scholarly journals An overview of the potential anticancer properties of cardamonin

2020 ◽  
Vol 1 (6) ◽  
Author(s):  
Shanaya Ramchandani ◽  
Irum Naz ◽  
Namrata Dhudha ◽  
Manoj Garg
Keyword(s):  
Anticancer Agent ◽  
Human Cancer ◽  
Model Systems ◽  
Preclinical Model ◽  
Cancer Treatments ◽  
Human Cancer Cell Lines ◽  
Anticancer Properties ◽  
Natural Medicine

Cancer is one of the leading causes of mortality, contributing to 9.6 million deaths globally in 2018 alone. Although several cancer treatments exist, they are often associated with severe side effects and high toxicities, leaving room for significant advancements to be made in the field. In recent years, several phytochemicals from plants and natural bioresources have been extracted and tested against various human malignancies using both in vitro and in vivo preclinical model systems. Cardamonin, a chalcone extracted from the Alpinia species, is an example of a natural therapeutic agent that has anti-cancer and anti-inflammatory effects against human cancer cell lines, including breast, lung, colon, and gastric, in both in vitro culture systems as well as xenograft mouse models. Earlier, cardamonin was used as a natural medicine against stomach related issues, diarrhea, insulin resistance, nephroprotection against cisplatin treatment, vasorelaxant and antinociceptive. The compound is well-known to inhibit proliferation, migration, invasion, and induce apoptosis, through the involvement of Wnt/β-catenin, NF-κB, and PI3K/Akt pathways. The good biosafety and pharmacokinetic profiling of cardamonin satisfy it as an attractive molecule for the development of an anticancer agent. The present review has summarized the chemo-preventive ability of cardamonin as an anticancer agent against numerous human malignancies.

Vitamin D as potential therapeutic anticancer agent

2018 ◽  
pp. 1-3
Keyword(s):  
Vitamin D ◽  
Anticancer Activity ◽  
Anticancer Agent ◽  
Antitumor Agents ◽  
Metastatic Potential ◽  
Anticancer Properties ◽  
Chemotherapy Agents

The role of vitamin D is implicated in carcinogenesis through numerous biological processes like induction of apoptosis, modulation of immune system inhibition of inflammation and cell proliferation and promotion of cell differentiation. Its use as additional adjuvant drug with cancer treatment may be novel combination for improved outcome of different cancers. Numerous preclinical, epidemiological and clinical studies support the role of vitamin D as an anticancer agent. Anticancer properties of vitamin D have been studied widely (both in vivo and in vitro) among various cancers and found to have promising results. There are considerable data that indicate synergistic potential of calcitriol and antitumor agents. Possible mechanisms for modulatory anticancer activity of vitamin D include its antiproliferative, prodifferentiating, and anti-angiogenic and apoptic properties. Calcitriol reduces invasiveness and metastatic potential of many cancer cells by inhibiting angiogenesis and regulating expression of the key molecules involved in invasion and metastasis. Anticancer activity of vitamin D is synergistic or additive with the antineoplastic actions of several drugs including cytotoxic chemotherapy agents like paclitaxel, docetaxel, platinum base compounds and mitoxantrone. Benefits of addition of vitamin D should be weighed against the risk of its toxicity.

scholarly journals Pseudomonas aeruginosa-mannose-sensitive hemagglutinin inhibits chemical-induced skin cancer through suppressing hedgehog signaling

2020 ◽  
Vol 245 (3) ◽  
pp. 213-220
Author(s):  
Dianhui Xiu ◽  
Min Cheng ◽  
Wenlei Zhang ◽  
Xibo Ma ◽  
Lin Liu
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Skin Cancer ◽  
Hedgehog Signaling ◽  
Anticancer Agent ◽  
Epithelial Mesenchymal Transition ◽  
Cell Counting ◽  
Mesenchymal Transition ◽  
Anticancer Properties

