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1.
Biomed Rep ; 4(4): 449-452, 2016 Apr.
Article in English | MEDLINE | ID: mdl-27073630

ABSTRACT

Candida albicans (C. albicans) is an opportunistic fungal pathogen, particularly observed in immunocompromised patients. C. albicans accounts for 50-70% of cases of invasive candidiasis in the majority of clinical settings. Terbinafine, an allylamine antifungal drug, has been used to treat fungal infections previously. It has fungistatic activity against C. albicans. Traditional Chinese medicines can be used as complementary medicines to conventional drugs to treat a variety of ailments and diseases. Berberine is a quaternary alkaloid isolated from the traditional Chinese herb, Coptidis Rhizoma, while berberrubine is isolated from the medicinal plant Berberis vulgaris, but is also readily derived from berberine by pyrolysis. The present study demonstrates the possible complementary use of berberine and berberrubine with terbinafine against C. albicans. The experimental findings assume that the potential application of these alkaloids together with reduced dosage of the standard drug would enhance the resulting antifungal potency.

2.
Phytother Res ; 28(5): 781-3, 2014 May.
Article in English | MEDLINE | ID: mdl-23913631

ABSTRACT

The anticancer action of gallotannins is a well-developed topic. We have demonstrated the in vivo antitumour activity of corilagin on Hep3B hepatoma using the xenograft athymic nude mice model. Here, we further report the potential sensitization of Hep3B hepatoma cells to cisplatin and doxorubicin by corilagin. Our results showed that corilagin is able to enhance the cytotoxicity of both cisplatin and doxorubicin on the Hep3B hepatoma cells. We speculate the possible use of corilagin in combination with low dosages of the anticancer chemotherapeutic standard drugs like cisplatin and doxorubicin, with the aim of obtaining an increment in the anticancer effect.


Subject(s)
Antineoplastic Agents/pharmacology , Carcinoma, Hepatocellular/pathology , Cisplatin/pharmacology , Doxorubicin/pharmacology , Glucosides/pharmacology , Liver Neoplasms/pathology , Animals , Antineoplastic Agents/administration & dosage , Cell Line, Tumor , Cell Survival/drug effects , Cisplatin/administration & dosage , Doxorubicin/administration & dosage , Drug Synergism , Glucosides/administration & dosage , Humans , Hydrolyzable Tannins , Mice , Mice, Nude , Xenograft Model Antitumor Assays
3.
Bioorg Med Chem Lett ; 23(8): 2373-6, 2013 Apr 15.
Article in English | MEDLINE | ID: mdl-23473678

ABSTRACT

We explore the possible cellular cytotoxic activity of an amphiphilic silicon(IV) phthalocyanine with axially ligated rhodamine B under ambient light experimental environment as well as its in vivo antitumour potential using Hep3B hepatoma cell model. After loading into the Hep3B hepatoma cells, induction of cellular cytotoxicity and cell cycle arrest were detected. Strong growth inhibition of tumour xenograft together with significant tumour necrosis and limited toxicological effects exerted on the nude mice could be identified.


Subject(s)
Antineoplastic Agents/pharmacology , Indoles/chemistry , Indoles/pharmacology , Rhodamines/chemistry , Rhodamines/pharmacology , Silicon/pharmacology , Animals , Antineoplastic Agents/chemistry , Cell Line, Tumor , Humans , Isoindoles , Liver Neoplasms/drug therapy , Mice , Mice, Nude , Random Allocation , Silicon/chemistry , Xenograft Model Antitumor Assays
4.
Int Immunopharmacol ; 13(3): 308-15, 2012 Jul.
Article in English | MEDLINE | ID: mdl-22561123

