cd, Cr, Cu, Fe, Hg, Mn, Ni, Pb, and Zn in commercial canned and pouched cat foods (salmon, tuna, liver, fish, and other aquatic products) and assess the potential health risks to kitten (≤ 1 years old) and adult cats (≥ 1 years old) associated with the recommended average consumption rate of labels. The study was also aimed to adapt the health risk assessment method to animal health and to support clinical prevention and diagnosis. The detected levels of the metals were below the data from other studies, except the mean Fe in all and Pb levels in salmon and kitten foods. Target hazard quotient (THQ) and total target hazard quotient (TTHQ) values did not exceed 1. That means the studied metals do not pose a health risk for adult cats and kittens. Dietary Hg and Cd should also be considered in the differential diagnosis of cases with clinical or postmortem findings, especially regarding neurological, kidney, and liver tissues. In conclusion, although canned/pouched consumption does not pose a health risk with regard to metals, further studies of health risk assessment for other pollutants by this first adaptation method will be necessary.

Pharmacokinetics of furosemide in goats following intravenous, intramuscular, and subcutaneous administrations.

Furosemide, a loop diuretic drug, is recommended for use in cases of edema, ascites, congestive heart failure, toxicosis, and acute renal failure in goats. However, its pharmacokinetics and bioavailability have not been reported yet in this species. The aim of this study was to determine the pharmacokinetics and bioavailability of furosemide in goats following intravenous (IV), intramuscular (IM), and subcutaneous (SC) administrations at a dose of 2.5 mg/kg. Six clinically healthy goats received furosemide by each route in a three-way crossover pharmacokinetic design with a 15-day washout period between administrations. The plasma concentrations of furosemide were determined using the high-performance liquid chromatography-UV method and analyzed by non-compartmental analysis. The elimination half-life following IV, IM, and SC administration was 0.71 (0.67-0.76) h, 0.69 (0.61-0.74) h, and 0.70 (0.67-0.79) h, respectively. The volume of distribution at steady state and total clearance for the IV route were 0.17 (0.16-0.19) L/kg and 0.30 (0.27-0.33) L/h/kg, respectively. The peak plasma concentrations of furosemide following IM and SC administrations were 11.19 (10.33-11.95) and 6.49 (5.92-7.00) µg/ml at 0.23 (0.16-0.25) and 0.39 (0.33-0.42) h, respectively. The bioavailability was 109.84 (104.92-116.99)% and 70.80 (55.77-86.67)% for the IM and SC routes, respectively. The pharmacokinetics of furosemide following the IV, IM, and SC administrations in goats demonstrated significant differences, which may have clinical and toxicological implications requiring further investigations.

Distribution and Ecotoxicological Risk Assessment of Heavy Metals in Streams of Amanos Mountains from Southern Turkey.

Assessing the potential ecological risks of chemical pollutants like heavy metals is a key tool of a sustainable environment. With this goal, ecotoxicological significant metal (Al, As, Cd, Cr, Cu, Fe, Hg, Ni, Pb, and Zn) levels of the water (n = 32) and sediment (n = 32) samples of streams [rural (8 points) and urban (8 points) sides] on Amanos Mountains were determined by inductively coupled plasma-optical emission spectrometry (ICP-OES) and ecotoxicological risk assessment was performed through the potential ecological risk index (RI). The study region with intense urban activities has also ecological importance with regards to wildlife. It is located on the migration route of birds, hosts loggerhead and green sea turtles, Mediterranean seals, and some terrestrial species like mountain gazelle and striped hyena. All calculated RI values were below the potential risk limits and the ecotoxicological risk was observed to be very low. Metal levels should be monitored periodically, and necessary measures should be taken before the reflection of the increase to be determined by the risk assessment on the ecosystem.

Pharmacokinetics of meloxicam, carprofen, and tolfenamic acid after intramuscular and oral administration in Japanese quails (Coturnix coturnix japonica).

