scholarly journals Antitumour Effects of Isocurcumenol Isolated from Curcuma zedoaria Rhizomes on Human and Murine Cancer Cells

2011 ◽  
Vol 2011 ◽  
pp. 1-13 ◽  
Author(s):  
S. Lakshmi ◽  
G. Padmaja ◽  
P. Remani
Keyword(s):  
Cancer Cells ◽  
Biological Activities ◽  
Curcuma Zedoaria ◽  
Cytotoxic Effects ◽  
Traditional System ◽  
Significant Toxicity ◽  
The Family ◽  
Ascitic Tumour ◽  
Reducing Properties

Curcuma zedoaria belonging to the family Zingiberaceae has been used in the traditional system of medicine in India and Southwest Asia in treating many human ailments and is found to possess many biological activities. The rationale of the present study was to isolate, identify, and characterize antitumour principles from the rhizomes of Curcuma zedoaria, to assess its cytotoxic effects on human and murine cancer cells, to determine its apoptosis inducing capacity in cancer cells, and to evaluate its tumour reducing properties in in vivo mice models. Isocurcumenol was characterized as the active compound by spectroscopy and was found to inhibit the proliferation of cancer cells without inducing significant toxicity to the normal cells. Fluorescent staining exhibited the morphological features of apoptosis in the compound-treated cancer cells. In vivo tumour reduction studies revealed that a dose of 35.7 mg/kg body weight significantly reduced the ascitic tumour in DLA-challenged mice and increased the lifespan with respect to untreated control mice.

Botany, Phytochemistry, Pharmacology and Toxicity of Strychnos nux-vomica L.: A Review

2018 ◽  
Vol 46 (01) ◽  
pp. 1-23 ◽  
Author(s):  
Rixin Guo ◽  
Ting Wang ◽  
Guohong Zhou ◽  
Mengying Xu ◽  
Xiankuo Yu ◽  
...  
Keyword(s):  
Biological Activities ◽  
Iridoid Glycosides ◽  
Animal Experiments ◽  
Flavonoid Glycosides ◽  
Antitumor Effects ◽  
Detoxification Mechanism ◽  
The Family ◽  
Pharmacology And Toxicology

Strychnos nux-vomica L. belongs to the genus Strychnos of the family Loganiaceae and grows in Sri Lanka, India and Australia. The traditional medicinal component is its seed, called Nux vomica. This study provides a relevant and comprehensive review of S. nux-vomica L., including its botany, ethnopharmacology, phytochemistry, pharmacology and toxicology, thus providing a foundation for future studies. Up to the present day, over 84 compounds, including alkaloids, iridoid glycosides, flavonoid glycosides, triterpenoids, steroids and organic acids, among others, have been isolated and identified from S. nux-vomica. These compounds possess an array of biological activities, including effects on the nervous system, analgesic and anti-inflammatory actions, antitumor effects, inhibition of the growth of pathogenic microorganisms and regulation of immune function. Furthermore, toxicity and detoxification methods are preliminarily discussed toward the end of this review. In further research on S. nux-vomica, bioactivity-guided isolation strategies should be emphasized. Its antitumor effects should be investigated further and in vivo animal experiments should be performed alongside in vitro testing. The pharmacological activity and toxicology of strychnine [Formula: see text]-oxide and brucine [Formula: see text]-oxide should be studied to explore the detoxification mechanism associated with processing more deeply.

scholarly journals Effect and Mechanism of Total Flavonoids Extracted fromCotinus coggygriaagainst Glioblastoma CancerIn VitroandIn Vivo

2015 ◽  
Vol 2015 ◽  
pp. 1-9 ◽  
Author(s):  
Gang Wang ◽  
JunJie Wang ◽  
Li Du ◽  
Fei Li
Keyword(s):  
Cell Proliferation ◽  
Cancer Cells ◽  
Biological Activities ◽  
Therapeutic Modality ◽  
Major Constituent ◽  
Total Flavonoids ◽  
Cancer Cell Proliferation ◽  
Induced Apoptosis ◽  
Cotinus Coggygria