Pseudomonas aeruginosa-mannose-sensitive hemagglutinin (PAM) is an inactivate P. aeruginosa with mannose-sensitive hemagglutinin. Recently, the anticancer properties of PAM against many cancers have been reported across a range of studies. However, the exact mechanism through which PAM prevents skin cancer remains unclear. The aim of this study is to show to what extent PAM could inhibit the dimethylbenzanthracene (DMBA)/12-O-tetradecanoylphorbol-13-acetate (TPA)-induced skin cancer. JB6 cells were treated by TPA so as to establish an in vitro model. The effects of PAM on proliferation of the cells were analyzed using cell counting kit-8 assays. Effects on epithelial–mesenchymal transition (EMT) were assayed by real-time PCR and Western blotting. A DMBA/TPA-induced skin cancer mouse model was also established. The results showed that TPA promoted EMT changes through the activation of the hedgehog (Hh) pathway, which was reversed by PAM. Moreover, PAM inhibited the cancer growth and Hh pathway in vivo. These data indicate that PAM may serve as a potential anticancer agent for the treatment of skin cancer. Impact statement Pseudomonas aeruginosa-mannose-sensitive hemagglutinin (PAM) restrained the chemical-induced skin cancer cells in vitro and in vivo partly through suppressing the Hh signaling pathway, indicating that PAM may be a promising anticancer agent for treating skin cancer.

scholarly journals A newfangled coordinated ruthenium phloretin complex reprogramming breast cancer microenvironment interceded by modulation of PI3K/Akt/mTOR/VEGF pathway and modifying the antioxidant status correlated with intensified apoptotic events.

2020 ◽  
Author(s):  
Chenyang He ◽  
Guo Yu ◽  
Anil Kumar Mondru ◽  
Tania Chakraborty ◽  
Souvik Roy
Keyword(s):  
Breast Carcinoma ◽  
Cell Lines ◽  
Human Cancer ◽  
In Vivo Model ◽  
Human Cancer Cell Lines ◽  
Vegf Pathway ◽  
Breast Carcinoma Cell Lines ◽  
Mcf 7

Abstract Background: Our recent investigation directed to synthesize and characterize a novel ruthenium– phloretin complex accompanied by the study of antioxidant in addition to DNA binding capabilities, and to determine the chemotherapeutic activity against breast carcinoma in vitro and in vivo approach.Methods: Ruthenium–phloretin complex was synthesized and characterized using various spectroscopic methods. The complex was further investigated to determine its efficacy in both MCF-7 and MDA-MB-231 human cancer cell lines and finally in an in vivo model of DMBA induced mammary carcinogenesis in ratsResults: Our studies confirm that the chelation of the metal and ligand was materialize by the 3-OH and 9-OH functional groups of the ligand and the complex is found crystalline and was capable of intercalating with CT-DNA. The complex was capable of reducing cellular propagation and initiate apoptotic events in MCF-7 and MDA-MB-231 breast carcinoma cell lines. Additionally, ruthenium-phloretin complex could modulate p53 intervene apoptosis in the breast carcinoma, initiated by the intrinsic apoptotic trail facilitated by the Bcl2 and Bax and at the same time down regulating the PI3K/Akt/mTOR pathway coupled with MMP9 regulated tumor invasive pathways.Conclusions: Ruthenium-phloretin chemotherapy could interrupt, revoke or suspend the succession of breast carcinoma by altering intrinsic apoptosis along with the antiangiogenic pathway, hence fulfilling the role of a prospective candidate in cancer chemotherapeutics in the in the near future.

scholarly journals A Newfangled Coordinated Ruthenium Phloretin Complex Reprogramming Breast Cancer Microenvironment Interceded by Modulation of PI3K/Akt/Mtor/VEGF Pathway and Modifying The Antioxidant Status Correlated With Intensified Apoptotic Events.

