• Journal of Ginseng Research
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• 제42권4호
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• pp.512-523
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• 2018

Background: 20(S)-Protopanaxadiol (20S-PPD) is a fully deglycosylated ginsenoside metabolite and has potent dermal antiaging activity. However, because of its low aqueous solubility and large molecular size, a suitable formulation strategy is required to improve its solubility and skin permeability, thereby enhancing its skin deposition. Thus, we optimized microemulsion (ME)-based hydrogel (MEH) formulations for the topical delivery of 20S-PPD. Methods: MEs and MEHs were formulated and evaluated for their particle size distribution, morphology, drug loading capacity, and stability. Then, the deposition profiles of the selected 20S-PPD-loaded MEH formulation were studied using a hairless mouse skin model and Strat-M membrane as an artificial skin model. Results: A Carbopol-based MEH system of 20S-PPD was successfully prepared with a mean droplet size of 110 nm and narrow size distribution. The formulation was stable for 56 d, and its viscosity was high enough for its topical application. It significantly enhanced the in vitro and in vivo skin deposition of 20S-PPD with no influence on its systemic absorption in hairless mice. Notably, it was found that the Strat-M membrane provided skin deposition data well correlated to those obtained from the in vitro and in vivo mouse skin studies on 20S-PPD (correlation coefficient $r^2=0.929-0.947$). Conclusion: The MEH formulation developed in this study could serve as an effective topical delivery system for poorly soluble ginsenosides and their deglycosylated metabolites, including 20S-PPD.

• 한국독성학회:학술대회논문집
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• 한국독성학회 2002년도 Current Trends in Toxicological Sciences
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• pp.106-106
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• 2002

Several epidemiological studies suggested that arsenic exposure was strongly correlated with the development of cardiovascular disease such as hypertension. In order to examine whether arsenic affects vasomotor tone in blood vessels, we investigated the effect of arsenic on agonist-induced vasorelaxation using the isolated rat aortic rings in in vitro organ bath system.(omitted)

• 대한한방내과학회지
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• 제39권1호
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• pp.44-68
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• 2018

Objective: This study aimed to investigate the trend in the research on breast cancer using traditional Korean medicine (TKM) and establish the direction for further study. Methods: Breast cancer studies using Korean medicine were searched using the Oriental Medicine Advanced Searching Integrated System (OASIS). The search term was 'breast' and there was no restriction in year. The searched studies were analyzed according to the type of research. Results: 1. 83 studies were searched. The types and numbers of study were as follows: 42 were in vitro studies, 5 were in vivo studies, 12 were studies for review, and 27 were clinical research including case reports. 2. Various cell lines such as MCF-7, MDA-MB-231, SKBR3, and MCF-10A were used for in vitro studies. The studies reported a decrease in cell viability, induction of apoptosis, and change of expression in cancer-related genes. In vivo studies also reported induction of apoptosis, and anti-proliferative activity of herbal medicine against the cancer cells. 3. Among the clinical research, 8 were cross-sectional studies, 3 were controlled-trial, and 15 were case reports. The baseline characteristics of breast cancer patients were analyzed in the cross-sectional studies. Interventions such as pharmacopuncture, herbal medicine, massage, Qi gong, acupuncture, electroacupuncture and moxibustion were used in clinical research. 4. Research on the review of breast cancer covered various subjects as follows: herbal medicine, acupuncture, pattern identification of breast cancer in traditional Korean medicine, analysis of previous experimental studies, and clinical trials. Conclusion: We have found the applicability of TKM for treatment of breast cancer through this review. It is necessary to conduct further studies, such as well-designed clinical trials based on the results from experimental research.

• Journal of Pharmaceutical Investigation
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• 제17권3호
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• pp.127-133
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• 1987

Dissolution characteristics and urinary excreted amount of commercially available three brands of sulfisoxazole tablets were investigated in order to elucidate the in vitro-in vivo correlations and relative bioavailability in humans. All the tablets tested met the K.P. IV and the USP XXI specifications for tablet weight variation, content uniformity, disintegration and dissolution. The disintegration and dissolution rate constants of sulfisoxazole tablets in pH 2.0 HCl-KCl buffer were reduced more significantly (p<0.05) than those in diluted HCl $(1{\rightarrow}12.5)$ and pH 6.5 phosphate buffer. It seemed to be attributed to the pH dependent solubility of sulfisoxazole. We could see that the relative bioavailability of brand B to sulfisoxazole powder was about 90% and that its value was higher than those of other two brands from the urinary excretion data obtained from eight healthy male volunteers by means of Latin square cross over design. No useful correlation was observed between the in vitro and in vivo studies in this experiment.

