Leticia Aparecida Silva Batista;Alexandre Henrique dos Reis-Prado;Hebertt Gonzaga dos Santos Chaves;Lara Cancella de Arantes;Luis Fernando Santos Alves Morgan;Carolina Bosso Andre;Thais Yumi Suzuki;Francine Benetti
Restorative Dentistry and Endodontics
/
v.48
no.4
/
pp.39.1-39.23
/
2023
Objectives: This study aimed to investigate the effectiveness of different topical/systemic agents in reducing the damage caused by bleaching gel to pulp tissue or cells. Materials and Methods: Electronic searches were performed in July 2023. In vivo and in vitro studies evaluating the effects of different topical or systemic agents on pulp inflammation or cytotoxicity after exposure to bleaching agents were included. The risk of bias was assessed. Results: Out of 1,112 articles, 27 were included. Nine animal studies evaluated remineralizing/anti-inflammatories agents in rat molars subjected to bleaching with 35%-38% hydrogen peroxide (HP). Five of these studies demonstrated a significant reduction in inflammation caused by HP when combined with bioglass or MI Paste Plus (GC America), or following KF-desensitizing or Otosporin treatment (n = 3). However, orally administered drugs did not reduce pulp inflammation (n = 4). Cytotoxicity (n = 17) was primarily assessed using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay on human dental pulp cells and mouse dental papilla Cell-23 cells. Certain substances, including sodium ascorbate, butein, manganese chloride, and peroxidase, were found to reduce cytotoxicity, particularly when applied prior to bleaching. The risk of bias was high in animal studies and low in laboratory studies. Conclusions: Few in vivo studies have evaluated agents to reduce the damage caused by bleaching gel to pulp tissue. Within the limitations of these studies, it was found that topical agents were effective in reducing pulp inflammation in animals and cytotoxicity. Further analyses with human pulp are required to substantiate these findings.
Seventeen compounds derived from traditional Chinese medicines (TCMs) were tested for their antiviral activity against porcine reproductive and respiratory syndrome virus (PRRSV) in vitro. Visualization with the cytopathologic effect (CPE) assay and the 3-(4, 5-dimethyithiazol-2-yl)-2,5-diphenyltetrazolium bromide test were used to determine the 50% cytotoxic concentration ($CC_{50}$) and 50% effective concentration ($EC_{50}$) in cultured Marc-145 cells. Among the tested compounds, chlorogenic acid and scutellarin showed potential anti-PRRSV activity. The $EC_{50}$ values were $270.8{\pm}14.6{\mu}g/ml$ and $28.21{\pm}26.0{\mu}g/ml$ and the selectivity indexes were >5.54 and 35.5, respectively. The time-of-addition and virucidal assay indicated that the anti-PRRSV activity of the two compounds could be due to their inhibiting the early stage of virus replication and/or inactivating the virus directly. The inhibition of the virus attachment was not observed in the adsorption inhibition assay. The inhibition ratios of chlorogenic acid and scutellarin were, respectively, 90.8% and 61.1% at the maximum non-cytotoxic concentrations. The results have provided a basis for further exploration of their antiviral properties and mechanisms in vivo. We believe that the chlorogenic acid and scutellarin have a great potential to be developed as new anti-PRRSV drugs for clinical application.
Kim, Se-Mi;Yoon, Hwa;Yoo, Hee-Doo;Kim, Kyung-Ran;Kang, Hyun-Ah;Cho, Hea-Young;Lee, Yong-Bok
Journal of Pharmaceutical Investigation
/
v.38
no.3
/
pp.199-205
/
2008
Famciclovir, 9-(4-hydroxy-3-hydroxymethylbut-1-yl) guanine, is an oral prodrug of the antiherpesvirus nucleoside analogue, penciclovir. In human, famciclovir is orally well absorbed and then undergoes extensive first pass metabolism to penciclovir and essentially no parent compound is recovered from plasma or urine. The purpose of the present study was to evaluate the bioequivalence of two famciclovir tablets, Famvir tablet 750 mg (Novartis Korea Ltd.) and Famcivir tablet 750 mg (Hanmi Pharmaceutical. Co., Ltd.), according to the guidelines of the Korea Food and Drug Administration (KFDA). The release of famciclovir from the two famciclovir formulations in vitro was tested using KP VIII Apparatus II method with water. Twenty six healthy male subjects, $23.38{\pm}1.72$ years in age and $68.59{\pm}7.84\;kg$ in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After a single tablet containing 750 mg as famciclovir was orally administered, blood samples were taken at predetermined time intervals and the concentrations of penciclovir in serum were determined using HPLC with UV detector. The dissolution profiles of two formulations ere similar at water. The pharmacokinetic parameters such as $AUC_t$, $C_{max}$ and $T_{max}$ were calculated and ANOVA test was utilized for the statistical analysis of the parameters using logarithmically transformed $AUC_t$, $C_{max}$ and untransformed $T_{max}$. The results showed that the differences between two formulations based on the reference drug, $Famvir^{(R)}$ tablet 750 mg, were -0.53%, 1.12% and -24.82% for $AUC_t$, $C_{max}$ and $T_{max}$, respectively. There were no sequence effects between two formulations in these parameters. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log 0.8 to log 1.25 (e.g., $log\;0.9569{\sim}log\;1.0423$ and $log\;0.8763{\sim}log\;1.2136$ for $AUC_t$ and $C_{max}$, respectively). Thus, the criteria of the KFDA bioequivalence guideline were satisfied, indicating Famcivir tablet 750 mg was bioequivalent to Famvir tablet 750 mg.