Flavonoids, a major constituent ofCotinus coggygria(CC), have been reported to possess diverse biological activities, including antigenotoxic and hepatoprotective effects; however, few studies have investigated the biological activity of the total flavonoids ofCotinus coggygria, especially in terms of its cytotoxicity in cancer cells. In the present study, theCotinus coggygriaflavonoids (CCF) were extracted fromCotinus coggygriaand characterized by HPLC. These results indicated that CCF extracts could inhibit cell proliferation, with IC50values of 128.49 µg/mL (U87), 107.62 µg/mL (U251), and 93.57 µg/mL (DBTRG-05MG). The current investigation also revealed that CCF induced apoptosis in highly malignant glioblastoma cells, a process that apparently involved the inhibition of Akt coupled with ERK protein expression. This finding suggests that the PI3K/Akt-ERK signaling pathway is regulated by CCF and leads to the inhibition of the glioblastoma cancer cells. Furthermore, a significant antitumor effect of CCF was observed in xenograft animal models of glioblastoma multiformein vivo. Taken together, these data suggest that CCF is the active component in theCotinus coggygriaplant that offers potential therapeutic modality in the abrogation of cancer cell proliferation, including the induction of apoptosis.

scholarly journals Nanoformulation of a Novel Pyrano[2,3-c] Pyrazole Heterocyclic Compound AMDPC Exhibits Anti-Cancer Activity via Blocking the Cell Cycle through a P53-Independent Pathway

Molecules ◽  
2019 ◽  
Vol 24 (3) ◽  
pp. 624 ◽  
Author(s):  
Xuanrong Sun ◽  
Longchao Zhang ◽  
Mengshi Gao ◽  
Xiangjie Que ◽  
Chenfeng Zhou ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Cancer Cells ◽  
Biological Activities ◽  
Polymeric Micelle ◽  
In Vivo Studies ◽  
One Pot ◽  
Anti Cancer ◽  
G2 Phase ◽  
Anti Tumor Activity

Pyrano[2,3-c]pyrazole derivatives have been reported as exerting various biological activities. One compound with potential anti-tumor activity was screened out by MTT assay from series of dihydropyrazopyrazole derivatives we had synthesized before using a one-pot, four-component reaction, and was named as 6-amino-4-(2-hydroxyphenyl)-3-methyl-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile (hereinafter abbreviated as AMDPC). The IC50 of AMDPC against Bcap-37 breast cancer cells was 46.52 μg/mL. Then the hydrophobic AMDPC was encapsulated in PEG-PLGA block copolymers, and then self-assembled as polymeric micelle (mPEG-PLGA/AMDPC) to improve both physiochemical and release profiles. The effect of mPEG-PLGA/AMDPC on BCAP-37 cancer cells showed similar anti-tumor effects as AMDPC. Furthermore, the anti-tumor mechanism of mPEG-PLGA/AMDPC was investigated, which can probably be attributed to stimulating the expression of P21 gene and therefore protein production on BCAP-37 cells, and then blocked the cell cycle through the P53-independent pathway both in S phase and G2 phase. Thus, mPEG-PLGA/AMDPC is a promising therapeutic agent for cancer treatment, and further in vivo studies will be developed.

scholarly journals Cytokine-Induced Guanylate Binding Protein 1 (GBP1) Release from Human Ovarian Cancer Cells

Cancers ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 488
Author(s):  
Grazia Carbotti ◽  
Andrea Petretto ◽  
Elisabeth Naschberger ◽  
Michael Stürzl ◽  
Stefania Martini ◽  
...  
Keyword(s):  
Ovarian Cancer ◽  
Cancer Cells ◽  
Binding Protein ◽  
Biological Activities ◽  
Full Length ◽  
Ovarian Cancer Cells ◽  
Ifn Γ ◽  
Guanylate Binding Protein