• 약학회지
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• 제47권5호
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• pp.331-338
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• 2003

A butyrolactone ester of cefazolin (CFZ-BTL) was synthesized by the esterification of cefazolin (CFZ) with $\alpha$-bromo-${\gamma}$-butyrolactone. The synthesis was confirmed by the spectroscopic analysis. The CFZ-BTL was more lipophilic than the CFZ when assessed by n-octanol/water partition coefficients at various pH. The CFZ-BTL itself did not show any antimicrobial activity in vitro, but after oral administration of CFZ-BTL to rabbits, exerted significant anti-microbial activity in serum samples when measured by the inhibion zone method in nutrient agar plates, due to conversion of CFZ-BTL to an active metabolite, probably CFZ, in the body. The CFZ-BTL was also converted into CFZ as confirmed by in vitro incubation study, with tissue homogenates (liver, blood and intestine) of rabbits. The liver showed the fastest conversion rate, probably via the hydrolysis mechanism. In vivo metabolism of CFZ-BTL to CFZ was also confirmed in vivo serum samples by HPLC. The oral bioavailability of CFZ-BTL in rabbits was 1.6-fold increased when compared to CFZ, resulting from followed by enhanced lipophilicity increased passive absorption in the intestine.

• 한국수정란이식학회지
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• 제12권1호
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• pp.37-48
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• 1997

I. The Factors Influencing In Vivo Embryo Production by Condition of Superovulation Treatment These studies were carried out to establish an effective and practical system for comrnercialization of embryo production techniques by analyzing several factors influencing in vivo embryo production on superovulation treatment in Korean native cattle. In vivo embryos were flushed 226 times from 128 donors.The results obtained from the studies on the factors influencing in vivo embryo production by superovulation treatment were as follows : FSH-P had a significiant advantage(83.0%) over SUPER-OV in the percentage of fertilized embryos(P<0.01). No difference was found loetween FSH-P and SUPER-OV in the percentage of transferable and freezable embryos.2. The response of superovulation by SUPER-OV was greater than that of FSH-P The donors having 8~9 and more than 10 of corpora lutea(CL) derived by FSH-P were 40.0%(most frequent) and 33%, respectively. The donors having more than 12 and 10 CL derived by SUPER -OV were 33.3% (most frequent) and 56.6%, respectively.3. Embryo production after treatment of repeated superovulation was remarkablely decreased at 3rd time by FSH-P but did not differ among 1, 2 and 3rd times by SUPER-OV. Embryo production on intervals of repeated superovulation was significantly different for the number and percentage of fertilized, transferable and free-zable' embryos in FSH-P (P<0.01) and rernarkablely decreased in repeated superovulation of 81~120 interval days. The SUPER-OV showed no differences in interval days of repeated superovulation and was found better than FSH-P in the response of repeated superovulation. (Key words : in Vivo embryo, superovulation, FSH -P, SUPER-OV)

• Journal of Ginseng Research
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• 제41권4호
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• pp.477-486
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• 2017

Background: Our previous studies have demonstrated that ginsenoside-Rg1 can promote angiogenesis in vitro and in vivo through activation of the glucocorticoid receptor (GR). Furthermore, microRNA (miRNA) expression profiling has shown that Rg1 can modulate the expression of a subset of miRNAs to induce angiogenesis. Moreover, Rb1 was shown to be antiangiogenic through activation of a different pathway. These studies highlight the important functions of miRNAs on ginseng-regulated physiological processes. The aim of this study was to determine the angiogenic properties of Korean Red Ginseng extract (KGE). Methods and Results: Combining in vitro and in vivo data, KGE at $500{\mu}g/mL$ was found to induce angiogenesis. According to the miRNA sequencing, 484 differentially expressed miRNAs were found to be affected by KGE. Among them, angiogenic-related miRNAs; miR-15b, -23a, -214, and -377 were suppressed by KGE. Meanwhile, their corresponding angiogenic proteins were stimulated, including vascular endothelial growth factor, vascular endothelial growth factor receptor-2, endothelial nitric oxide synthase, and MET transmembrane tyrosine kinase. The miRNAs-regulated signaling pathways of KGE were then found by Cignal 45-Pathway Reporter Array, proving that KGE could activate GR. Conclusion: KGE was found capable of inducing angiogenesis both in vivo and in vitro models through activating GR. This study provides a valuable insight into the angiogenic mechanisms depicted by KGE in relation to specific miRNAs.

