• Journal of Pharmacopuncture
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• v.25 no.4
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• pp.344-353
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• 2022

Objectives: Auraptene is the most abundant natural prenyloxycoumarin. Recent studies have shown that it has multiple biological and therapeutic properties, including antioxidant properties. Erythrocytes are constantly subjected to oxidative damage that can affect proteins and lipids within the erythrocyte membrane and lead to some hemoglobinopathies. Due to the lack of sufficient information about the antioxidant effects of auraptene on erythrocytes, this study intended to evaluate the potential of this compound in protecting radical-induced erythrocytes damages. Methods: The antioxidant activity of auraptene was measured based on DPPH and FRAP assays. Notably, oxidative hemolysis of human erythrocytes was used as a model to study the ability of auraptene to protect biological membranes from free radical-induced damage. Also, the effects of auraptene in different concentrations (25-400 µM) on AAPH-induced lipid/protein peroxidation, glutathione (GSH) content and morphological changes of erythrocytes were determined. Results: Oxidative hemolysis and lipid/protein peroxidation of erythrocytes were significantly suppressed by auraptene in a time and concentration-dependent manner. Auraptene prevented the depletion of the cytosolic antioxidant GSH in erythrocytes. Furthermore, it inhibited lipid and protein peroxidation in a time and concentration-dependent manner. Likewise, FESEM results demonstrated that auraptene reduced AAPH-induced morphological changes in erythrocytes. Conclusion: Auraptene efficiently protects human erythrocytes against free radicals. Therefore, it can be a potent candidate for treating oxidative stress-related diseases.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.6 no.2
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• pp.171-176
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• 2020

Covalent organic frameworks (COFs) are porous crystalline polymers in which organic units are linked by covalent bonds and have a regular arrangement at the atomic level. Recently, the COFs have been much attention in bio-medical area such as bio-imaging, drug delivery, and therapeutics. These 2D nanoparticles are proving their value in nanomedicine due to their large surface area, functionalization through functional groups exposed on the surface, chemical stability due to covalent bonding, and high biocompatibility. The high ω-electron density and crystallinity of COFs makes it a promising candidate for bioimaging probes, and its porosity and large surface area make it possible to be utilized as a drug delivery vehicle. However, the low dispersibility in water, the cytotoxicity problems of COFs are still challenged to be solved in the future. In this regard, several efforts that increase the degree of dispersion through functionalization on the surface of COFs for the application to the biomedical field have been reported. In this review, we would like to describe the advantages and limitations of COFs for bio-imaging and anti-cancer treatment.

• Proceedings of the Plant Resources Society of Korea Conference
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• 2022.09a
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• pp.20-20
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• 2022

Herein, we demonstrate that butein (1) can prevent swelling in a murine lymphedema model by suppressing tumor necrosis factor α (TNF-α) production. Butein derivatives were synthesized and evaluated to identify compounds with in vitro anti-inflammatory activity. Among them, 20 µM of compounds 7j, 7m, and 14a showed 50% suppression of TNF-α production in mouse peritoneal macrophages after lipopolysaccharide stimulation. Compound 14a, exhibited the strongest potency with an in vitro IC₅₀ of 14.6 µM and suppressed limb volume by 70% in a murine lymphedema model. The prodrug strategy enabled a six-fold increase in kinetic solubility of compound 1 and five-fold higher levels of active metabolite in the blood for compound 14a via oral administration in the pharmacokinetics study. We suggest that the compound 14a could be developed as a potential therapeutic agent targeting anti-inflammatory activity to alleviate lymphedema progression.

• Proceedings of the Plant Resources Society of Korea Conference
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• 2020.08a
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• pp.89-89
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• 2020

In this study, we evaluated the effect of the extracts from Lonicera caerulea leaves (LCLE), branches (LCBE) and fruits (LCFE) on the cell growth and migration in human colorectal cancer cells, HCT116 and SW480 cells. LCLE and LCBE dose- and time-dependently inhibited the proliferation of HCT116 and SW480 cells. However, LCFE did not affect the proliferation of HCT116 and SW480 cells. In addition, LCLE and LCBE dramatically cell migration and wound healing in HCT116 cells. LCLE and LCBE decreased β-catenin protein level but not mRNA level in HCT116 and SW480 cells. Furthermore, LCLE decreased TCF4 level in both protein and mRNA level in HCT116 and SW480 cells. However, LCBE decreased TCF4 protein level but not mRNA level in HCT116 and SW480 cells. Based on these findings, LCLE and LCBE may inhibit the cell proliferation and migration through blocking Wnt signaling activation in human colorectal cancer cells. Therefore, LCLE and LCBE may be a potential candidate for the development of chemopreventive or therapeutic agents for human colorectal cancer.