Objective : Dopamine transporter concentrations have been known to decrease in Parkinson's disease(PD). The aim of the present study was to evaluate the correlation between SPECT measurements of [I-123]N-(3-iodopropene-2-yl)-$2{\beta}$-carbomethoxy-$3{\beta}$-(4-chlorophenyl) tropane(IPT) as an imaging agent for measuring changes in transporter concentrations with PD. Patients and Methods : IPT labelled with $4.87{\pm}1.29mCi$($180.19{\pm}47.73MBq$) of [I-123] was intravenously injected into 23 patients(age : $58{\pm}12$) with PD and three normal controls(NC)(age : $37{\pm}7$) as bolus. Brain SPECT were then performed at 1 hour and 2 hours after injection on a double headed camera. The statistical parameters were the contrast ratio of left basal ganglia(BG) and right basal ganglia to occipital cortex(OCC) per milli curies of injected radiotracer at 1 hour and 2 hours. The correlations were evaluated between these parameters and Hoehn-Yahr classification of the patients. Results : The(BG - OCC)/OCC/mCi ratios at 1 hour and 2 hours for PD and NC were $0.14{\pm}0.07$ and $0.27{\pm}0.07$(1 hour) and $0.12{\pm}0.07$ and $0.34{\pm}0.04$(2 hour), respectively. The(BG - OCC)/OCC/mCi ratios of Parkinson's disease were decreased with higher grade of Hoehn-Yahr classification of the patients. The ratio between BG and OCC for PD were clearly separated from NC and may be useful outcome measures for clinical diagnosis. Conclusion : The findings suggest that IPT may be a very useful tracer for early diagnosis and treatment of PD and study of dopamine re-uptake site.
Kim, Hee-Joung;Im, Joo-Hyuck;Yang, Seoung-Oh;Ryu, Jin-Sook;Choi, Yun-Young;Lee, Myung-Chong;Lee, Hee-Kyung
The Korean Journal of Nuclear Medicine
/
v.30
no.1
/
pp.35-46
/
1996
Dopamine transporter concentrations have been known to decrease in Parkinson's disease (PD) or increase in Tourette's disorder. The purpose of this study was to evaluate the effectiveness of [I-123]N-(3-iodopropene-2-yl)-$2{\beta}$-carbomethoxy-$3{\beta}$-(4-chlorophenyl) tropane (IPT) as an imaging agent for measuring changes in transporter concentrations with PD. IPT labelled with 6.69+/-0.64 mCi(247.53+/-23.68 MBq) of I-123 was intravenously injected into ten patients(age: 55+/-11) with PD, and six normal controls(NC)(age: 46+/-14) as a bolus. Dynamic SPECT scans of the brain were then performed for 5 minutes each over 120 minutes on a triple headed camera. Time activity curves were generated for the left basal ganglia(LBG), right basal ganglia(RBC), and occipital cortex(OCC). The statistical parameters included the time to peak activity, the contrast ratio of LBG and RBG to OCC at several time points, and the accumulated specific binding counts/mCi/pixel(ASBC) from 0 to 115 minutes. The uptake of IPT in the brains of PD and NC peaked within 10 minutes of injection in all subjects. The maximum target to background ratio in the basal ganglia of PD and NC occurred at 85+/-20 min and 110+/-6 min of injection, respectively. The BG/OCC ratios at 115 minutes for PD and NC were 2.15+/-0.54 and 4.26+/-0.73, respectively. The ASBC at 115 minutes for PD and NC were 152.91+/-50.09 and 289.51+/-49.00, respectively. The ratio of BG/OCC for the NC was significantly higher than the ratio for PD. SPECT data matched with clinical diagnosis for PDs. The ratio between BG and OCC and the ASBC for PD were clearly separated from NC and may be useful outcome measures for clinical diagnosis. The findings suggest that IPT may be a very useful tracer for early diagnosis of PD and study of dopamine reuptake site.