The aim of this study was to determine the pharmacokinetics of meloxicam (MLX), carprofen (CRP), and tolfenamic acid (TA) in Japanese quails (Coturnix coturnix japonica) following intramuscular (IM) and oral administration at doses of 1, 10, and 2 mg/kg, respectively. A total of 72 quails were randomly divided into 3 equal groups as MLX, CRP, and TA. Each group was separated into two sub-groups that received IM and oral administration of each drug. Plasma concentrations of MLX, CRP, and TA were determined using HPLC-UV and analyzed by non-compartmental method. The t1/2ʎz and MRT of MLX, CRP, and TA after oral administration were similar to those after IM administration. The Vdarea /F of MLX, CRP, and TA after IM administration was 0.28, 2.05, and 0.20 L/kg. The Cl/F of MLX, CRP, and TA after IM administration was 0.12, 0.19, and 0.09 L/h/kg. MLX, CRP, and TA after oral administration showed significantly lower Cmax and longer Tmax compared with IM administration. The relative bioavailability of MLX, CRP, and TA following oral administration in quails was 76.13%, 61.46%, and 57.32%, respectively. The IM and oral route of MLX, CRP, and TA can be used for the treatment of various conditions in quails. However, further research is necessary to determine the pharmacodynamics and safety of MLX, CRP, and TA before use in quails.

Pharmacokinetics of tolfenamic acid after different administration routes in geese (Anser cygnoides).

The pharmacokinetics and bioavailability of tolfenamic acid were determined in geese (Anser cygnoides) following intravenous (IV), intramuscular (IM), subcutaneous (SC), and oral administrations at 2 mg/kg dose. In this study, eight healthy geese (3.5 ± 0.5 kg) were used. The study was performed in four periods according to a crossover design with a 15-day washout period between two administrations. The plasma concentrations of tolfenamic acid were analyzed using HPLC-UV, and pharmacokinetic parameters were calculated by noncompartmental analysis. The elimination half-life was 1.73, 2.51, 2.34, and 2.31 hr for IV, IM, SC, and oral routes, respectively. The volume of distribution at steady state and total clearance after IV administration were 0.25 L/kg and 0.16 L hr-1  kg-1 , respectively. The peak plasma concentrations of tolfenamic acid after IM, SC, and oral administrations were 4.89, 2.94, and 2.92 µg/ml at 0.25, 0.75, and 1 hr, respectively. The bioavailability was 87.91, 77.87, and 76.03% for the IM, SC, and oral routes, respectively. Tolfenamic acid, which exhibits the good bioavailability and plasma concentration following IM, SC, and oral administrations at 2 mg/kg dose, may be useful in the treatment of inflammatory disease conditions in geese.

Pharmacokinetics of tolfenamic acid in goats after different administration routes.

The aim of this study was to determine the pharmacokinetics and bioavailability of tolfenamic acid in goats after intravenous (IV), intramuscular (IM), subcutaneous (SC), and oral (PO) administrations at 2 mg/kg dose. In this study, eight clinically healthy goats were used. The study comprised four periods, according to a crossover design with at least a 15-day washout period between treatments. Plasma concentrations of tolfenamic acid were determined by HPLC-UV, and the pharmacokinetic parameters were estimated using a non-compartmental method. Following IV administration, terminal elimination half-life, volume of distribution at steady state, and total clearance were 1.60 h, 0.37 L/kg, and 0.27 L/h/kg, respectively. The mean peak plasma concentration following IM, SC, and PO administrations was 1.77, 1.22, and 0.30 µg/ml, respectively. The mean bioavailability following IM, SC, and PO administrations was 64.46, 55.43, and 19.46%, respectively. The PO route, which exhibits both the low plasma concentration and bioavailability, is not recommended in goats. The IV, IM, and SC routes, which show comparable pharmacokinetic profiles, may be proposed for use in goats. However, the multi-dose and pharmacodynamic studies are necessary to establish more accurately its safety and efficacy in the goat.

Levels of Metals and Organochlorine Pesticides in Kidney, Liver, and Muscle Tissues of Wild Boars (Sus scrofa) from Hatay Province, Eastern Mediterranean Region, Turkey.