We showed that IL-27 shares several effects with IFN-γ in human cancer cells. To identify novel extracellular mediators, potentially involved in epithelial ovarian cancer (EOC) biology, we analyzed the effect of IL-27 or IFN-γ on the secretome of cultured EOC cells by mass-spectrometry (nano-UHPLC-MS/MS). IL-27 and IFN-γ modulate the release of a limited fraction of proteins among those induced in the whole cell. We focused our attention on GBP1, a guanylate-binding protein and GTPase, which mediates several biological activities of IFNs. Cytokine treatment induced GBP1, 2, and 5 expressions in EOC cells, but only GBP1 was secreted. ELISA and immunoblotting showed that cytokine-stimulated EOC cells release full-length GBP1 in vitro, through non-classical pathways, not involving microvesicles. Importantly, full-length GBP1 accumulates in the ascites of most EOC patients and ex-vivo EOC cells show constitutive tyrosine-phosphorylated STAT1/3 proteins and GBP1 expression, supporting a role for Signal Transducer And Activator Of Transcription (STAT)-activating cytokines in vivo. High GBP1 gene expression correlates with better overall survival in the TCGA (The Cancer Genome Atlas) dataset of EOC. In addition, GBP1 transfection partially reduced EOC cell viability in an MTT assay. Our data show for the first time that cytokine-stimulated tumor cells release soluble GBP1 in vitro and in vivo and suggest that GBP1 may have anti-tumor effects in EOC.

scholarly journals Toxicological Evaluation of Piceatannol, Pterostilbene, and ε-Viniferin for Their Potential Use in the Food Industry: A Review

Foods ◽  
2021 ◽  
Vol 10 (3) ◽  
pp. 592
Author(s):  
Concepción Medrano-Padial ◽  
Ana Isabel Prieto ◽  
María Puerto ◽  
Silvia Pichardo
Keyword(s):  
Food Industry ◽  
Biological Activities ◽  
In Vitro Tests ◽  
Toxicological Evaluation ◽  
Cytotoxic Effects ◽  
Cancerous Cell ◽  
Toxicological Studies ◽  
Genotoxicity Testing

The application of stilbenes in the food industry is being considered because of their biological activities. Piceatannol, pterostilbene and ε-viniferin have awakened the industry’s interest. However, before they can be commercialized, we must first guarantee their safety for consumers. The present work reviews the toxicological studies performed with these stilbenes. A wide variety of studies has demonstrated their cytotoxic effects in both cancer and non-cancerous cell lines. In contrast, although DNA damage was detected by some authors, in vitro genotoxic studies on the effects of piceatannol, pterostilbene, and ε-viniferin remain scarce. None of the three reviewed substances have been evaluated using the in vitro tests required by the European Food Safety Authority (EFSA) as the first step in genotoxicity testing. We did not find any study on the toxic effects of these stilbenes in vivo. Thus, more studies are needed to confirm their safe use before they can be authorized as additive in the food industry.

scholarly journals Small Molecule Cjoc42 Improves Chemo-Sensitivity and Increases Levels of Tumor Suppressor Proteins in Hepatoblastoma Cells and in Mice by Inhibiting Oncogene Gankyrin

2021 ◽  
Vol 12 ◽  
Author(s):  
Amber M. D’Souza ◽  
Ashley Cast ◽  
Meenasri Kumbaji ◽  
Maria Rivas ◽  
Ruhi Gulati ◽  
...  
Keyword(s):  
Tumor Suppressor ◽  
Liver Cancer ◽  
Cancer Cells ◽  
Biological Activities ◽  
Tumor Suppressor Proteins ◽  
Pediatric Liver ◽  
Poor Outcomes ◽  
Relapsed Disease ◽  
Different Doses