Kim, Se-Mi;Cho, Hea-Young;Kang, Hyun-Ah;Lee, Yong-Bok
Korean Journal of Clinical Pharmacy
/
v.18
no.1
/
pp.38-44
/
2008
Rebamipide, ($\pm$)-2-(4-chlorobenzoylamino)-3-[2(1H)-quinolinon-4-yl] propionic acid, is used for mucosal protection, healing of gastroduodenal ulcers, and treatment of gastritis. It works by enhancing mucosal defense, scavenging free radicals and temporarily activating genes encoding cyclooxygenase-2. The purpose of the present study was to evaluate the bioequivalence of two rebamipide tablets, $Mucosta^{(R)}$ (Korea Otsuca Pharmaceuticals Co., Ltd.) and Mustar (Korean Drug Co., Ltd.), according to the guidelines of the Korea Food and Drug Administration (KFDA). The release of rebamipide from the two rebamipide formulations in vitro was tested using KP VIII Apparatus II method with pH 6.8 dissolution medium. Twenty six healthy male subjects, $23.46{\pm}2.63$ years in age and $66.62{\pm}8.97\;kg$ in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After a single tablet containing 100 mg as rebamipide was orally administered, blood samples were taken at predetermined time intervals and the concentrations of rebamipide in serum were determined using HPLC with fluorescence detector. The dissolution profiles of two formulations were similar in the tested dissolution medium. The pharmacokinetic parameters such as $AUC_t$, $C_{max}$ and $T_{max}$ were calculated, and ANOVA test was utilized for the statistical analysis of the parameters using logarithmically transformed $AUC_t$, $C_{max}$ and untransformed $T_{max}$. The results showed that the differences between two formulations based on the reference drug, $Mucosta^{(R)}$ were -5.08, 3.52 and -9.71 % for $AUC_t$, $C_{max}$ and $T_{max}$, respectively. There were no sequence effects between two formulations in these parameters. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log 0.8 to log 1.25 (e.g., log 0.84$\sim$log 1.07 and log 0.90$\sim$log 1.17 for $AUC_t$ and $C_{max}$, respectively). Thus, the criteria of the KFDA bioequivalence guideline were satisfied, indicating Mustar tablet was bioequivalent to $Mucosta^{(R)}$ tablet.
Proximate composition, total phenolics and total flavonoids level, DPPH radical scavenging activity, and cytotoxicity were determined in the methanol extracts of different plant parts of Youngia sonchifolia at reproductive growth stage. Crude protein and crude fat were present as the highest amount in flowers, and crude fiber in the stems and roots. The highest content of phenolics [mg ferulic acid equivalents (FAE) $kg^{-1}$ dry weight (DW)] was found in flowers (highest) and followed by leaves, stems and roots (lowest). Flavonoids [mg rutin equivalents $kg^{-1}$ DW] level, however, showed the highest in leaf extracts and lowest in root extracts. The antioxidant potential of the methanol extracts from the plants dose-dependently increased DPPH (1,1-diphenyl-2-picrylhydrazyl) free radical scavenging activity (%). DPPH radical scavenging activity were highest in root extracts ($IC_{50}=1,135.6\;mg\;kg^{-1}$) and followed by leaf, stem and flower extracts. By way of MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) assay, methanol extracts of roots showed the highest anticancer activity on human cancer cell line Calu-6 for human pulmonary carcinoma ($IC_{50}=196.3\;mg\;kg^{-1}$) and HCT-116 for human colon carcinoma ($IC_{50}=623.6\;mg\;kg^{-1}$).