ABSTRACT

Corilagin (beta-1-O-galloyl-3,6-(R)-hexahydroxydiphenoyl-d-glucose), a gallotannin identified in several plants, including Phyllanthus urinaria, has been shown to exhibit versatile medicinal activities. As far as possible anti-inflammatory effects of corilagin, only few reports are available, and the potential use of corilagin as possible therapeutic molecule for cystic fibrosis has not been evaluated. In the present paper we report experiments aimed at determining the activity of corilagin on nuclear factor kappaB (NF-kappaB) binding to DNA target and on the expression of the major pro-inflammatory gene involved in cystic fibrosis, interleukin-8 (IL-8). Both IL-8 mRNA content and IL-8 protein secretion were analyzed in cystic fibrosis bronchial IB3-1 cells stimulated by tumor necrosis factor-alpha (TNF-alpha), one of the most potent pro-inflammatory agents. The data obtained demonstrate that corilagin binds to NF-kappaB, inhibits NF-kappaB/DNA interactions and affects IL-8 gene expression in TNF-alpha treated IB3-1 cells. In addition, corilagin inhibits TNF-alpha induced secretion of MCP-1 and RANTES, exhibiting low or no effect on the release of G-CSF, IL-6 and VEGF. Therefore, corilagin might be of interest for experimental anti-inflammatory therapy of cystic fibrosis.


Subject(s)
Cystic Fibrosis/drug therapy , Glucosides/pharmacology , Interleukin-8/genetics , NF-kappa B/antagonists & inhibitors , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Base Sequence , Cell Line , Chemokine CCL2/metabolism , Chemokine CCL5/metabolism , Cystic Fibrosis/genetics , Cystic Fibrosis/immunology , Cystic Fibrosis/metabolism , Cystic Fibrosis Transmembrane Conductance Regulator/genetics , Down-Regulation/drug effects , Humans , Hydrolyzable Tannins , Interleukin-8/metabolism , Mutation , NF-kappa B/metabolism , RNA, Messenger/genetics , RNA, Messenger/metabolism , Tumor Necrosis Factor-alpha/pharmacology
5.
Chem Biodivers ; 8(10): 1853-63, 2011 Oct.
Article in English | MEDLINE | ID: mdl-22006713

ABSTRACT

Six new protopanaxadiol-type ginsenosides, named ginsenosides Ra(4) -Ra(9) (1-6, resp.), along with 14 known dammarane-type triterpene saponins, were isolated from the root of Panax ginseng, one of the most important Chinese medicinal herbs. The structures of the new compounds were determined by spectroscopic methods, including 1D- and 2D-NMR, HR-MS, and chemical transformation as (20S)- 3-O-{ß-D-6-O-[(E)-but-2-enoyl]glucopyranosyl-(1→2)-ß-D-glucopyranosyl}-20-O-[ß-D-xylopyranosyl-(1→4)-α-L-arabinopyranosyl-(1→6)-ß-D-glucopyranosyl]protopanaxadiol (1), (20S)-3-O-[ß-D-6-O-acetylglucopyranosyl-(1→2)-ß-D-glucopyranosyl]-20-O-[ß-D-xylopyranosyl-(1→4)-α-L-arabinopyranosyl-(1→6)-ß-D-glucopyranosyl]protopanaxadiol (2), (20S)-3-O-{ß-D-6-O-[(E)-but-2-enoyl]glucopyranosyl-(1→2)-ß-D-glucopyranosyl}-20-O-[ß-D-glucopyranosyl-(1→6)-ß-D-glucopyranosyl]protopanaxadiol (3), (20S)-3-O-{ß-D-6-O-[(E)-but-2-enoyl]glucopyranosyl-(1→2)-ß-D-glucopyranosyl}-20-O-[α-L-arabinopyranosyl-(1→6)-ß-D-glucopyranosyl]protopanaxadiol (4), (20S)-3-O-{ß-D-4-O-[(E)-but-2-enoyl]glucopyranosyl-(1→2)-ß-D-glucopyranosyl}-20-O-[α-L-arabinofuranosyl-(1→6)-ß-D-glucopyranosyl]protopanaxadiol (5), (20S)-3-O-{ß-D-6-O-[(E)-but-2-enoyl]glucopyranosyl-(1→2)-ß-D-glucopyranosyl}-20-O-[α-L-arabinofuranosyl-(1→6)-ß-D-glucopyranosyl]protopanaxadiol (6). The sugar moiety at C(3) of the aglycone of each new ginsenoside is butenoylated or acetylated.