Objective: Relapsed hepatoblastoma (HBL) and upfront hepatocellular carcinoma (HCC) are notoriously chemoresistant tumors associated with poor outcomes. Gankyrin (Gank) is a known oncogene that is overexpressed in pediatric liver cancer and implicated in chemo-resistance. The goal of this study was to evaluate if the Gank-tumor suppressor axis is activated in chemoresistant hepatoblastoma patients and examine if an inhibitor of Gank, Cjoc42, might improve the chemosensitivity of cancer cells.Methods: Expression of Gank and its downstream targets were examined in fresh human HBL samples using immunostaining, QRT-PCR, and Western Blot. Cancer cells, Huh6 (human HBL) and Hepa1c1c7 (mouse HCC) were treated with Cjoc42 and with Cjoc42 in combination with cisplatin or doxorubicin. Cell proliferation, apoptosis, and chemoresistance were examined. To examine activities of Cjoc42 in vivo, mice were treated with different doses of Cjoc42, and biological activities of Gank and cytotoxicity of Cjoc42 were tested.Results: Elevation of Gank and Gank-mediated elimination of TSPs are observed in patients with minimal necrosis after chemotherapy and relapsed disease. The treatment of Huh6 and Hepa1c1c7 with Cjoc42 was not cytotoxic; however, in combination with cisplatin or doxorubicin, Cjoc42 caused a significant increase in cytotoxicity compared to chemotherapy alone with increased apoptosis. Examination of Cjoc42 in WT mice showed that Cjoc42 is well tolerated without systemic toxicity, and levels of tumor suppressors CUGBP1, Rb, p53, C/EBPα, and HNF4α are increased by blocking their Gank-dependent degradation.Conclusions: Our work shows that Cjoc42 might be a promising adjunct to chemotherapy for the treatment of severe pediatric liver cancer and presents mechanisms by which Cjoc42 increases chemo-sensitivity.

Preparation and Dosimetry Assessment of 166Dy2O3/166Ho2O3-iPSMA Nanoparticles for Targeted Hepatocarcinoma Radiotherapy

2021 ◽  
Vol 21 (11) ◽  
pp. 5449-5458
Author(s):  
Omar Canseco-Hernández ◽  
Guillermina Ferro-Flores ◽  
Nallely Jimenez-Mancilla ◽  
Liliana Aranda-Lara ◽  
Blanca Ocampo-Garcia ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Absorbed Dose ◽  
Radiation Doses ◽  
Cell Nuclei ◽  
High Radiation ◽  
Cytotoxic Effects ◽  
Transmission Electron ◽  
Specific Membrane

This research aimed to prepare 166Dy2O3-iPSMA/166Ho2O3-iPSMA nanoparticles (166Dy2O3/166Ho2O3-iPSMA NPs) and assess the radiation absorbed dose produced by the nanosystem to hepatic cancer cells by using experimental in vitro and in vivo biokinetic data. Dy2O3NPs were synthesized and functionalized with the prostate-specific membrane antigen inhibitor peptide (iPSMA). Fourier transform infrared (FTIR) spectroscopy, transmission electron microscope (TEM), dynamic light scattering (DSL) and zeta potential analyses indicated the formation of Dy2O3-iPSMA NPs (46.11 ± 13.24 nm). After neutron activation, a stable 166Dy2O3/166Ho2O3- iPSMA nanosystem was obtained, which showed adequate affinity to the PSMA receptor in HepG2 cancer cells (Kd = 9.87 ± 2.27 nM). in vitro studies indicated high 166Dy2O3/166Ho2O3-iPSMA internalization in cancer cells, with high radiation doses to cell nuclei (107 Gy) and cytotoxic effects, resulting in a significant reduction in HepG2 cell viability (decreasing to 2.12 ± 0.31%). After intratumoral administration in mice, the nanosystem biokinetic profile indicated significant retention into the tumoral mass, producing ablative radiation doses (>70 Gy).

