• Journal of Society of Preventive Korean Medicine
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• v.17 no.2
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• pp.169-178
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• 2013

Objectives : Many cancers acquired resistance to chemotherapy, thus limiting its anticancer efficacy. It is known that Glutathione (GSH) is related to the development of drug resistance. The expression of GSH synthesizing glutamylcysteine ligase (GCL) was controlled by nuclear factor-E2-related factor(Nrf2). Previous studies showed that pharmacological depletion of GSH results in ROS increase, apoptotic response, and sensitization to oxidizing stimuli. In the current study, we examined Saussurea Lappa (SL) have the inhibitory effect on Nrf2 activity using human lung cancer A549 cells overexpressing Nrf2. Methods : Cell viability of A549 cells on SL treatment was determined by MTT assay. To detect the apeptosis in SL-treated A549 cells, sub-G1 population was measured by flow cytometry analysis (FACS). The level ROS was determined by FACS and fluorescence microscopy. To investigate whether SL have effect the suppression on Nrf2, we performed western blotting analysis. The GSH content was measured since GSH plays an important role in response to oxidative stress and was regulated by Nrf2. Results : A549 cells treated with an SL extract showed a substantial decrease in cell viability, along with a concomitant increase in apoptosis compared to untreated cells. Treatment of the SL extract led to increased Reactive oxygen species (ROS) production and a suppression of Nrf2. In addition, the antioxidant NAC attenuated SL-induced ROS generation, Nrf2 inhibition, and apoptosis. Taken together, these data show that the SL extract induced the production of ROS, and the inhibition of Nrf2, consequently resulting in A549 cell death. Conclusions : These results suggest that SL might be an effective agent to enhance anticancer drug sensitivity via Nrf2 inhibition.

• Advances in Traditional Medicine
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• v.1 no.1
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• pp.97-106
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• 2000

The preventive effect of herbal formulation, ‘Dae-Bo-Won-Chun’(DBWC), on the progress of bone loss induced by ovariectomy (OVX) was studied in rats. From light microseopic analyses, a porous or erosive appearances were observed on the surface of trabecular bone of tibia in ovariectomized rats. Whereas those of the same bone in sham rats were composed of fine particles. The trabecular bone area and trabecular thickness in ovariectomized rats decreased by 50% from those in sham-operated rats, these decreases were completely inhibited by administration of DBWC at concentration of 10mg/kg per day for 7 weeks. The mechanical strength in femur neck was decreased by ovariectomy, and this was significantly suppressed by the administration of DBWC. Serum phosphorus, alkaline phosphatase, and thyroxine levels in ovariectomized rats were increased compared to those in sham-operated rats, and increases were completely inhibited by the administration of DBWC. These results strongly suggest that DBWC is effective in preventing the development of bone loss induced by ovariectomy in rats.

• Korean Journal of Medicinal Crop Science
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• v.26 no.5
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• pp.417-429
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• 2018

Background: The objective of this study was to make colloidal dispersions of the active compounds of radix of Angelica gigas Nakai that could be charaterized as nano-composites using hot melt extrusion (HME). Food grade hydrophilic polymer matrices were used to disperse these compound in aqueous media. Methods and Results: Extrudate solid formulations (ESFs) mediated by various HPMCs (hydroxypropyl methylcelluloses) and Na-Alg polymers made from ultrafine powder of the radix of Angelica gigas Nakai were developed through a physical crosslink method (HME) using an ionization agent (treatment with acetic acid) and different food grade polymers [HPMCs, such as HP55, CN40H, AN6 and sodium alignate (Na-Alg)]. X-ray powder diffraction (XRD) analysis confirmed the amorphization of crystal compounds in the HP55-mediated extrudate solid formulation (HP55-ESF). Differential scanning calorimetry (DSC) analysis indicated a lower enthalpy (${\Delta}H=10.62J/g$) of glass transition temperature (Tg) in the HP55-ESF than in the other formulations. Infrared fourier transform spectroscopy (FT-IR) revealed that new functional groups were produced in the HP55-ESF. The content of phenolic compounds, flavonoid (including decursin and decursinol angelate) content, and antioxidant activity increased by 5, 10, and 2 times in the HP55-ESF, respectively. The production of water soluble (61.5%) nano-sized (323 nm) particles was achieved in the HP55-ESF. Conclusions: Nano-composites were developed herein utilizing melt-extruded solid dispersion technology, including food grade polymer enhanced nano dispersion (< 500 nm) of active compounds from the radix of Angelica gigas Nakai with enhanced solubility and bioavailability. These nano-composites of the radix of Angelica gigas Nakai can be developed and marketed as products with high therapeutic performance.

