• Asian Pacific Journal of Cancer Prevention
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• v.16 no.13
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• pp.5371-5376
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• 2015

Berberine (B1), isolated from stems of Coscinium fenestratum (Goetgh.) Colebr, was used as a principle structure to synthesize three phenolic derivatives: berberrubine (B2) with a single phenolic group, berberrubine chloride (B3) as a chloride counter ion derivative, and 2,3,9,10-tetra-hydroxyberberine chloride (B4) with four phenolic groups, to investigate their direct and indirect antioxidant activities. For DPPH assay, compounds B4, B3, and B2 showed good direct antioxidant activity ($IC_{50}$ values=$10.7{\pm}1.76$, $55.2{\pm}2.24$, and $87.4{\pm}6.65{\mu}M$, respectively) whereas the $IC_{50}$ value of berberine was higher than $500{\mu}M$. Moreover, compound B4 exhibited a better DPPH scavenging activity than BHT as a standard antioxidant ($IC_{50}=72.7{\pm}7.22{\mu}M$) due to the ortho position of hydroxyl groups and its capacity to undergo intramolecular hydrogen bonding. For cytotoxicity assay against human fibrosarcoma cells (HT1080) using MTT reagent, the sequence of $IC_{50}$ value at 7-day treatment stated that B1 < B4 < B2 ($0.44{\pm}0.03$, $2.88{\pm}0.23$, and $6.05{\pm}0.64{\mu}M$, respectively). Berberine derivatives, B2 and B4, showed approximately the same level of CAT expression and significant up-regulation of SOD expression in a dose-dependent manner compared to berberine treatment for 7-day exposure using reverse transcription-polymerase chain reaction (RT-PCR) assays. Our findings show a better direct-antioxidant activity of the derivatives containing phenolic groups than berberine in a cell-free system. For cell-based system, berberine was able to exert better cytotoxic activity than its derivatives. Berberine derivatives containing a single and four phenolic groups showed improved up-regulation of SOD gene expression. Cytotoxic action might not be the main effect of berberine derivatives. Other pharmacological targets of these derivatives should be further investigated to confirm the medical benefit of phenolic groups introduced into the berberine molecule.

• Journal of the Korean Association of Oral and Maxillofacial Surgeons
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• v.26 no.1
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• pp.53-58
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• 2000

Treatment of oral cancers with chemotherapeutic agents are evaluated as an effective method for remission to reduce cancer proliferation nowadays. But, minimization of side-effects such as bone marrow suppression, gastrointestinal toxicity and renal damage is another problem to be solved. Thus, a possible approach to develop a clinically applicable chemotherapeutic agents is to screen anticancer activity among traditional medicinal plants which have been used for thousands of years with very low side-effects in orient. In this study we focused on screening anti-oral cancer activities among 14 traditional medicinal plant extracts that revealed anticancer activities on other solid tumors. The results were as follow : 1. Methanol extract of Lepidium apetalum showed the highest anti-oral cancer activity against A253 cells. At concentration of $4{\mu}g/ml$, the cell viability was 48% under our experimental condition. $IC_{50}$ value obtained was $4{\mu}g/ml$. 2. Methanol extract of Coptis japonica and Solanum nigrum were effective on KB cells. Cell viability observed were 62% and 67% at concentration of $4{\mu}g/ml$, and $IC_{50}$ values were $12{\mu}g/ml$ and $10{\mu}g/ml$ respectively. 3. When the methanol extract of Lonicera caerule was combined with $2{\mu}g/ml$ of cisplatin, the anticancer activity was synergistically increased. One hundred ${\mu}g/ml$ of Lonicera caerule showed 92%(alone) or 59%(combined with cisplatin) cell viabilities. $IC_{50}$ value of Lonicera caerule extract against KB cells was reduced from $301{\mu}g/ml$ to $126{\mu}g/ml$ when combined with $2{\mu}g/ml$ of cisplatin. 4. Medicinal plant extracts effective on both A253 and KB cells were Coptis japonica, Lepidium apetalum, Solanum nigrum, Caesalpiniae Lignum, Curcuma aromatica.