The purpose of this study was to investigate the antioxidant and anti-inflammatory activities of hot water (AMPW) and 70% ethanol (AMPE) extracts of apple mango (Mangifera indica L.) peel. The antioxidant activities were measured using a total polyphenol, electron-donating, 2,2'-azinobis [3-ethylbenzothiazoline6-sulfonic acid] (ABTS) radical scavenging assay. The total polyphenol content of AMPW and AMPE was 66.08 ± 0.62 mg TAE/100 g and 100.13 ± 0.23 mg TAE/100 g, respectively. As a result of measuring the electrondonating ability, at a concentration of 1,000 ㎍/ml, AMPW and AMPE showed an effectiveness of 86% and 94%, respectively. The ABTS assay showed 80% and 98% respective radical scavenging activity for AMPW and AMPE, at a concentration of 1,000 ㎍/ml. The cell viability on macrophage cells was performed using a 3-[4,5-dimethyl-thiazol-2-yl]-2,5-diphenyl-tetrazoliumbromide (MTT) assay, and the results showed more than 90% cell viability at a 100 ㎍/ml concentration. Anti-inflammatory activity was verified by confirming nitric oxide (NO) production inhibitory activity, inducible nitric oxide synthase (iNOS), and cyclooxygenase-2 (COX-2) protein and mRNA expression inhibitory activity from lipopolysaccharide (LPS)-treated RAW 264.7 cells. The NO production inhibitory effects were measured using the Griess assay, which confirmed 45% and 40% inhibition after treatment with AMPW and AMPE, respectively. Moreover, the protein and mRNA expression of inflammatory-related factors iNOS and COX-2, decreased in a concentrationdependent manner. In conclusion, this study showed antioxidant and anti-inflammatory effects of Mangifera indica L. peel and revealed its promising potential for application as an antioxidant and anti-inflammatory agent.
Zaltoprofen, (2-(10,11-dihydro-10-oxodibenzo[b,f]thiepin-2-yl)propionic acid) is an NSAID with powerful anti-inflammatory effects as well as an analgesic action on inflammatory pain. The purpose of the present study was to evaluate the bioequivalence of two zaltoprofen tablets, $Soleton^{\circledR}$ (CJ Corp.) and SCD Zaltoprofen (Samchundang Pharmaceutical Co., Ltd.), according to the guidelines of the Korea Food and Drug Administration (KFDA). The release of zaltoprofen from the two zatoprofen formulations in vitro was tested using KP Vlll Apparatus ll method with various dissolution media. Twenty six healthy male subjects, $23.2{\pm}2.26$ years in age and$64.7{\pm}8.08$ kg in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After a single tablet containing 80 mg as zaltoprofen was orally administered, blood samples were taken at predetermined time intervals and the concentrations of zaltoprofen in serum were determined using HPLC with UV detector. The dissolution profiles of two formulations were similar in all tested dissolution media. The pharmacokinetic parameters such as $AUC_t$, $C_{max}$ and $T_{max}$ were calculated, and ANOVA test was utilized for the statistical analysis of the parameters using logarithmically transformed $AUC_t$, $C_{max}$ and untransformed $T_{max}$. The results showed that the differences between two formulations based on the reference drug, $Soleton^{\circledR}$ were 6.33, 5.91 and 17.7% for $AUC_t$, $C_{max}$ and untransformed $T_{max}$, respectively. There were no sequence effects between two formulations in these parameters. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log 0.8 to log 1.25 (e.g.,log $1.01{\sim}1og\;1.11$ and log $0.928{\sim}1og\;1.18$ for $AUC_t$ and $C_{max}$, respectively). Thus, the criteria of the KFDA bioequivalence guideline were satisfied, indicating SCD Zaltoprofen tablet was bioequivalent to $Soleton^{\circledR}$ tablet.
Panax ginseng has been used as a traditional medicine for several centuries in Korea. A laboratory experiment using methanol extracts of freeze-dried leaves and roots in the different ages of P. ginseng was conducted to determine the content of phenolics and flavonoids, antioxidant activity and cytotoxicity. The results indicate that the total phenolics level [mg ferulic acid equivalents (FAE) $kg^{-1}$ DW] was higher in leaves (22.0 to 76.3 mg $kg^{-1}$) than roots (19.0 to 28.3 mg $kg^{-1}$) of P. ginseng. The total content of phenolics in roots increased with increase in age of P. ginseng from one to six years. However, the content of phenolics in P. ginseng leaf decreased with the increase in age. Total flavonoid [mg naringin equivalents $kg^{-1}$ DW] was more detected in the leaves (30.3 to 138.6 mg $kg^{-1}$) than in the roots (0.0 to 10.6 mg $kg^{-1}$) of P. ginseng. The total flavonoid level in leaves decreased with increase in age of P. ginseng. The antioxidant potential of the methanol extracts from the plants dose-dependently increased. DPPH free radical scavenging activity was higher in leaves (36.9 to 82.8%) than in roots (14.8 to 39.4%), and in young plants than in old ones. According to 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, the methanol extracts from 5 year-root part showed the highest cytotoxicity against Calu-6, followed by 2 year- and 3 year-roots. However, the methanol extracts from 6 year- and 4 year-roots had lower cytotoxicity. Total phenolics content in both leaves and roots was highly correlated with the DPPH radical scavenging ($r^2=0.7366$ to 0.7870) and nitrite scavenging ($r^2=0.5604$ to 0.8794) activities, suggesting that they contribute to the antioxidant properties of the P. ginseng plants.
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