scholarly journals A 3D Heterotypic Multicellular Tumor Spheroid Assay Platform to Discriminate Drug Effects on Stroma versus Cancer Cells

2019 ◽  
Vol 25 (3) ◽  
pp. 265-276
Author(s):  
Zoe Weydert ◽  
Madhu Lal-Nag ◽  
Lesley Mathews-Greiner ◽  
Christoph Thiel ◽  
Henrik Cordes ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Stromal Cells ◽  
High Throughput Screening ◽  
Drug Testing ◽  
Therapeutic Window ◽  
Multicellular Tumor Spheroid ◽  
Cytotoxic Effects ◽  
Primary Tumors

Three-dimensional (3D) cell culture models are thought to mimic the physiological and pharmacological properties of tissues in vivo more accurately than two-dimensional cultures on plastic dishes. For the development of cancer therapies, 3D spheroid models are being created to reflect the complex histology and physiology of primary tumors with the hopes that drug responses will be more similar to and as predictive as those obtained in vivo. The effect of additional cell types in tumors, such as stromal cells, and the resulting heterotypic cell–cell crosstalk can be investigated in these heterotypic 3D cell cultures. Here, a high-throughput screening-compatible drug testing platform based on 3D multicellular spheroid models is described that enables the parallel assessment of toxicity on stromal cells and efficacy on cancer cells by drug candidates. These heterotypic microtissue tumor models incorporate NIH3T3 fibroblasts as stromal cells that are engineered with a reporter gene encoding secreted NanoLUC luciferase. By tracking the NanoLUC signal in the media over time, a time-related measurement of the cytotoxic effects of drugs on stromal cells over the cancer cells was possible, thus enabling the identification of a therapeutic window. An in vitro therapeutic index parameter is proposed to help distinguish and classify those compounds with broad cytotoxic effects versus those that are more selective at targeting cancer cells.

scholarly journals Promising Anticancer Activities of Alismatis rhizome and Its Triterpenes via p38 and PI3K/Akt/mTOR Signaling Pathways

Nutrients ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 2455
Author(s):  
Eungyeong Jang ◽  
Jang-Hoon Lee
Keyword(s):  
Cancer Cells ◽  
Signaling Pathways ◽  
Biological Activities ◽  
Experimental Models ◽  
Mtor Signaling ◽  
Flowering Plant ◽  
In Vivo Studies ◽  
Anticancer Activities

The flowering plant genus Alisma, which belongs to the family Alismataceae, comprises 11 species, including Alisma orientale, Alisma canaliculatum, and Alisma plantago-aquatica. Alismatis rhizome (Ze xie in Chinese, Takusha in Japanese, and Taeksa in Korean, AR), the tubers of medicinal plants from Alisma species, have long been used to treat inflammatory diseases, hyperlipidemia, diabetes, bacterial infection, edema, oliguria, diarrhea, and dizziness. Recent evidence has demonstrated that its extract showed pharmacological activities to effectively reverse cancer-related molecular targets. In particular, triterpenes naturally isolated from AR have been found to exhibit antitumor activity. This study aimed to describe the biological activities and plausible signaling cascades of AR and its main compounds in experimental models representing cancer-related physiology and pathology. Available in vitro and in vivo studies revealed that AR extract possesses anticancer activity against various cancer cells, and the efficacy might be attributed to the cytotoxic and antimetastatic effects of its alisol compounds, such as alisol A, alisol B, and alisol B 23-acetate. Several beneficial functions of triterpenoids found in AR might be due to p38 activation and inhibition of the phosphatidylinositol 3-kinase (PI3K)/protein kinase B (Akt)/mammalian target of rapamycin (mTOR) signaling pathways. Moreover, AR and its triterpenes inhibit the proliferation of cancer cells that are resistant to chemotherapy. Thus, AR and its triterpenes may play potential roles in tumor attack, as well as a therapeutic remedy alone and in combination with other chemotherapeutic drugs.

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