• Herbal Formula Science
• /
• v.25 no.2
• /
• pp.271-302
• /
• 2017

Objectives : Jakyakgamcho-tang has been used to treat muscular tension, spasm and pain. On this study, new clinical uses of Jakyakgamcho-tang were confirmed and the other pharmacological results were summarized by analysing trends of modern experimental studies and clinical studies. Methods : Papers related to Jakyakgamcho-tang were searched on PUBMED, RISS, and National Assembly Library, and classified by categories and effects of clinical application and a variety of experiment around abstract. Also, figures were used for sketching out a timeline of expressing when these papers were read and core research content was described as a digest for identifying research trends. Results : Until today, there are 104 researches about the antispasmodic, analgesic, anti-inflammatory effects of Jakyakgamcho-tang. In total, 91 papers were analyzed in this study. In matter of subject, researches on the antispasmodic effects were 17 cases, researches on the analgesic effects were 14 cases, researches on gynecological therapeutics were 14 cases, researches on pharmacokinetics were 12 cases, researches on the constituent identification were 7 cases, studies about constituents efficacy were 6 cases, studies about interactions with drugs were 6 cases. Conclusion : The traditional use of Jakyakgamcho-tang on muscle tension, spasm and pain has proven to have effects through the experimental evidences. Other effects of Jakyakgamcho-tang such as gynecological therapeutics, anti-inflammatory effects, are now emerging as a new area in clinical use. Futhermore as an auxiliary treatment, Jakyakgamcho-tang is a good alternative for muscle cramps during maintenance of hemodialysis, myalgia or arthralgia induced by anticancer drugs, amenorrhea induced by neuroleptics.

• Journal of Microbiology and Biotechnology
• /
• v.27 no.3
• /
• pp.616-623
• /
• 2017

Ginsenoside Rg3, a saponin extracted from ginseng, has various pharmacological and biological activities; however, its effects against Brucella infection are still unclear. Herein, the inhibitory effects of ginsenoside Rg3 against intracellular parasitic Brucella infection were evaluated through bacterial infection, adherence assays, and LAMP-1 colocalization, as well as immunoblotting and FACS for detecting MAPK signaling proteins and F-actin polymerization, respectively. The internalization, intracellular growth, and adherence of Brucella abortus in Rg3-treated RAW 264.7 cells were significantly decreased compared with the Rg3-untreated control. Furthermore, an apparent reduction of F-actin content and intensity of F-actin fluorescence in Rg3-treated cells was observed compared with B. abortus-infected cells without treatment by flow cytometry analysis and confocal microscopy, respectively. In addition, treating cells with Rg3 decreased the phosphorylation of MAPK signaling proteins such as ERK 1/2 and p38 compared with untreated cells. Moreover, the colocalization of B. abortus-containing phagosomes with LAMP-1 was markedly increased in Rg3-treated cells. These findings suggest that ginsenoside Rg3 inhibits B. abortus infection in mammalian cells and can be used as an alternative approach in the treatment of brucellosis.

• Microbiology and Biotechnology Letters
• /
• v.48 no.3
• /
• pp.383-388
• /
• 2020

Elephant garlic (Allium ampeloprasum L.) has been reported to have several pharmacological effects. However, its anti-adipogenic effect and the possible molecular mechanisms have not yet been reported. In this study, we demonstrate that elephant garlic extracts suppress adipogenesis in 3T3-L1 adipocytes. Raw and steamed elephant garlic extracts (REG and SEG, respectively) suppressed the differentiation of adipocytes and cellular lipid accumulation. Of note, the anti-differentiation effect of REG treatment on 3T3-L1 cells resulted in cytotoxicity, whereas SEG-treated cells displayed no such cytotoxicity. Additionally, SEG treatment significantly reduced the adipogenesis-related gene expression of PPAR γ, C/EBPα, adiponectin, Ap2, and LPL. To our knowledge, these results are the first evidence of the anti-adipogenic effects of elephant garlic extracts on 3T3-L1 adipocytes.