• Journal of Applied Biological Chemistry
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• v.66
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• pp.171-178
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• 2023

Morus alba, a popular medicinal plant belonging to the family Moraceae, has long been used commonly in traditional medicine and has various physiological activities, including antidiabetic, anti-microbial, diuretic, anti-oxidant, and anti-cancer activities. Morusinol was isolated from the root bark of M. alba; however, its biological effects have not yet been reported. Therefore, we examined the inhibitory effects of morusinol on human platelet aggregation, Ca²⁺ mobilization, and αIIb/β₃ activity. Our data showed that collagen-induced human platelet aggregation was inhibited by morusinol without cytotoxicity. In this study, we examined whether morusinol inhibits platelet aggregation through the regulation of integrin αIIb/β₃ and its associated signaling molecules. We observed that morusinol inhibited αIIb/β₃ activation by regulating vasodilator-stimulated phosphoprotein, phosphatidylinositol-3 kinase, Akt (protein kinase B), and glycogen synthase kinase-3α/β. These results show that morusinol inhibited fibronectin adhesion, fibrinogen binding, and clot retraction. Taken together, morusinol shows strong antiplatelet and anti-clot retraction effects and is a potential therapeutic drug candidate to prevent platelet-related thrombosis and cardiovascular disease.

• Journal of Life Science
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• v.20 no.7
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• pp.1027-1033
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• 2010

Liriope platyphylla has traditionally been used in Korea and China as a therapeutic drug for the treatment of coughing, sputum, neurodegenerative disorders, obesity, and diabetes. In an effort to assess the functions of a novel extract from Liriope platyphylla in diabetes therapy, the insulin secretion abilities of 10 extracts were screened via measurements of insulin concentration in the culture supernatant using an Insulin ELISA kit. The results of this assay showed the highest levels of insulin in the LP9M80-H treated group, followed by the LP-H, LP-M, LP-E and LP9M80-C treated groups, whereas other extracts did not induce insulin secretion in the HIT-T15 cells. However, the extracts capable of stimulating insulin secretion simultaneously evidenced high apoptotic activity as compared with other extracts. Therefore, one of these extracts, LP9M80-H, was initially selected as the optimal candidate for a therapeutic drug and its optimal concentration was determined. The results of the ELISA and MTT assay demonstrated that a concentration of approximately 100-125 ug/ml of LP9M80-H was optimal with regards to cell viability and insulin secretion in the HIT-T15 cells. These results suggest that LP9M80-H could be considered as an excellent candidate for a diabetes-therapeutic drug that could induce insulin secretion in pancreatic $\beta$-cells.

• The Korean Journal of Nuclear Medicine
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• v.31 no.4
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• pp.433-439
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• 1997

$^{166}Ho$-chitosan complex, or $^{166}Ho$-CHICO, is a candidate pharmaceutical for intracavitary radiation therapy of cystic brain tumors because of the desirable nuclear characteristics of $^{166}Ho$ for therapeutic use and the suitable biological and chemical characteristics of chitosan, not to mention its ready producibility The amount of $^{166}Ho$-CHICO to be administered to obtain the goal therapeutic effect can be suggested by predicting the dose to the cyst wall for a varying pharmaceutical dose. When $^{166}Ho$-CHICO is infused into the cyst, the major part of the energy delivery by beta particles emitted from $^{166}Ho$ occurs in the cyst wall within 4mm in depth from the cyst wall surface. Also, realizing the attachment of $^{166}Ho$-CHICO to the cyst wall surface would change the predictions of dose to the cyst wall.