Subject(s)
Ginsenosides/chemistry , Panax/chemistry , Plant Roots/chemistry , Sapogenins/chemistry , Acylation , Molecular Structure , Plants, Medicinal/chemistry
6.
Eur J Pharmacol ; 668(1-2): 88-98, 2011 Oct 01.
Article in English | MEDLINE | ID: mdl-21703260

ABSTRACT

20(S)-Protopanaxadiol (PPD), a metabolite of ginsenosides, has been demonstrated to possess cytotoxic effects on several cancer cell lines. The molecular mechanism is, however, not well understood. In this study, we have shown that PPD inhibits cell growth and induces apoptosis in human hepatocarcinoma HepG2 cells. PPD-treated cells showed a massive cytoplasmic vacuolization and a dramatic change of endoplasmic reticulum (ER) morphology. The induction of ER stress is associated with the upregulation of ER stress-associated genes and proteins. PPD activates the unfolded protein response (UPR) through the phosphorylation of PERK and eIF2α, the splicing of XBP1 mRNA, and the cleavage of AFT6. PPD also induces the intrinsic and extrinsic apoptotic pathways. It activates DR5, caspase-8, -9, -3, and promotes the cleavage of PARP while it downregulates Bcl-2, Bcl-x(L) and mitochondrial membrane potential. Knockdown of one of the three UPR limbs by specific siRNAs did not affect PPD-induced apoptosis, which was however, significantly suppressed by the downregulation of CHOP. Western blot analysis showed that PPD-stimulated downregulation of Bcl-2 protein, increase of DR5 protein, activation of caspase-8 and cleavage of PARP were significantly inhibited in CHOP siRNA-transfected cells. Taken together, we have identified ER as a molecular target of PPD and our data support the hypothesis that PPD induces HepG2 cell apoptosis through the ER stress pathway.


Subject(s)
Apoptosis/drug effects , Endoplasmic Reticulum Stress/drug effects , Ginsenosides/metabolism , Liver Neoplasms/pathology , Sapogenins/metabolism , Sapogenins/pharmacology , Extracellular Signal-Regulated MAP Kinases/metabolism , Hep G2 Cells , Humans , MAP Kinase Signaling System/drug effects , Mitochondria/drug effects , Mitochondria/metabolism , Receptors, TNF-Related Apoptosis-Inducing Ligand/metabolism , Transcription Factor CHOP/metabolism , Unfolded Protein Response/drug effects , Up-Regulation/drug effects , Vacuoles/drug effects , Vacuoles/metabolism , p38 Mitogen-Activated Protein Kinases/metabolism
7.
J Agric Food Chem ; 59(1): 200-5, 2011 Jan 12.
Article in English | MEDLINE | ID: mdl-21141994

ABSTRACT

Ginseng, the root of Panax ginseng C. A. Meyer (Araliaceae), is one of the most important traditional medicines and functional foods. A detailed phytochemical investigation on the roots of P. ginseng led to the isolation of 6 new natural protopanaxatriol (PPT)-type ginsenosides, ginsenosides Re(1)-Re(6) (compounds 1-6), along with 10 known PPT-type ginsenosides. Their structures were elucidated on the basis of chemical and spectroscopic analyses, including high-resolution mass spectrometry (HRMS) and 1D and 2D nuclear magnetic resonance (NMR). The unusual α-D-glucopyranosyl-(1→3)-ß-D-glucopyranosyl sugar chain, as found in compounds 1 and 2, is reported in the genus Panax for the first time.


Subject(s)
Ginsenosides/chemistry , Panax/chemistry , Plant Extracts/chemistry , Sapogenins/chemistry , Molecular Structure , Plant Roots/chemistry
8.
Phytomedicine ; 18(1): 11-5, 2010 Dec 15.
Article in English | MEDLINE | ID: mdl-21036022

ABSTRACT

We have investigated the potential in vivo anti-tumour activity of corilagin using the Hep3B hepatocellular carcinoma cell line and an athymic nude mice xenograft model. The purity of corilagin was confirmed by high performance liquid chromatographic analysis. Corilagin was administrated intraperitoneally for a continuous period of 7 days at a concentration of 15 mg/kg of body weight per day. A significant inhibition of tumour growth was observed when treated mice are compared with control groups. Furthermore, analysis of enzymes markers of liver function, including alanine aminotransferase and asparate aminotransferase, suggested that current therapeutic dosage of corilagin did not exert adverse effect on liver. Our observations support the view that corilagin is considerably effective to retard the in vivo growth of xenografted Hep3B hepatocellular carcinoma.