• The Korean Journal of Physiology and Pharmacology
• /
• v.19 no.6
• /
• pp.549-555
• /
• 2015

We attempted to investigate molecular mechanisms underlying phenotypic change of vascular smooth muscle cells (VSMCs) by determining signaling molecules involved in chemokine production. Treatment of human aortic smooth muscle cells (HAoSMCs) with thrombin resulted not only in elevated transcription of the (C-C motif) ligand 11 (CCL11) gene but also in enhanced secretion of CCL11 protein. Co-treatment of HAoSMCs with GF109230X, an inhibitor of protein kinase C, or GW5074, an inhibitor of Raf-1 kinase, caused inhibition of ERK1/2 phosphorylation and significantly attenuated expression of CCL11 at transcriptional and protein levels induced by thrombin. Both Akt phosphorylation and CCL11 expression induced by thrombin were attenuated in the presence of pertussis toxin (PTX), an inhibitor of Gi protein-coupled receptor, or LY294002, a PI3K inhibitor. In addition, thrombin-induced production of CCL11 was significantly attenuated by pharmacological inhibition of Akt or MEK which phosphorylates ERK1/2. These results indicate that thrombin is likely to promote expression of CCL11 via PKC/Raf-1/ERK1/2 and PTX-sensitive protease-activated receptors /PI3K/Akt pathways in HAoSMCs. We propose that multiple signaling pathways are involved in change of VSMCs to a secretory phenotype.

• Asian Pacific Journal of Cancer Prevention
• /
• v.16 no.18
• /
• pp.8191-8196
• /
• 2016

Inhibition of EGFR-EGF interactions forms an important therapeutic rationale in treatment of non-small cell lung carcinoma. Established inhibitors have been successful in reducing proliferative processes observed in NSCLC, however patients suffer serious side effects. Considering the narrow therapeutic window of present EGFR inhibitors, the present study centred on identifying high efficacy EGFR inhibitors through structure based virtual screening strategies. Established inhibitors - Afatinib, Dacomitinib, Erlotinib, Lapatinib, Rociletinib formed parent compounds to retrieve similar compounds by linear fingerprint based tanimoto search with a threshold of 90%. The compounds (parents and respective similars) were docked at the EGF binding cleft of EGFR. Patch dock supervised protein-protein interactions were established between EGF and ligand (query and similar) bound and free states of EGFR. Compounds ADS103317, AKOS024836912, AGN-PC-0MXVWT, GNF-Pf-3539, SCHEMBL15205939 were retrieved respectively similar to Afatinib, Dacomitinib, Erlotinib, Lapatinib, Rociletinib. Compound-AGN-PC-0MXVWT akin to Erlotinib showed highest affinity against EGFR amongst all the compounds (parent and similar) assessed in the study. Further, AGN-PC-0MXVWT brought about significant blocking of EGFR-EGF interactions in addition showed appreciable ADMET properties and pharmacophoric features. In the study, we report AGN-PC-0MXVWT to be an efficient and high efficacy inhibitor of EGFR-EGF interactions identified through computational approaches.