• The Journal of Korean Medicine
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• v.42 no.3
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• pp.44-55
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• 2021

Objectives: As the use of herbal medicinal products (HMPs) increases worldwide, systematic verification of the safety of HMPs is required. The induction of cardiotoxicity is one of the major factors in post-approval withdrawal of medicinal products, and drug-induced cardiotoxicity assessment is emerging as an important step in drug development. In the present study, we evaluated human ether-à-go-go-related gene (hERG) potassium channel-related cardiotoxicity to predict the risk of cardiac arrhythmia in thirteen herbal medicines known to have cardiac toxicity. Methods: We measured the inhibition rate of hERG potassium channel activity of 13 medicinal herbal extracts in hERG-expressing HEK 293 cells using an automated patch-clamping system. Quinidine was used as a positive control for inhibition of hERG activity. Results: Extracts of Evodiae Fructus, Strychni Semen, and Corydalis Tuber potently inhibited the activity of hERG, and IC₅₀ values were 3.158, 19.87, and 41.26 ㎍/mL, respectively. Cnidi Fructus, Ephedra Herba, Lithospermi Radix, Polygoni Multiflori Radix, Visci Ramulus et Folium, Asiasari Radix et Rhizoma, and Scolopendra weakly inhibited hERG activity, and the IC₅₀ value for each herbal medicine was more than 400 ㎍/mL. Aconiti Kusnezoffii Tuber and two types of Aconiti Lateralis Radix Preparata (Po and Yeom) had weak inhibitory activity against hERG, and the IC₅₀ values were more than 700 ㎍/mL. The IC₅₀ value of quinidine against hERG was 1.021 𝜇M. Conclusion: Evodiae Fructus, Strychni Semen, and Corydalis Tuber acted as potent inhibitors against hERG. These herbal medicines may cause cardiac arrhythmia through QT prolongation, so care should be taken when taking them.

• Biomolecules & Therapeutics
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• v.18 no.2
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• pp.205-210
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• 2010

Several studies have shown that plant-derived polyphenols reduce cardiovascular accidents in high-risk patients and the inhibition of platelet function may be responsible for part of this benefit. Lindera obtusiloba is widely used in traditional herbal medicine for the treatment of cardiovascular and inflammatory diseases. Therefore, the antiplatelet and antithrombotic activities of Lindera obtusiloba Extracts (LOE) on in vitro platelet aggregation, radical scavenging activity and in vivo murine pulmonary thrombosis were examined. LOE was able to directly scavenge the stable DPPH radical in a concentration-dependent manner and its $IC_{50}$ value was 3.9 ${\pm}$ 0.1 ${\mu}g$/ml. LOE significantly inhibited collagen- and ADP-induced platelet aggregation in a concentration-dependent manner and its $IC_{50}$ value is 0.9 ${\pm}$ 0.1 mg/ml and 0.4 ${\pm}$ 0.1 mg/ml respectively. The inhibitory effect of LOE was comparable to aspirin ($IC_{50}$ values were 1.0 ${\pm}$ 0.5 and 1.0 ${\pm}$ 0.7 mg/ml, respectively). Furthermore, oral administration of LOE suppressed the death of mice with pulmonary thrombosis induced by intravenous injection of collagen plus epinephrine. Taken together, our results suggest LOE may be a promising candidate for antithrombotic agent, and the antithrombotic effect of LOE may be due to, at least in part, antiplatelet activity.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.35 no.3
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• pp.229-233
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• 2009

20 species of plants were extracted with Methanol and were investigated for DPPH radical scavenging activity and ABTs free radical scavenging activity to quest anti-oxidation ability depending on the proton beam irradiation quantity. In the proton beam irradiation, 15 species's activities increased but among them, Pharbities nil Choisy decreased at 10 KGray and 4 species' activity didn't change at all. In hydrogen ion radical elimination activity, Ulmus macrocarpa (84 %) showed the highest and Pharbitis nil Choisy showed 6 % decreasing at more than 1 KGray. By comparison with untreated $IC_{50}$ value, the beam-treated $IC_{50}$ value increased 6.3 times for Dioscorea batatas Decne. at 1 KGray, 2.1 times for Trichosanthes kirilowii Max., and 2.8 times for Dioscorea batatas Decne. at 5 KGray. In ABTs free radical elimination activity, the activity increased 60 % for Terminalia chebula Retzius compared with untreated one. Besides, the beam-treated $IC_{50}$ value increased 2 times for Gray Ephedra sinica Stapf, 2.5 times for Terminalia chebula Retz. and 2.4 times for Arctium lappa Linne at 1 KGray.