2020 ◽  
Author(s):  
Chenyang He ◽  
Junli Wang ◽  
Tania Chakraborty ◽  
Souvik Roy
Keyword(s):  
Breast Carcinoma ◽  
Cell Lines ◽  
Human Cancer ◽  
In Vivo Model ◽  
Human Cancer Cell Lines ◽  
Vegf Pathway ◽  
Breast Carcinoma Cell Lines ◽  
Mcf 7

Abstract Background: Our recent investigation directed to synthesize and characterize a novel ruthenium– phloretin complex accompanied by the study of antioxidant in addition to DNA binding capabilities, and to determine the chemotherapeutic activity against breast carcinoma in vitro and in vivo approach.Methods: Ruthenium–phloretin complex was synthesized and characterized using various spectroscopic methods. The complex was further investigated to determine its efficacy in both MCF-7 and MDA-MB-231 human cancer cell lines and finally in an in vivo model of DMBA induced mammary carcinogenesis in ratsResults: Our studies confirm that the chelation of the metal and ligand was materialize by the 3-OH and 9-OH functional groups of the ligand and the complex is found crystalline and was capable of intercalating with CT-DNA. The complex was capable of reducing cellular propagation and initiate apoptotic events in MCF-7 and MDA-MB-231 breast carcinoma cell lines. Additionally, ruthenium-phloretin complex could modulate p53 intervene apoptosis in the breast carcinoma, initiated by the intrinsic apoptotic trail facilitated by the Bcl2 and Bax and at the same time down regulating the PI3K/Akt/mTOR pathway coupled with MMP9 regulated tumor invasive pathways.Conclusions: Ruthenium-phloretin chemotherapy could interrupt, revoke or suspend the succession of breast carcinoma by altering intrinsic apoptosis along with the antiangiogenic pathway, hence fulfilling the role of a prospective candidate in cancer chemotherapeutics in the in the near future.

scholarly journals Full Structural Characterization of Homoleptic Complexes of Diacetylcurcumin with Mg, Zn, Cu, and Mn: Cisplatin-level Cytotoxicity in Vitro with Minimal Acute Toxicity in Vivo

Molecules ◽  
2019 ◽  
Vol 24 (8) ◽  
pp. 1598 ◽  
Author(s):  
William Meza-Morales ◽  
M. Mirian Estévez-Carmona ◽  
Yair Alvarez-Ricardo ◽  
Marco A. Obregón-Mendoza ◽  
Julia Cassani ◽  
...  
Keyword(s):  
Acute Toxicity ◽  
Metal Complexes ◽  
Single Crystal ◽  
Cytotoxic Activity ◽  
Therapeutic Potential ◽  
Human Cancer ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines

At the present time, scientists place a great deal of effort worldwide trying to improve the therapeutic potential of metal complexes of curcumin and curcuminoids. Herein, the synthesis of four homoleptic metal complexes with diacetylcurcumin (DAC), using a ligand designed to prevent the interaction of phenolic groups, rendering metal complexes through the β-diketone functionality, is reported. Due to their physiological relevance, we used bivalent magnesium, zinc, copper, and manganese for complexation with DAC. The resulting products were characterized by ultraviolet-visible (UV-Vis), fluorescence spectroscopy, infrared spectroscopy (IR), liquid and solid-state nuclear magnetic resonance (NMR), electron paramagnetic resonance (EPR), magnetic moment, mass spectrometry (MS), single crystal, and powder X-ray diffraction (SCXRD and PXRD). Crystallization was achieved in dimethylsulfoxide (DMSO) or N,N-dimethylformamide (DMF) as triclinic systems with space group P-1, showing the metal bound to the β-diketone function, while the 1H-NMR confirmed the preference of the enolic form of the ligand. Single crystal data demonstrated a 1:2 metal:ligand ratio. The inhibition of lipid peroxidation was evaluated using the thiobarbituric acid reactive substance assay (TBARS). All four metal complexes (Mg, Zn, Cu, and Mn) exhibited good antioxidant effect (IC50 = 2.03 ± 0.27, 1.58 ± 0.07, 1.58 ± 0.15 and 1.24 ± 0.10 μM respectively) compared with butylated hydroxytoluene (BHT) and α-tocopherol. The cytotoxic activity in human cancer cell lines against colon adenocarcinoma (HCT-15), mammary adenocarcinoma (MCF-7), and lung adenocarcinoma (SKLU-1) was found comparable ((DAC)2Mg), or ca. 2-fold higher ((DAC)2Zn) than cisplatin. The acute toxicity assays indicate class 5 toxicity, according to the Organization for Economic Co-operation and Development (OECD) guidelines at doses of 3 g/kg for all complexes. No mortality or changes in the behavior of animals in any of the treated groups was observed. A therapeutic potential can be envisaged from the relevant cytotoxic activity upon human cancer cell lines in vitro and the undetected in vivo acute toxicity of these compounds.