Increases in the levels of environmental contaminants are reflected in wild animals, which are early indicators of pollution. Hatay is an ecologically important region with a high intensity of industrial and agricultural activities. This study aimed to investigate the contamination levels of metals and organochlorine pesticides associated with environmental pollution in tissues of wild boars from Turkey. The highest mean levels (mg kg-1) of metals were 0.05 for As, 0.51 for Cd, 6.30 for Cu, 0.07 for Hg, 0.54 for Ni, and 0.57 for Pb in kidney tissues and 0.22 for Cr, 353.38 for Fe, 2.86 for Mn, and 46.76 for Zn in liver tissues. The Cd and Pb levels exceeded the maximum residue limits (MRLs) in some tissues. Among the studied pesticides, only p,p'-DDE contamination was quantified, and the mean levels were 3.6, 0.1, and 0.5 µg kg-1 in liver, kidney, and muscle tissues respectively. In conclusion, Hatay Province requires monitoring in terms of environmentally important contaminants, mainly Cd, Pb, and DDT isomers.

Pharmacokinetics, bioavailability and tissue residues of doxycycline in Japanese quails (Coturnix coturnix japonica) after oral administration.

This study aimed to determine the bioavailability, tissue residue and withdrawal time of doxycycline after oral administration in Japanese quails (Coturnix coturnix japonica). Japanese quails received doxycycline at 20 mg/kg dose following either single intravenous or oral administration, or 5-day oral administration. Doxycycline concentrations in plasma, liver, kidney, muscle, and skin + fat were determined using high-performance liquid chromatography-ultraviolet. The Withdrawal Time v1.4 software was used to calculate withdrawal times. Following single oral administration, terminal elimination half-life, area under the concentration-time curve from 0 to infinitive time, peak plasma concentration (Cmax) and time to reach Cmax were 10.98 h, 215.84 (h*µg)/mL, 15.33 µg/mL, and 2 h, respectively. The oral bioavailability was 25.84% in quails. In this study, the mean doxycycline concentration was below the maximum residue limit (MRL) at day 4 in skin + fat (0.120 µg/g), and at day 5 in kidney (0.41 µg/g), liver (0.26 µg/g), and muscle (<0.05 µg/g lowest limit of quantification). The highest concentrations of doxycycline after 5-day oral administration were found in kidney compared with other tissues and plasma. These results indicate that the withdrawal times required for doxycycline to reach concentrations

Effect of ketoprofen co-administration on pharmacokinetics of cefquinome following repeated administration in goats.

The pharmacokinetics of cefquinome (2 mg/kg every 24 hr for 5 days) was determined following intramuscular administration alone and co-administration with ketoprofen (3 mg/kg every 24 hr for 5 days) in goats. Six goats were used for the study. In the study, the crossover pharmacokinetics design with 20-day washout period was performed in two periods. Plasma concentrations of cefquinome were assayed using high-performance liquid chromatography by ultraviolet detection. The mean terminal elimination half-life (t1/2ʎz ), area under the concentration-time curve (AUC0-24 ), peak concentration (Cmax ), apparent volume of distribution (Vdarea /F), and total body clearance (CL/F) of cefquinome after the administration alone were 4.85 hr, 11.06 hr*µg/ml, 2.37 µg/mL, 1.23 L/kg, and 0.17 L/h/kg after the first dose, and 5.88 hr, 17.01 hr*µg/mL, 3.04 µg/mL, 0.95 L/kg, and 0.11 L/h/kg after the last dose. Ketoprofen significantly prolonged t1/2ʎz of cefquinome, increased AUC0-24 and Cmax , and decreased Vdarea /F and CL/F. Cefquinome exhibited low accumulation after the administration alone and in combination with ketoprofen. These results indicated that ketoprofen prolonged the elimination of cefquinome in goats. The 24-hr dosing intervals at 2 mg/kg dose of cefquinome, which co-administered with ketoprofen, may maintain T> minimum inhibitory concentration (MIC) values above 40% in the treatment of infections caused by susceptible pathogens with the MIC value of ≤0.75 µg/ml in goats with an inflammatory condition.

Effect of dose on the intravenous pharmacokinetics of tolfenamic acid in goats.