Subject(s)
Antineoplastic Agents, Phytogenic/therapeutic use , Carcinoma, Hepatocellular/drug therapy , Glucosides/therapeutic use , Liver Neoplasms/drug therapy , Phytotherapy , Plant Extracts/therapeutic use , Animals , Antineoplastic Agents, Phytogenic/administration & dosage , Antineoplastic Agents, Phytogenic/pharmacology , Cell Line, Tumor , Glucosides/administration & dosage , Glucosides/pharmacology , Humans , Hydrolyzable Tannins , Liver/drug effects , Liver/enzymology , Mice , Mice, Nude , Plant Extracts/administration & dosage , Plant Extracts/pharmacology , Xenograft Model Antitumor Assays
9.
Forsch Komplementmed ; 17(4): 209-13, 2010.
Article in English | MEDLINE | ID: mdl-20829599

ABSTRACT

AIM: Recently, we have demonstrated that silymarin has a comparable pharmaceutical activity as Phyllanthus urinaria extract when used to rescue mice from acetaminophen-induced acute liver injury. In the present study, we further compared the therapeutic action of silymarin with N-acetyl cysteine (commonly used in clinical practice for emergency treatments) as a rescuer in mice after administering a lethal dose of acetaminophen for 24 h. METHODS: Acute liver injury was induced in the treatment groups by intraperitoneally administered acetaminophen at a dose of 550 mg/kg body weight on day 1. The control group received an equal volume of physiological saline intraperitoneally. From day 2 to 4, the treatment groups received various doses of silymarin or N-acetyl cysteine orally once daily, while the control group and the acetaminophen group received an equal volume of water orally. The mortality rate was recorded in all groups. On day 5, all mice were sacrificed for examination. RESULTS: Silymarin greatly improved the counteracting effects on mortality rate as compared to N-acetyl cysteine. CONCLUSION: Silymarin should be further considered as an antidote for patients with acetaminopheninduced acute hepatic injury and delayed treatment.


Subject(s)
Acetaminophen/toxicity , Antioxidants/therapeutic use , Chemical and Drug Induced Liver Injury/drug therapy , Silymarin/therapeutic use , Alanine Transaminase/drug effects , Alanine Transaminase/metabolism , Animals , Aspartate Aminotransferases/drug effects , Aspartate Aminotransferases/metabolism , Chemical and Drug Induced Liver Injury/etiology , Chemical and Drug Induced Liver Injury/pathology , Liver/drug effects , Liver/pathology , Mice , Mice, Inbred C57BL
10.
Phytomedicine ; 16(8): 751-60, 2009 Aug.
Article in English | MEDLINE | ID: mdl-19386480

ABSTRACT

Acetaminophen is a commonly used drug for the treatment of patients with common cold and influenza. However, an overdose of acetaminophen may be fatal. In this study we investigated whether mice, administered intraperitoneally with a lethal dose of acetaminophen, when followed by oral administration of Phyllanthus urinaria extract, may be prevented from death. Histopathological analysis of mouse liver sections showed that Phyllanthus urinaria extract may protect the hepatocytes from acetaminophen-induced necrosis. Therapeutic dose of Phyllanthus urinaria extract did not show any toxicological phenomenon on mice. Immunohistochemical staining with the cytochrome P450 CYP2E1 antibody revealed that Phyllanthus urinaria extract reduced the cytochrome P450 CYP2E1 protein level in mice pre-treated with a lethal dose of acetaminophen. Phyllanthus urinaria extract also inhibited the cytochrome P450 CYP2E1 enzymatic activity in vitro. Heavy metals, including arsenic, cadmium, mercury and lead, as well as herbicide residues were not found above their detection limits. High performance liquid chromatography identified corilagin and gallic acid as the major components of the Phyllanthus urinaria extract. We conclude that Phyllanthus urinaria extract is effective in attenuating the acetaminophen induced hepatotoxicity, and inhibition of cytochrome P450 CYP2E1 enzyme may be an important factor for its therapeutic mechanism.