• 약학회지
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• 제42권6호
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• pp.572-575
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• 1998

Chitosan has been known to have hypocholesterolemic and hypolipidemic effects in animal studies. Chitosan also absorbs bile acids in vitro and in vivo, which might result in the hypocholesterolemic action. Trialkyl chitosan derivatives were prepared and tested for bile acid absorption activity in vitro. The derivatives showed enhanced absorption capacities which were comparable to cholestyramine.

• Asian Pacific Journal of Cancer Prevention
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• 제13권7호
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• pp.3065-3071
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• 2012

Aim: The present investigation was to evaluate the effects of essential oils of Wedelia chinensis (Osbeck) on free radicals and in vivo antioxidant properties. Methods: Essential oils were extracted using hydro-distillation and compound analysis was performed by GC-MS analysis. Screening for inhibitory activity was conducted by DPPH and OH-scavenging assays. In addition an in vivo study was carried out in cell line implanted cancer bearing mice with assessment of levels of catalase, superoxide dismutase, glutathione peroxidase, lipid peroxidation, nitric oxide and reduced glutathione. Finally, lungs were dissected out for histopathology study of metastasis. Results: GC-MS analysis revealed the presence of carvocrol and trans-caryophyllene as the major compounds with 96% comparison with the Wilily and NBS libraries. The essential oil exhibited significant inhibition in DPPH free radical formation. Whereas reducing power and hydroxyl radical scavenging activity are dose dependent. When compared with the standard, it was found that the essential oil has more or less equal activity in scavenging free radicals produced. In the animal studies, the level of antioxidant enzymes catalase, superoxide dismutase and glutathione peroxidase, as well as glutathione, were found to be increased in treated groups whereas lipid peroxidation and nitric oxide were reduced. Histopathology report also shows that the essential oil has a significant combating effect against cancer development. Conclusion: In all the in vitro assays, a significant correlation existed between the concentrations of the essential oil and percentage inhibition of free radicals. The in vivo studies also has shown a very good antioxidant property for the essential oil during cancer development. From, these results the essential oil can be recommended for treating disease related to free radicals and to prevent cancer development.

• 대한핵의학회지
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• 제38권2호
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• pp.198-204
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• 2004

Tumor cell proliferation is considered to be a useful prognostic indicator of tumor aggressiveness and tumor response to therapy but in vitro measurement of individual proliferation is complex and tedious work. PET imaging provides a noninvasive approach to measure tumor growth rate in situ. Early approaches have used $^{18}F$-FDG or methionine to monitor proliferation status. These 2 tracers detect changes in glucose and amino acid metabolism, respectively, and therefore provide only an indirect measure of proliferation status. More recent studies have focused on DNA synthesis itself as a marker of cell proliferation. Cell lines and tissues with a high proliferation rate require high rates of DNA synthesis. $[^{11}C]Thymidine$ was the first radiotracer for noninvasive imaging of tumor proliferation. The short half-life of $^{11}C$ and rapid metabolism of $[^{11}C]Thymidine$ in vivo make the radiotracer less suitable for routing use. Halogenated thymidine analogs such as 5-iodo-2-deoxyuridine (IUdR) can be successfully used as cell proliferation markers for in vitro studies because these compounds are rapidly incorporated into newly synthesized DNA. IUdR has been evaluated as a potential in vivo tracer in nuclear medicing but the image qualify and the calculation of proliferation rates are impaired by its rapid in vivo degradation. Hence, the thymidine analog $3'-deoxy-3'-^{18}F-fluorothymidine$ (FLT) was recently introduced as a stable proliferation marker with a suitable nuclide half-life and stable in vivo. $[^{18}F]FLT$ is phosphorylated to 3-fluorothymidine monophosphate by thymidine kinase 1 and reflects thymidine kinase 1 activity in proliferating cell. $[^{18}F]FLT$ PET is feasible in clincal use and well correlates with cellular proliferation. Choline is a precursor for the biosynthesis of phospholipids (in particular, phosphatidylcholine), which is the essential component of all eukaryotic cell membranes and $[^{11}C]choline$, which is a new marker for cellular proliferation.