• Journal of Life Science
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• v.17 no.8 s.88
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• pp.1034-1038
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• 2007

Hypericin (HyH) is a substance which is isolated a medicinal herb, Hypericum perforatum L., commonly known as St. John's Wort. Hypericum erectum is a long-lived herb that is distributed in Korea. Cloned HyH genes H. erectum of were conformed by sequencing. The cDNA Hyp-1 sequence has 732 bp with an open reading frame of 567. Thus coding for a protein of 152 amino acid residues. A BLAST re-search using the deduced nucleotide sequences in HyH gene produced significant alignments with the H. perforatum. Sequences in HyH gene showed significant homology with Rubus idaeus putative allergen Rub-i-1 mRNA, Protein sequence comparisons revealed significant homology between Hyp-1 and the phenolic oxidative coupling protein hyp-1 of H. perforatum (98%). Additionally, Hyp-1 showed sig-nificant homology with various other classes of allergens, including Pru-av-1 (62%) from Prunus avium and allergen Bet-vl-Sc3 from Betula pendula (60%). Thus, the result of this study may offer an important information to establish an assay system for chemicals of the herbal medicines for H. erectum as well as H. perforatum.

• Journal of Pharmacopuncture
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• v.19 no.1
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• pp.70-73
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• 2016

Objectives: This study was performed to determine the lethal and the inhibitory effects of ethanol extracts of Achillea millefolium (A. millefolium) and Hypericum perforatum (H. perforatum) on Toxoplasma gondii (T. gondii) RH strain tachyzoites in vitro. Methods: The tachyzoites were treated with concentrations of 10, 50, and 100 mg/mL of A. millefolium and H. perforatum extracts within 10, 30, and 45 minutes in the wells. The mortality rates of tachyzoites treated with extracts were determined by using alkaline methylene blue staining. Also, the tachyzoites in cell cultures were treated with concentrations of 50, 100, and 200 mg/mL of these extracts. The cell viability, inhibition concentration ($IC_{50}$), and selectivity were determined from MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assays. Results: In the cell-free in vitro study, all of tachyzoites were killed at concentrations of 100 mg/mL of both extracts while at concentration 10 mg/mL, the mortality was 4.53% - 5.31%. In the cell culture study, the values of the effective concentration ($EC_{50}$) were 215 and $153{\mu}g/mL$ and the selectivities were 0.73 and 0.69 for the A. millefolium and the H. perforatum extracts, respectively. Conclusion: We conclude that neither extracts has any significant effect on the tachyzoites of T. gondii in cell cultures.

• 한국약용작물학회:학술대회논문집
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• 2011.09a
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• pp.174-175
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• 2011

• 한국약용작물학회:학술대회논문집
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• 2008.05a
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• pp.300-301
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• 2008

• Journal of Pharmacopuncture
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• v.22 no.2
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• pp.102-108
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• 2019

Objectives: Esophageal squamous cell carcinoma (ESCC) is considered as a deadly medical condition that affects a growing number of people worldwide. Targeted therapy of ESCC has been suggested recently and required extensive research. With cyclin D1 as a therapeutic target, the present study aimed at evaluating the anticancer effects of doxorubicin (Dox) or Hypericum perforatum L. (HP) extract encapsulated in poly(lactic-co-glycolic acid) (PLGA) nanoparticles on the ESCC cell line KYSE30. Methods: Nanoparticles were prepared using double emulsion method. Cytotoxicity assay was carried out to measure the anti-proliferation activity of Dox-loaded (Dox NPs) and HP-loaded nanoparticles (HP NPs) against both cancer and normal cell lines. The mRNA gene expression of cyclin D1 was evaluated to validate the cytotoxicity studies at molecular level. Results: Free drugs and nanoparticles significantly inhibited KYSE30 cells by 55-73% and slightly affected normal cells up to 29%. The IC50 of Dox NPs and HP NPs was ~ 0.04-0.06 mg/mL and ~ 0.6-0.7 mg/mL, respectively. Significant decrease occurred in cyclin D1 expression by Dox NPs and HP NPs (P < 0.05). Exposure of KYSE-30 cells to combined treatments including both Dox and HP extract significantly increased the level of cyclin D1 expression as compared to those with individual treatments (P < 0.05). Conclusion: Dox NPs and HP NPs can successfully and specifically target ESCC cells through downregulation of cyclin D1. The simultaneous use of Dox and HP extract should be avoided for the treatment of ESCC.