• Mycobiology
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• v.36 no.2
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• pp.102-105
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• 2008

The acetylcholinesterase (AChE) inhibitor of Yarrowia lipolytica S-3 was maximally produced when it was incubated at $30^{\circ}C$ for 36 h in an optimal medium containing 1% yeast extract, 2% peptone and 2% glucose, with an initial pH 6.0. The final AChE inhibitory activity under these conditions was an $IC_{50}$ value of 64mg/ml. After partial purification of the AChE inhibitor by means of systematic solvent extraction, the final $IC_{50}$ value of the partially purified AChE inhibitor was 0.75 mg/ml. We prepared a test product by using the partially purified AChE inhibitor and then determined its stability for the development of a new antidementia commercial product. The test product was stable at room temperature for 15 weeks.

• Natural Product Sciences
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• v.14 no.3
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• pp.192-195
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• 2008

Three known compounds, puerarol (1), pueroside B (2), and ononin (3), were isolated from an EtOAc-soluble fraction of the roots of Pueraria lobata. The isolates (1 - 3) were subjected to an in vitro bioassay to evaluate their inhibitory activity on the formation of advanced glycation end products (AGEs). Puerarol (1) exhibited a remarkable inhibitory activity on AGEs formation with $IC_{50}$ value of $2.05{\pm}0.32{\mu}M$ as compared with positive control, aminoguanidine ($IC_{50}$ value : $905.32{\pm}7.58{\mu}M$).

• Korean Journal of Pharmacognosy
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• v.29 no.3
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• pp.169-172
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• 1998

Hyaluronidase is one of the mucopolysaccharide-splitting enzyme and is related to the permeability of the vascular system and inflammation. An anti-hyaluronidase assay guided fractionation of the methanolic extract of Uncariae Ramulus et Uncus has furnished a pentacyclic triterpene, ursolic acid (compound I). Compound I exhibited hyaluronidase inhibitory activity with $IC_{50}$ value of 0.15 mM, and disodium cromoglycate showed the inhibitory activity with $IC_{50}$ value of 1.78 mM as a positive control.

• Natural Product Sciences
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• v.9 no.1
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• pp.34-37
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• 2003

We examined methanol extracts prepared from the Korean plants for their inhibitory effects on rat lens aldose reductase (RLAR) activity in vitro. Among 41 plant extracts, the extracts of Lagerstroemia indica, Punica granatum, Eurya japonica, Liquidambar styraciflua, and Vitis coignetiae exhibited highest inhibitory potency, even more potent than tetramethylene glutaric acid (TMG), known as one of typical aldose reductase inhibitors $(IC_{50}\;value,\;0.51\;{\mu}g/ml)$. Especially, the extract of Lagerstroemia indica (Lythraceae), exhibited the most inhibitory potency $(IC_{50}\;value,\;0.069\;{\mu}/ml)$ on RLAR.

• International Journal of Oral Biology
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• v.30 no.4
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• pp.117-123
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• 2005

Various aspects of antioxidant activity in vitamin C were evaluated in this study. Relatively high level of 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity was detected in vitamin C, but not in non-antioxidative vitamin, vitamin B1. Vitamin C also reduced the production of lipid peroxidation in Chinese hamster lung fibroblast (V79-4) cells with $IC_{50}$ value of $4{\mu}g/ml$. Vitamin B1 showed comparable reduction in lipid peroxidation products ($IC_{50}$ value was about $10{\mu}g/ml$). It was shown that vitamin C also dose-dependently enhanced the activities of superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPX) in V79-4 cells, and these effects were not observed in vitamin Bl-treated cells. Our data suggest that well-known antioxidant vitamin C involved in direct activation of SOD, CAT and GPX.