• Journal of Pharmaceutical Investigation
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• v.39 no.4
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• pp.257-261
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• 2009

Effective therapeutics for renal failures have not yet been developed until now. Recently, there was a report showing that Wen-pi-tang-Hab-Wu-ling-san (WHW) prescriptions had the potential to prevent renal failures through the increased expression of HSP-27 and HSP-72 after ischemia/reperfusion. Therefore, formulation studies by pH-specific released systems were carried out to exhibit the optimal activity of WHW prescriptions in this study. WHW prescriptions were separately extracted using water into two parts of stomach-released (SR) and intestine-released (IR) extracts. Subsequently, the double-layered tablet was prepared using the SR extracts and pharmaceutical additives and enteric-coated IR tablet. Dissolution studies were carried out to figure out the release of cinnamic acid and icarrin from SR tablet, IR tablet and double-layered tablet, respectively. The complete release of cinnamic acid from SR tablet showed 90min after dissolution in pH 1.2 and insignificant drug released from IR tablet. As well as, icarrin from IR tablet completely released in pH 6.8 and 7.4 as enteric-coating film dissolved.

• Journal of Society of Preventive Korean Medicine
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• v.21 no.3
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• pp.87-98
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• 2017

Objectives : The objective of present study is to evaluate anti-arthritic effects of dried pomegranate concentrate powders (PCP), Eucommiae Cortex aqueous (EC) and ethanolic (ECe) extracts, Achyranthis Radix aqueous (AR) and ethanolic (ARe) extracts on the primary cultured rat articular chondrocytes. Methods : MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium Bromide) assay was performed cytotoxic effect of test substances. In addition, anti-inflammatory effects were also observed on the lipopolysaccaride (LPS) treated chondrocytes through prostaglandin $E_2\;(PGE_2)$ production and 5-lipoxygenase (LPO) activities, and inhibitory effects on metalloproteinase (MMP)-2 and MMP-9 activities were observed on the recombinant human interleukin $(rhIL)-1{\alpha}$ treated chondrocytes with their extracellular matrix (ECM) related mRNA expressions - collagen type II, SOX9 and aggrecan. Results : As results, ECe and ARe showed obvious cytotoxicity against primary cultured rat articular chondrocytes at a dose level of 10 mg/ml, respectively. However, no obvious cytotoxic effects of PCP, EC and AR were demonstrated at a dose level of 10 mg/ml, on the primary cultured rat articular chondrocytes. In addition, treatment of LPS $50{\mu}g/ml$ induced significant increases of $PGE_2$ contents and 5-LPO activities indicating inflammatory responses of the primary cultured rat articular chondrocytes, and also decreases of cell viabilities, increases of MMP-2 and MMP-9 activities with decreases of extracellular matrix (ECM) related collagen type II, SOX9 and aggrecan mRNA expressions were observed by treatment of $rhIL-1{\alpha}$ 50 ng/ml, suggesting damages on the primary cultured rat articular chondrocytes and related ECM degradations. However, these inflammatory responses and related ECM degradations were inhibited by pretreatment of all test substances, in order of PCP > ECe > ARe > EC > AR, and $rhIL-1{\alpha}$ induced chondrocytes deaths are inhibited by treatment in order of PCP > EC > AR > ECe > ARe. Conclusions : Taken together, it is expected that mixed formulation of PCP as main components with appropriate proportion of EC and AR as additional components will be achieved a potent alternative medicinal food for osteoarthritis.