• Advances in Traditional Medicine
• /
• v.8 no.4
• /
• pp.339-348
• /
• 2008

Butea frondosa has been used traditionally as a topical formulation in the treatment of many diseases and disorders. Two compounds [BF-1 (crystalline flavonol quercetin) and BF-2 (tannin) from ethyl acetate fraction of ethanolic extract] were isolated from the bark of Butea frondosa. The stereostructures of the compounds were determined on the basis of chemical and physicochemical evidence. BF-1 and BF-2 were screened in vitro for possible antibacterial property against 112 bacteria comprising 3 genera of Gram-positive and 12 genera of Gram-negative types. It was found that both BF-1 and BF-2 exhibited inhibitory activity against several bacteria. Most of these strains were inhibited by BF-1 at $50-200\;{\mu}g/ml$, while BF-2 ($MIC_{50}$ $400\;{\mu}g/ml$) was much less active. The bacteria could be arranged in the decreasing order of sensitivity towards BF-1 in the following manner: S. aureus, Bacillus spp., Salmonella spp., Vibrio spp., Shigella spp., E. coli and Pseudomonas spp. The $MIC_{50}$ of the compound was $50\;{\mu}g/ml$ while the $MIC_{90}$ was $100\;{\mu}g/ml$. The decreasing order of sensitivity towards BF-2 was V. cholerae, Bacillus spp., S. aureus, V. parahaemolyticus, Salmonella spp. and Proteus spp. BF-1 was bactericidal in action. In vivo studies with this extract showed that it could offer statistically significant protection (p < 0.01) to mice challenged with a virulent bacterium. The inhibitory activity of Butea frondosa against Gram-positive and Gram-negative bacteria indicates its usefulness in the treatment of common bacterial infections. The potentiality of BF-1 as an antibacterial agent may be confirmed further by pharmacological studies.

• Korean Journal of Clinical Pharmacy
• /
• v.26 no.4
• /
• pp.312-317
• /
• 2016

Objective: Midazolam is mainly metabolized by cytochrome P450 (CYP) 3A. Inhibition or induction of CYP3A can affect the pharmacological activity of midazolam. The aims of this study were to develop a population pharmacokinetic (PK) model and evaluate the effect of CYP3A-mediated interactions among ketoconazole, rifampicin, and midazolam. Methods: Three-treatment, three-period, crossover study was conducted in 24 healthy male subjects. Each subject received 1 mg midazolam (control), 1 mg midazolam after pretreatment with 400 mg ketoconazole once daily for 4 days (CYP3A inhibition phase), and 2.5 mg midazolam after pretreatment with 600 mg rifampicin once daily for 10 days (CYP3A induction phase). The population PK analysis was performed using a nonlinear mixed effect model ($NONMEM^{(R)}$ 7.2) based on plasma midazolam concentrations. The PK model was developed, and the first-order conditional estimation with interaction was applied for the model run. A three-compartment model with first-order elimination described the PK. The influence of ketoconazole and rifampicin, CYP3A5 genotype, and demographic characteristics on PK parameters was examined. Goodness-of-fit (GOF) diagnostics and visual predictive checks, as well as bootstrap were used to evaluate the adequacy of the model fit and predictions. Results: Twenty-four subjects contributed to 900 midazolam concentrations. The final parameter estimates (% relative standard error, RSE) were as follows; clearance (CL), 31.8 L/h (6.0%); inter-compartmental clearance (Q) 2, 36.4 L/h (9.7%); Q3, 7.37 L/h (12.0%), volume of distribution (V) 1, 70.7 L (3.6%), V2, 32.9 L (8.8%); and V3, 44.4 L (6.7%). The midazolam CL decreased and increased to 32.5 and 199.9% in the inhibition and induction phases, respectively, compared to that in control phase. Conclusion: A PK model for midazolam co-treatment with ketoconazole and rifampicin was developed using data of healthy volunteers, and the subject's CYP3A status influenced the midazolam PK parameters. Therefore, a population PK model with enzyme-mediated drug interactions may be useful for quantitatively predicting PK alterations.

• The Journal of Internal Korean Medicine
• /
• v.25 no.3
• /
• pp.482-491
• /
• 2004