Subject(s)
Acetaminophen/toxicity , Chemical and Drug Induced Liver Injury/prevention & control , Cytochrome P-450 CYP2E1 Inhibitors , Liver/metabolism , Phyllanthus , Phytotherapy , Plant Extracts/therapeutic use , Animals , Chemical and Drug Induced Liver Injury/mortality , Chemical and Drug Induced Liver Injury/pathology , Gallic Acid/isolation & purification , Gallic Acid/pharmacology , Gallic Acid/therapeutic use , Glucosides/isolation & purification , Glucosides/pharmacology , Glucosides/therapeutic use , Hepatocytes/drug effects , Hydrolyzable Tannins , Liver/pathology , Metals, Heavy/analysis , Mice , Mice, Inbred C57BL , Necrosis/drug therapy , Phyllanthus/chemistry , Plant Extracts/chemistry , Plant Extracts/pharmacology , Plants, Medicinal/chemistry
11.
Int J Mol Med ; 18(5): 975-9, 2006 Nov.
Article in English | MEDLINE | ID: mdl-17016630

ABSTRACT

We have previously demonstrated the possible growth inhibitory activity of both first generation of the effective microorganism fermentation extract (EM-X) as well as the second generation (EM-X2) on cancer cell lines in vitro. The possible anti-angiogenic potential of EM-X has not been reported. Herein we show that using the concentrated EM-X, the growth of human umbilical cord endothelial cells (HUCE) was significantly inhibited in vitro. Enzyme linked immunosorbent assay suggested that the concentrated EM-X is able to reduce the level of vascular endothelial growth factor (VEGF) from Hep3B hepatocellular carcinoma (HCC) cells. The conditioned culture medium obtained from the concentrated EM-X incubated Hep3B HCC cells possessed significant antiproliferative effect on the HUCE cells. Moreover, in vivo chick chorioallantoic membrane assay further demonstrated that the concentrated EM-X is able to greatly inhibit the basic fibroblast growth factor induced angiogenesis from chick embryo experiment. We speculate that the anti-cancer potential of this concentrated EM-X involved growth inhibition on cancer cell and antiangiogenic effect on HUCE cells.


Subject(s)
Angiogenesis Inhibitors/pharmacology , Endothelium, Vascular/drug effects , Plant Extracts/pharmacology , Vascular Endothelial Growth Factor A/antagonists & inhibitors , Animals , Cell Line, Tumor , Cell Proliferation/drug effects , Chick Embryo , Chromatography, High Pressure Liquid , Culture Media, Conditioned , Down-Regulation , Endothelium, Vascular/cytology , Humans , Plant Extracts/analysis , Umbilical Cord/cytology , Vascular Endothelial Growth Factor A/analysis
12.
Int J Mol Med ; 17(2): 279-84, 2006 Feb.
Article in English | MEDLINE | ID: mdl-16391827

ABSTRACT

The effective microorganism fermentation extract (EM-X, the first generation) was claimed to possess strong anti-oxidation property. On the other hand, we have shown that the second generation of the effective microorganism fermentation extract (EM-X2) possessed growth inhibition on human cancer cells involving MDA-MB231 breast cancer and K-562 chronic myelogenous leukaemia cells. Elevation of super oxide dismutase activity from EM-X2 treated cancer cell extract was observed. However, the possible anti-cancer activity of the first generation of the EM-X was not reported. Here we demonstrate that the concentrated form of the EM-X from its original fluid also possess antiproliferation ability together with induction of apoptosis on the human cancer cell lines including Hep3B hepatocellular carcinoma (HCC) and KG1a acute myelogenous leukaemia (AML). Similar effect could also be demonstrated on primary cultured bone marrow samples isolated from patients with AML. Morphological inspection revealed that common apoptotic feature was found on these concentrated EM-X treated cancer cells. Both the anchorage-dependent clonogenicity assay on Hep3B HCC and methyl-cellulose colony formation assay on KG1a cells and bone marrow cells from AML patients further revealed the ability of the concentrated EM-X on reducing their colony formation ability. Incubating KG1a with concentrated EM-X readily induced apoptosis as demonstrated by flow cytometric analysis. Interestingly, few growth inhibition effect of the concentrated EM-X was observed on both the SV40 transformed THLE-2 liver epithelial cells and primary cultured non-malignant haematological disordered bone marrow. Collectively, this concentrated EM-X is effective in inducing cell death and reducing the regeneration potential of both Hep3B HCC and KG1a AML cells in vitro.


Subject(s)
Apoptosis/drug effects , Carcinoma, Hepatocellular/pathology , Fermentation , Leukemia, Myeloid, Acute/pathology , Plant Extracts/pharmacology , Antioxidants/pharmacology , Bone Marrow Cells/cytology , Bone Marrow Cells/drug effects , Cell Line, Tumor , Cell Proliferation/drug effects , Culture Media , Epithelial Cells , Humans , Transformation, Genetic
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