• Journal of Pharmacopuncture
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• v.16 no.2
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• pp.15-22
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• 2013

Objective: Evaluations of the in-vitro anti-bacterial activities of aqueous extracts of Acacia catechu (L.F.)Willd, Castanea sativa, Ephedra sinica stapf and Shilajita mumiyo against gram-positive bacteria (Staphylococcus aureus, Streptococcus pneumonia) and gram-negative bacteria (Escherichia coli, klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa) are reasonable since these ethnomedicinal plants have been used in Persian folk medicine for treating skin diseases, venereal diseases, respiratory problems and nervous disorders for ages. Methods: The well diffusion method (KB testing) with a concentration of $250{\mu}g/disc$ was used for evaluating the minimal inhibitory concentrations (MIC). Maximum synergistic effects of different combinations of components were also observed. Results: A particular combination of Acacia catechu (L.F.) Willd, Castanea sativa, Ephedra sinica stapf and shilajita mumiyo extracts possesses an outstanding anti-bacterial activity. It's inhibiting effect on microorganisms is significant when compared to the control group (P<0.05). Staphylococcus aureus was the most sensitive microorganism. The highest anti-bacterial activity against gram-positive bacteria (Staphylococcus aureus, Streptococcus pneumonia) or gram-negative bacteria (Escherichia coli, Klebsiella pneumonia, Proteus mirabilis, and Pseudomonas aeruginosa) was exerted by formula number 2 (table 1). Conclusion: The results reveal the presence of anti-bacterial activities of Acacia catechu, Castanea sativa husk, Ephedra sp. and Mumiyo against gram-positive and gram-negative bacteria. Synergistic effects in a combined formula, especially in formula number 2 (ASLAN$^{(R)}$) can lead to potential sources of new antiseptic agents for treatment of acute or chronic skin ulcers. These results considering the significant anti-bacterial effect of the present formulation, support ethnopharmacological uses against diarrheal and venereal diseases and demonstrate use of these plants to treat infectious diseases.

• The Journal of Korean Obstetrics and Gynecology
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• v.25 no.2
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• pp.89-107
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• 2012

Objectives: This study was performed to develop therapeutic prescription that is more significant than existing ones through extraction method and formulation changes. Methods: Yukmijihwangtang(YMJHT) was extracted in 80% ethanol, and their relative anti-oxidant activities as well as anti-inflammatory effects through immune modulation were measured. Results: Both water and ethanol extracted YMJHT showed does-dependent DPPH elimination activities. ROS inhibition activity was greater in water extracted YMJHT except for Moutan Cortex. NO inhibition assay results indicated that all groups showed higher NO inhibition activities in RAW 264.7 cells in dose dependent manner. Water extracted group showed higher NO inhibition activity than that of ethanol extracted group. TNF-${\alpha}$ secretion inhibition assay using RAW 264.7 cells, water extracted YMJHT showed higher activity than ethanol extracts. Growth rate of spleen cells was greater in all tested groups, with higher rate in YMJHT-EtOH than YMJHT-DW. Suppression of gene expression of IFN-r in spleen cells stimulated by Con A was higher in YMJHT-EtOH than YMJHT-DW. Suppression of gene expression of IL-10 in spleen cells stimulated by Con A was highest in YMJHT-DW with 40%. Suppression of gene expression of IL-4 in spleen cells stimulated by Con A were significant with 90% or higher in all groups and that of IL-12p35 were also higher than 90% in all cases. Conclusions: From the results, it shows that YMJHT has anti-inflammatory effects through immune modulation. However, the difference between YMJHT-EtOH and YMJHT-DW was not that significant. Further studies are needed to find out effective extraction methods of herbal medicine.