The objective of this study was to determine the pharmacokinetics of tolfenamic acid (TA) following intravenous (IV) administration at doses of 2 and 4 mg/kg in goats. In this study, six healthy goats were used. TA was administered intravenously to each goat at 2 and 4 mg/kg doses in a cross-over pharmacokinetic design with a 15-day washout period. Plasma concentrations of TA were analyzed using the high performance liquid chromatography with ultraviolet detector, and pharmacokinetic parameters were assigned by noncompartmental analysis. Following IV administration at dose of 2 mg/kg, area under the concentration-time curve (AUC0-∞ ), elimination half-life (t1/2ʎz ), total clearance (ClT ) and volume of distribution at steady state (Vdss ) were 6.64 ± 0.81 hr* µg/ml, 1.57 ± 0.14 hr, 0.30 ± 0.04 L h-1  kg-1 and 0.40 ± 0.05 L/kg, respectively. After the administration of TA at a dose of 4 mg/kg showed prolonged t1/2ʎz , increased dose-normalized AUC0-∞ , and decreased ClT . In goats, TA at 4 mg/kg dose can be administered wider dose intervals compared to the 2 mg/kg dose. However, further studies are needed to determine the effect of different doses on the clinical efficacy of TA in goats.

Effects of Single and Repeated Doses on Disposition and Kinetics of Doxycycline Hyclate in Goats.

The aims of this study in goats were to determine the pharmacokinetics of doxycycline hyclate following single intravenous (IV), intramuscular (IM) and oral administrations of 20 mg/kg and to evaluate the pharmacokinetics and accumulation of doxycycline hyclate after repeated oral administrations at a 20 mg/kg dose every 24 h for 5 days. Six healthy male goats were used for the study. The study was performed in four periods according to a longitudinal study with a 15-day washout period. Plasma concentrations of doxycycline were determined using HPLC-UV and analyzed by a non-compartmental method. IM injection of doxycycline caused swelling and pain due to irritation in the injection site. After IM and oral administrations, terminal elimination half-life (t1/2λz) and mean residence time (MRT) were prolonged and areas under the curve (AUCs) were low. The mean bioavailability of IM and oral administration was 51.51% and 31.39%, respectively. Following repeated oral administration, the accumulation ratio of doxycycline was 1.76. Pharmacokinetic properties including weak accumulation, wide distribution volume and long elimination half-life can make doxycycline hyclate valuable for repeated use via an oral route in the treatment of some infectious diseases in goats. However, the determination of pharmacodynamic effects on susceptible pathogens isolated from goats is also necessary to confirm the drug dosage regimen.

Effect of castration procedure on the pharmacokinetics of meloxicam in goat kids.

The aim of this study was to determine the changes in the pharmacokinetics of meloxicam in goat kids who were castrated following the administration of xylazine. Six goat kids were used for the study. The study was performed in two periods according to a longitudinal study, with a 15-day washout period between periods. In the first period (Control group), 1 mg/kg meloxicam was administered by i.v. route to kids. In the second period (Castration group), the kids were sedated with 0.3 mg/kg xylazine and castration was performed following meloxicam administration. Plasma meloxicam concentration was analyzed using HPLC-UV, and pharmacokinetic parameters were calculated by noncompartmental model. In the control group following the administration of meloxicam, mean elimination half-life (t1/2 ʎz ), area under the concentration-time curve (AUC0-∞ ), total body clearance (ClT ), and volume of distribution at steady-state (Vdss ) were 13.50 ± 0.62 hr, 41.10 ± 2.86 hr µg/ml, 24.43 ± 1.75 ml hr-1  kg-1 , and 0.45 ± 0.03 L/kg, respectively. In the castration group, the t1/2 ʎz of meloxicam prolonged, AUC0-∞ increased, and ClT and Vdss decreased. In conclusion, the excretion of meloxicam from the body slowed and the t1/2 ʎz was prolonged in the castrated goat kids following xylazine administration. However, there is a need to determine the pharmacodynamics of meloxicam in castrated goat kids.

Tyrosol prevents AlCl3 induced male reproductive damage by suppressing apoptosis and activating the Nrf-2/HO-1 pathway.

Aluminium is a ubiquitous element that occurs naturally in the soil making human exposure to it is unavoidable. Tyrosol is present in olive oil and is known to have antioxidant effects. Therefore, the present study explores the toxic effects of aluminium chloride (AlCl3 ) and evaluates the possible protection by tyrosol in male rats. Testicular injury was induced by the administration of AlCl3 (34 mg kg-1  day-1 ). Rats were treated with either tyrosol (20 mg kg-1 day-1 ) or AlCl3 (34 mg kg-1 day-1 ). The experiment lasted for 10 weeks. Biochemical, histopathological and protein expression profiles were determined to decipher the role of tyrosol in protecting the cellular damage. Further, histomorphometric analyses of testes showed deranged architecture along with other noted abnormalities. AlCl3 group rats' testes showed decreased GSH levels, CAT activities, Nrf-2, HO-1, bcl-2 expressions and sperm motility whereas increased caspase-3 expressions, MDA levels, abnormal and dead/live sperm ratio. However, tyrosol treatment attenuated these changes. The present results demonstrate the beneficial role of tyrosol treatment in AlCl3 induced testicular toxicity alterations of rat.