Alzheimer's disease(AD) is a geriatric dementia that is widespread in old age. In the near future AD may be the biggest problem in public health service. Although a variety of oriental therapies in the study of Jimitang have been traditionally utilized for the treatment of AD, their pharmacological effects and active mechanisms have not been fully elucidated. This study in an investigation of effects of Jimitang on apoptotic cell death induced by CT105 overexpression in SK-N-SH neuroblastoma cell lines. DNA fragmentation, neurite outgrowth assay and LDH activity assay were examined. The regeneratory and inhibitory effects on Alzheimer's disease in pCT105-induced neuroblastoma cell lines by Jimitang water extract were examined. Findings from these experiments have shown that Jimitang inhibits the synthesis or activities of CT105, which has neurotoxicities and apoptotic activities in cell lines. In addition, pretreatment of $Jimitang(>50\;{\mu}g/mL\;for\;12\;hours)$ partially prevented CT(105)-induced cytotoxicity in SK-N-SH cell lines, and were inhibited by pretreatment. $Jimitang(>50\;{\mu}g/mL\;for\;12\;hours)$ repaired CT(105)-induced neurite outgrowth when SK-N-SH cell lines were transfected with CT(105). Results of this study show that. in the Jimitang group, the apoptosis in the nervous system in inhibited, the repair against the degerneration of neuroblastoma cells by CT105 expression is promoted. In addition, Jimitang was found to inhibit DNA fragmentation induced by CT105 overexpression, and promote neurite outgrowth. These findings suggest that Jimitang is beneficial for the treatment of AD.

• Asian Pacific Journal of Cancer Prevention
• /
• v.15 no.17
• /
• pp.7291-7296
• /
• 2014

Different plant parts of Flacourtia indica have long been used in Ayurvedic medicine. Previous studies have demonstrated that the methanolic extract of F. indica possess anti-inflammatory properties. The present study was aimed at investigating the anticancer effects of methanol extract of Flacourtia indica (FIM) aerial parts in human colon cancer (HCT116) cells. Treatment of cells with FIM at a concentration of $500{\mu}g/ml$ for 24 hours significantly reduced cell viability and induced apoptosis, which was associated with the increased cytoplasmic expression of cytochrome c, activation of caspase-3, and the cleavage of poly-(ADP-ribose) polymerase. Incubation with FIM also inhibited the levels of Bcl-2, Bcl-xl and survivin, which are the markers of cell proliferation, whereas the expression of Bax remained unchanged. Treatment with FIM led to the generation of reactive oxygen species (ROS) in a concentration-dependent manner. Pharmacological inhibition of ROS generation by pretreatment of cells with N-acetyl cysteine abrogated FIM-induced apoptosis in HCT116 cells. Thus, these results demonstrate that FIM has anti-proliferative and pro-apoptotic effects in HCT116 cells and the effects are, at least in part, due to the ROS dependent activation of caspases.

• Advances in Traditional Medicine
• /
• v.1 no.1
• /
• pp.55-63
• /
• 2000

Soeumin Sibjeundaibo-tang (SJDBT) and Soyangin Sibimijihwang-tang (SMJHT) have been used traditionally to improve the systemic blood circulation and biological energy production in the patients with circulatory and neuronal diseases. The object of this study is to determine the protective effects of SJDBT and SMJHT extracts on the spontaneous and glutamate-induced neuronal damages in cultured cells derived from mice cerebral cortex. At 14 days after beginning the cultures, the activity of lactate dehydrogenase released into the culture media was significantly decreased by treatment of cerebroneuronal cells with SJDBT and SMJHT (0.1 mg/ml) for 7 days. By comparison with the normal cells, cerebroneuronal morphology was dramatically changed by treatment of glutamate (1 mM) for 12 hrs, and this was conspicuously recovered by pretreatment of cerebroneural cells with SJDBT and SMJHT (0.1-1.0 mg/ml) for 2 days. Moreover, glutamated-induced DNA fragmentation was also protected by pretreatment of cerebroneuronal cells with those extracts. These results suggest that naturally occurring and glutamate-induced degeneration of cultured cerebrocortical cells may be related, in part, to the process of apoptotic cell death. The pharmacological properties of SJDBT and SMJHT extracts to improve cerebroneuronal degeneration may be considered as one of useful medicines that can prevent cerebrocortical impairments resulted from age-dependent and excitotoxicity-induced neuronal degeneration in human brain.