• Bulletin of the Korean Chemical Society
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• v.34 no.5
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• pp.1407-1413
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• 2013

A new compound, perforaphenonoside A (1), along with 11 known compounds (2-12) were isolated from a methanol extract of adventitious roots of Hypericum perforatum. Their chemical structures were elucidated using chemical and physical methods as well as comparison of NMR and mass spectral data with previously reported data. Their inhibition of NF-${\kappa}B$ and activation of PPAR was measured in HepG2 cells using a luciferase reporter system. Among the compounds 3, 6, 7 and 12 inhibited NF-${\kappa}B$ activation stimulated by TNF${\alpha}$ in a dose-dependent manner, with $IC_{50}$ values ranging from 0.85 to $8.10{\mu}M$. Moreover, compounds 1-3, 7, 11 and 12 activated the transcriptional activity of PPARs in a dose-dependent manner, with $EC_{50}$ values ranging from 7.3 to $58.7{\mu}M$. The transactivational effects of compounds 1-3, 7, 11 and 12 were evaluated on three individual PPAR subtypes. Among them, compound 2 activated $PPAR{\alpha}$ transcriptional activity, with 153.97% stimulation at $10{\mu}M$, while compounds 1, 2 and 11 exhibited transcriptional activity of $PPAR{\gamma}$, with stimulation from 124.76% to 126.91% at $10{\mu}M$.

• Korean Journal of Medicinal Crop Science
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• v.12 no.4
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• pp.304-308
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• 2004

Immune enhancing activities of water and ethanol extracts of Hypericum perforatum L. (HP) were examined. HP extracts inhibited the growth of human hepatocarcinoma, human gastric cancer cell and human breast cancer cells in concentration-dependent mammers over a concentration range of $0.05{\sim}1.0\;mg/ml$, showing inhibiton of more than 80% with the concentration of 1.0 mg/ml. However, HP the same concentration. Overall selectivity of the extracts on the three human cancer lines was over 3.5, which is higher than those from the conventional herbs. The growth of human immune B and T cells was enhanced up to 1.4 to 2.0 folds by the addition of the extracts for 4 days, compared to controls. Ethanol extracts of HP after 6 days incubation increased the secretions of tumor necrosis factor-alpha $(TNF-{\alpha})$ from T cells and interleukin-6 (IL-6) from B cells to 6.7 pg/cell and 6.8 pg/cell, respectively. These results suggest that HP has a potent immune enhancing effect.

• Applied Biological Chemistry
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• v.48 no.1
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• pp.65-69
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• 2005

The physiological activity of St. John's wort extracts were examined. Total phenol contents in the ethanol extracts $(246.0{\pm}10.5\;{\mu}g/ml)$ with St. John's wort leaf was higher than that in water extract $(237.4{\pm}13.2\;{\mu}g/ml)$. The electron donating ability in the water extracts and in the ethanol extracts were 95.0% and 95.2% respectively. Antioxidant protection factor of the ethanol extract was higher than that of the water extract. The water extract from St. John's wort leaves did not show an antimicrobial activity against Helicobacter pylori, but the ethanol extract revealed high antimicrobial activities such as 11 mm of clear zone in $100\;{\mu}g/ml$ of phenol content and 13 mm of clear zone in $150\;{\mu}g/ml$ of phenol content. The hot water extract showed an angiotensin converting enzyme inhibitory activity of 19.2%. The xanthin oxidase inhibitory activity of hot water and ethanol extract were very high, amounting to 84.8% and 100% respectively. The results suggested a possibility for developing the phenol compounds in St. John's wort as anti Helicobacter pylori, anti-oxidant and anti-gout agents.

• Biomolecules & Therapeutics
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• v.25 no.2
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• pp.158-164
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• 2017

Methylglyoxal (MGO) is a highly reactive metabolite of glucose which is known to cause damage and induce apoptosis in endothelial cells. Endothelial cell damage is implicated in the progression of diabetes-associated complications and atherosclerosis. Hypericin, a naphthodianthrone isolated from Hypericum perforatum L. (St. John's Wort), is a potent and selective inhibitor of protein kinase C and is reported to reduce neuropathic pain. In this work, we investigated the protective effect of hypericin on MGO-induced apoptosis in human umbilical vein endothelial cells (HUVECs). Hypericin showed significant anti-apoptotic activity in MGO-treated HUVECs. Pretreatment with hypericin significantly inhibited MGO-induced changes in cell morphology, cell death, and production of intracellular reactive oxygen species. Hypericin prevented MGO-induced apoptosis in HUVECs by increasing Bcl-2 expression and decreasing Bax expression. MGO was found to activate mitogen-activated protein kinases (MAPKs). Pretreatment with hypericin strongly inhibited the activation of MAPKs, including P38, JNK, and ERK1/2. Interestingly, hypericin also inhibited the formation of AGEs. These findings suggest that hypericin may be an effective regulator of MGO-induced apoptosis. In conclusion, hypericin downregulated the formation of AGEs and ameliorated MGO-induced dysfunction in human endothelial cells.