Correction to: Protective Effects of Tyrosol Against DSS-Induced Ulcerative Colitis in Rats.

The Funding Information is missing in the original article.

Protective Effects of Tyrosol Against DSS-Induced Ulcerative Colitis in Rats.

In this study, the effects of tyrosol were investigated in DSS-induced experimental ulcerative colitis model. For this purpose, rats were divided into five groups of seven rats in each: control group, colitis group (DSS-4%), tyrosol group (tyrosol 20 mg/kg), sulfasalazine (sulfasalazine+DSS 100 mg/kg), and treatment group (tyrosol+DSS 20 mg/kg). In the study, the active substances were administered to all animals for a period of 21 days. At the end of the study, malondialdehyde (MDA) levels increased (p < 0.001); GSH level (p < 0.05) along with GSH.Px (p < 0.01) and CAT (p < 0.001) activities decreased in the DSS-induced colitis group. However, with the administration of tyrosol, MDA and GSH levels along with GSH.Px and CAT activities came to the same levels as the control group. In the colitis group, an increase occurred in IL-6, COX-2, and NF-κB parameters, which created a significant difference compared to the control group (p < 0.001). Similarly, TNF-α levels also significantly increased with the administration of DSS (p < 0.05) which created a significant difference compared to the control group, while there was no difference among the other groups. As for the Nrf-2 data, it decreased with the administration of DSS which created a significant difference compared to the control group (p < 0.05), while there was no difference in other groups. In the colitis-induced group, IL-6, COX-2, and NF-κB gene expression levels also similarly increased but returned to the normal levels with the administration of tyrosol. In the histopathological scoring, the negativity that increased with the administration of DSS returned to the normal levels with the administration of tyrosol+DSS. In conclusion, according to the data obtained, tyrosol fixed the destruction picture in the DSS-induced colitis model, giving rise to thought that it has a protective effect.

Protective effects of conventional and colon-targeted lycopene and linalool on ulcerative colitis induced by acetic acid in rats.

OBJECTIVE: To compare the potential protective effects of conventional and colon-targeted lycopene (TLC) and linalool (TLN) on acetic acid (AA)-induced ulcerative colitis (UC) in rats. METHODS: Conventional and colon-targeted LC (10 mg/kg) and LN (200 mg/kg) were administered in vivo orally for 7 days and sulfasalazine (100 mg/kg) was also used as reference drug. Then, 4% AA was administered intrarectally to induce UC. Subsequently, the colon tissues were taken as samples for biochemical and histopathological analysis. RESULTS: Malondialdehyde (MDA), interleukin 1ß (IL-1ß), IL-6, cyclooxygenase-2 (COX-2) and nuclear factor kappa B (NF-κB) levels were decreased (p < 0.05) in the targeted groups compared to the AA group, whereas nuclear factor-erythroid 2-related factor 2 (Nrf-2) level was increased (p < 0.05). Tumor necrosis factor α (TNF-α) level was also decreased (p < 0.05) and catalase activity (CAT) was increased (p < 0.05) in the TLC group compared to the AA group. IL-1ß and IL-6 levels were lower in the TLC group compared to the conventional LC and sulfasalazine groups (p < 0.05). COX-2 and NF-κB levels were lower, while the Nrf-2 level was higher in the targeted groups compared to the conventional groups (p < 0.05). Furthermore, COX-2 level was lower and Nrf-2 level was higher in the targeted groups compared to the sulfasalazine group (p < 0.05). CONCLUSION: As expected, sulfasalazine was effective on all parameters analyzed, but the colon-targeted pretreatments were more effective from sulfasalazine on some parameters. Therefore, colon-targeted plant-derived therapies might be alternative approaches to provide protection against UC, which deserves to be investigated further.