Prothymosin α and Its C-Terminal Immunoreactive Decapeptide Show no Evidence of Acute Toxicity: A Preliminary in Silico, in Vitro and in Vivo Investigation

2021 ◽  
Vol 28 ◽  
Author(s):  
Anastasios I. Birmpilis ◽  
Panagiotis Vitsos ◽  
Ioannis V. Kostopoulos ◽  
Lillian Williams ◽  
Kyriaki Ioannou ◽  
...  
Keyword(s):  
Acute Toxicity ◽  
In Silico ◽  
Human Cancer ◽  
Cell Cycle Distribution ◽  
Human Cancer Cell Lines ◽  
Prothymosin Α ◽  
High Concentrations ◽  
Immunocompetent Mice

Background: Members of the α-thymosin family have long been studied for their immunostimulating properties. Among them, the danger-associated molecular patterns (DAMPs) prothymosin α (proTα) and its C-terminal decapeptide proTα(100–109) have been shown to act as immunomodulators in vitro, due to their ability to promote T helper type 1 (Th1) responses. Recently, we verified these findings in vivo, showing that both proTα and proTα(100-109) enhance antitumor-reactive T cell-mediated responses. Methods: In view of the eventual use of proTα and proTα(100-109) in humans, we investigated their safety profile in silico, in human leukocytes and cancer cells lines in vitro, and in immunocompetent mice in vivo, in comparison to the proTα derivative thymosin alpha 1 (Τα1), a 28-mer peptide extensively studied for its safety in clinical trials. Results: In silico prediction via computational tools showed that all three peptide sequences likely are non-toxic or do not induce allergic regions. In vitro, proTα, proTα(100-109) and Tα1 did not affect the viability of human cancer cell lines and healthy donor-derived leukocytes, did not promote apoptosis or alter cell cycle distribution. Furthermore, mice injected with proTα, proTα(100-109) and Tα1 at doses equivalent to the suggested dose regimen of Tα1 in humans, did not show signs of acute toxicity, whereas proTα and proTα(100-109) increased the levels of proinflammatory and Th1-type cytokines in their peripheral blood. Conclusion: Our preliminary findings suggest that proTα and proTα(100-109), even at high concentrations, are non-toxic in vitro and in an acute toxicity model in vivo; moreover, we show that the two peptides retain their immunomodulatory properties in vivo and, eventually, could be considered for therapeutic use in humans.

scholarly journals Eleucine indicaPossesses Antioxidant, Antibacterial and Cytotoxic Properties

2011 ◽  
Vol 2011 ◽  
pp. 1-6 ◽  
Author(s):  
Adel S. Al-Zubairi ◽  
Ahmad Bustamam Abdul ◽  
Siddig Ibrahim Abdelwahab ◽  
Chew Yuan Peng ◽  
Syam Mohan ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Human Cancer ◽  
Antioxidant Properties ◽  
Antibacterial Properties ◽  
Diffusion Method ◽  
Total Phenolic ◽  
Significant Activity ◽  
Human Cancer Cell Lines