• Proceedings of the Plant Resources Society of Korea Conference
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• 2018.04a
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• pp.72-72
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• 2018

The root of Angelica gigas Nakai (AGN) is used as a traditional herbal medicine in Korea for the treatment of many diseases. However, a major challenge associated with the usage of the active compounds from AGN is their poor water solubility. Therefore, this work aimed to enhance the solubility of active compounds by a chemical (viz. surfactant) and physical (hot melt extrusion) crosslinking method (CPC). Infrared Fourier transform spectroscopy (FT-IR) revealed multiple peaks in extrudate solids representing new functional groups including carboxylic acid, alkynes and benzene derivatives. Differential scanning calorimetry (DSC) analysis of the extrudate showed lower glass transition temperature (Tg) and lower enthalpy (${\Delta}H$) (Tg: $43^{\circ}C$; ${\Delta}H$: <6 (J/g)) compared to the non-extrudate (Tg $68.5^{\circ}C$; ${\Delta}H$: 123.2) formulations. X-ray powder diffraction (XRD) analysis revealed amorphization of crystal materials in extrudate solid. In addition, nanonization, enhanced solubility and higher extraction of phenolic compounds were achieved in the extrudate solid. Among the different extrudates, acetic acid- and Span 80-mediated formulations showed superior extractions. We conclude that the CPC method successfully enhanced the production of amorphous nano dispersions from extrudate solid formulations.

• Korean Journal of Pharmacognosy
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• v.39 no.4
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• pp.316-323
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• 2008

In this study, we have investigated the HPLC analysis methods and quantitative analysis of standard compounds for quality standardization of a medicinal crude drug GCSB-5, a herbal formulation consisting of 6 medicinal plants (Acanthopanacis Cortex, Achyranthis Radix, Ledebouriellae Radix, Cibotii Rhizoma, Glycine Semen, Eucommiae Cortex) which are used in traditional medicine to treat various bone disorders. HPLC analysis methods of acanthoside D(Acanthopanacis Cortex), 20-hydroxyecdysone(Achyranthis Radix) which were known standard compounds among 6 medicinal plants were developed on crude material and product. And validation of HPLC analysis methods were conformed for verification of HPLC methods by check to specificity, linearity, intra-day precision, inter-day precision and accuracy following ICH guideline. Content of acanthoside D and 20-hydroxyecdysone on raw material of GCSB-5 were decided at 0.577-0.578 mg/g and 0.311-0.312 mg/g. And we confirmed that content of acanthoside D and 20-hydroxyecdysone on GCSB-5 preparation were 0.302-0.303 mg/capsule and 0.113-0.115 mg/capsule.

• Natural Product Sciences
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• v.10 no.1
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• pp.16-19
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• 2004

Triphala churna is a widely used herbal formulation that contains equal proportion of dried fruit powder of Emblica officinalis, Terminalia chebula and Terminalia belirica. In the Indian system of medicine, it is used in cleaning wounds, urinary disorders, diabetes mellitus, leprosy, constipation, eyesight promotion, piles, and as a rejuvenator. In the present study, the methanolic extract of 5 commercial Triphala was evaluated for antioxidant activity by 1,1-diphenyl-2-picryl-hydrazyl free radical scavenging method, total phenolic content by Folin-Ciocalteu method and gallic acid equivalents (GAE) by high performance thin layer chromatographic (HPTLC) method. All extracts exhibited antioxidant activity significantly. The $IC_{50}$ of the extracts ranged between $7.16\;to\;12.96\;{\mu}g/ml$. The total phenolic content of the extracts was found to be 195.3-296.4 mg of GAE/gm of GAE/gm dw. The HPTLC chromatographic data reveal that the content of GAE present in the extract was found to be $7.17-4.11\;{\mu}g/ml$. The study reveals that out of the churnas analysed, C was found to exhibit the most potent antioxidant activity. A clear correlation between $IC_{50}$ and content of GAE nor the total phenolic content could be observed. The study reveals that the consumption of Triphala would exert several beneficial effects by virtue of its antioxidant activity.