• Journal of Ginseng Research
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• v.46 no.6
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• pp.750-758
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• 2022

Background: Mild cognitive impairment (MCI) is a transitional condition between normality and dementia. Ginseng is known to have effects on attenuating cognitive deficits in neurogenerative diseases. Ginsenosides are the main bioactive component of ginseng, and their protein targets have not been fully understood. Furthermore, no thorough analysis is reported in ginsenoside-related protein targets in MCI. Methods: The candidate protein targets of ginsenosides in brain tissues were identified by drug affinity responsive target stability (DARTS) coupled with label-free liquid chromatography-mass spectrometry (LC-MS) analysis. Network pharmacology approach was used to collect the therapeutic targets for MCI. Based on the above-mentioned overlapping targets, we built up a proteineprotein interaction (PPI) network in STRING database and conducted gene ontology (GO) enrichment analysis. Finally, we assessed the effects of ginseng total saponins (GTS) and different ginsenosides on mitochondrial function by measuring the activity of the mitochondrial respiratory chain complex and performing molecular docking. Results: We screened 2526 MCI-related protein targets by databases and 349 ginsenoside-related protein targets by DARTS. On the basis of these 81 overlapping genes, enrichment analysis showed the mitochondria played an important role in GTS-mediated MCI pharmacological process. Mitochondrial function analysis showed GTS, protopanaxatriol (PPT), and Rd increased the activities of complex I in a dose-dependent manner. Molecular docking also predicted the docking pockets between PPT or Rd and mitochondrial respiratory chain complex I. Conclusion: This study indicated that ginsenosides might alleviate MCI by targeting respiratory chain complex I and regulating mitochondrial function, supporting ginseng's therapeutic application in cognitive deficits.

• Journal of Life Science
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• v.34 no.5
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• pp.287-295
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• 2024

Hepatocellular carcinoma (HCC) is the second leading cause of cancer-related mortality worldwide, necessitating novel therapeutic strategies. The chemotherapeutic agents used to treat HCC patients are toxic and have serious side effects. Therefore, we investigated the efficacy of anticancer drugs that reduce side effects by targeting tumor cells without causing cytotoxicity in healthy hepatocytes. Berberine, an isoquinoline alkaloid derived from plant compounds, has emerged as a potential candidate for cancer treatment due to its diverse pharmacological properties. The effect of berberine on HepG2 cell viability was determined using the 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide assay. HepG2 cell proliferation was determined through a colony-forming assay. The effects of berberine on HepG2 cell migration were evaluated using a wound-healing assay. Berberine inhibited the proliferation of HepG2 cells, as well as colony formation and migration. Berberine treatment increased the expression of autophagy-related genes and proteins, including Beclin-1 and LC3-II, and elevated the activities and mRNA expression of Caspase-9 and Caspase-3. Additionally, in experiments utilizing the Cell-Derived Xenograft animal model, berberine treatment reduced tumor size and weight in a concentration-dependent manner. These results demonstrate the potential of berberine as a versatile anticancer agent with efficacy in both cellular and animal models of hepatocellular carcinoma. The findings herein shed light on berberine's efficacy against HCC, presenting opportunities for targeted and personalized therapeutic interventions.

• Food Science and Biotechnology
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• v.17 no.2
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• pp.343-348
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• 2008

In this study, antioxidant activity of methanol extract of Glycyrrhiza uralensis Fisch (GUE) against $H_2O_2$-induced DNA damage in human leucocytcs and cell death in PC12 cells was determined. The effect of GUE on $H_2O_2$-induced DNA damage in human leucocytcs was evaluated by the comet assay, where GUE ($1-50\;{\mu}g/mL$) was a dose dependent inhibitor of DNA damage induced by $H_2O_2$. The protective effect of GUE against $H_2O_2$-induced damage on PC12 cells was investigated by MTT reduction assay and lactate dehydrogenase release assay. A marked reduction in cell survival induced by $H_2O_2$ was significantly prevented by $1-50\;{\mu}g/mL$ of GUE. The enzyme activity of caspase-3 was elevated in $H_2O_2$-treated PC12 cells, while preincubation with GUE for 30 min inhibited $H_2O_2$-induced caspase-3 activation in a dose-dependent manner. In conclusion, GUE ameliorates $H_2O_2$-induced DNA damage in human leucocytes and has neuroprotective effect by preventing cell death in PC12 cell, suggesting that GU may be a potential candidate for novel therapeutic agents for neuronal diseases associated with oxidative stress.