The use of evidence-based complementary and alternative medicine is increasing rapidly.Eleucine indica(EI) is traditionally used in ailments associated with liver and kidneys. The therapeutic benefit of the medicinal plants is often attributed to their antioxidant properties. Therefore, the aim of this study was to screen the hexane, dicholoromethane, ethyl acetate (EA) and methanol extracts (MeTH) of EI for their antioxidant, antibacterial and anti-cancer effects using total phenolic contents (TPCs) and DPPH, disc diffusion method and MTT cytotoxicity assays, respectively. The MeTH was showed to have the highest TPC and scavenging activity (77.7%) on DPPH assay, followed by EA (64.5%), hexane (47.19%) and DCM (40.83%) extracts, whereas the MeTH showed no inhibitory effect on all tested bacteria strains. However, the EA extract exhibited a broad spectrum antibacterial activity against all tested bacteria exceptBacillus subtilis, in which this bacterium was found to be resistant to all EI extracts. Meanwhile, hexane extract was demonstrated to have a remarkable antibacterial activity against methicillin resistantStaphylococcus aureus(MRSA) andPseudomonas aeruginosa, while the dicholoromethane extract did not exhibit significant activity againstP. aeruginosa. None of the extracts showed significant cytotoxic activity towards MCF-7, HT-29 and CEM-SS human cancer cell lines after 72 h incubation time (IC50> 30 μg/ml). These results demonstrate that the extract prepared from the EI possesses antioxidant activityin vitroin addition to antibacterial properties. Further investigations are needed to verify the antioxidant effectsin vitroandin vivo.

scholarly journals Cannabinoid Quinones—A Review and Novel Observations

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1761
Author(s):  
Natalya M. Kogan ◽  
Maximilian Peters ◽  
Raphael Mechoulam
Keyword(s):  
Human Cancer ◽  
Mechanisms Of Action ◽  
High Efficacy ◽  
Topoisomerase Iiα ◽  
Human Cancer Cell Lines ◽  
Structure Activity ◽  
Related Compounds ◽  
Very High

A cannabinoid anticancer para-quinone, HU-331, which was synthesized by our group five decades ago, was shown to have very high efficacy against human cancer cell lines in-vitro and against in-vivo grafts of human tumors in nude mice. The main mechanism was topoisomerase IIα catalytic inhibition. Later, several groups synthesized related compounds. In the present presentation, we review the publications on compounds synthesized on the basis of HU-331, summarize their published activities and mechanisms of action and report the synthesis and action of novel quinones, thus expanding the structure-activity relationship in these series.

scholarly journals IN VITRO CYTOTOXIC ANTICANCER POTENTIAL OF BIOACTIVE FRACTION ISOLATED FROM INDONESIAN TIDAL SPONGE CALTHROPELLA SP.

2019 ◽  
Vol 12 (1) ◽  
pp. 380
Author(s):  
Fitria Susilowati ◽  
Respati Tri Swasono ◽  
Tatsufumi Okino ◽  
Winarto Haryadi
Keyword(s):  
High Resolution ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Bioactive Compounds ◽  
Human Cancer ◽  
Human Cancer Cell Lines ◽  
Anticancer Properties ◽  
Bioactive Fraction ◽  
Mcf 7

Objective: This study was taken to examine the cytotoxicity of the bioactive fraction isolated from marine sponge Calthropella sp. as a preliminary anticancer assay and identify its bioactive compounds.Methods: The cytotoxic activity was assessed by 3-(4,5-dimethylthiazol-2-y1)-2,5-diphenyltetrazolium bromide assay against three human cancer cell lines, namely human breast (MCF-7), human lung (H-460), and human liver (HepG-2). The bioactive compounds were identified using a high-resolution liquid chromatography–mass spectroscopy (LC–MS).Results: The active fraction 7 showed moderate to strong cytotoxic activity on all cell lines tested and promising a strong potent cytotoxicity against MCF-7 cell lines with IC50 value as low as 1.925 μg/mL comparable to control, cisplatin (IC50 0.977 μg/mL). In regard to the promising bioactive compounds, the high-resolution LC–MS predicted the existing of several known compounds such as bengamide Q, clavepictine A, 4’-N-methyl-5’- hydroxystaurosporine, carteriofenone A, and one strong possibility of a new compound.Conclusion: This study has revealed that the isolated bioactive fraction of Indonesian tidal sponge, Calthropella sp., possesses potential anticancer properties with a promising significant cytotoxicity on MCF-7 cell lines (IC50 1.925 μg/mL).

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