Amygdalin: Toxicity, Anticancer Activity and Analytical Procedures for Its Determination in Plant Seeds

Amygdalin (d-Mandelonitrile 6-O-β-d-glucosido-β-d-glucoside) is a natural cyanogenic glycoside occurring in the seeds of some edible plants, such as bitter almonds and peaches. It is a medically interesting but controversial compound as it has anticancer activity on one hand and can be toxic via enzymatic degradation and production of hydrogen cyanide on the other hand. Despite numerous contributions on cancer cell lines, the clinical evidence for the anticancer activity of amygdalin is not fully confirmed. Moreover, high dose exposures to amygdalin can produce cyanide toxicity. The aim of this review is to present the current state of knowledge on the sources, toxicity and anticancer properties of amygdalin, and analytical methods for its determination in plant seeds.

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Vitamin D as potential therapeutic anticancer agent

Journal of Cancer Science and Therapeutics ◽

10.36879/jcst.19.000106 ◽

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.

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Design of Lamivudine Loaded Nanoparticles for Oral Application by Nano Spray Drying Method: A New Approach to use an Antiretroviral Drug for Lung Cancer Treatment

Combinatorial Chemistry & High Throughput Screening ◽

10.2174/1386207323666200325155020 ◽

2020 ◽

Vol 23 (10) ◽

pp. 1064-1079

Author(s):

Ahmet Alper Öztürk ◽

İrem Namlı ◽

Kadri Güleç ◽

Şennur Görgülü

Keyword(s):

Lung Cancer ◽

Cancer Treatment ◽

Anticancer Activity ◽

Cell Line ◽

Anticancer Drugs ◽

Release Kinetics ◽

Prolonged Release ◽

Lung Cancer Treatment ◽

Anticancer Properties ◽

Ft Ir

Aims: To prepare lamivudine (LAM)-loaded-nanoparticles (NPs) that can be used in lung cancer treatment. To change the antiviral indication of LAM to anticancer. Background: The development of anticancer drugs is a difficult process. One approach to accelerate the availability of drugs is to reclassify drugs approved for other conditions as anticancer. The most common route of administration of anticancer drugs is intravenous injection. Oral administration of anticancer drugs may considerably change current treatment modalities of chemotherapy and improve the life quality of cancer patients. There is also a potentially significant economic advantage. Objective: To characterize the LAM-loaded-NPs and examine the anticancer activity. Methods: LAM-loaded-NPs were prepared using Nano Spray-Dryer. Properties of NPs were elucidated by particle size (PS), polydispersity index (PDI), zeta potential (ZP), SEM, encapsulation efficiency (EE%), dissolution, release kinetics, DSC and FT-IR. Then, the anticancer activity of all NPs was examined. Results: The PS values of the LAM-loaded-NPs were between 373 and 486 nm. All NPs prepared have spherical structure and positive ZP. EE% was in a range of 61-79%. NPs showed prolonged release and the release kinetics fitted to the Weibull model. NPs structures were clarified by DSC and FT-IR analysis. The results showed that the properties of NPs were directly related to the drug:polymer ratio of feed solution. NPs have potential anticancer properties against A549 cell line at low concentrations and non-toxic to CCD 19-Lu cell line. Conclusion: NPs have potential anticancer properties against human lung adenocarcinoma cells and may induce cell death effectively and be a potent modality to treat this type of cancer. These experiments also indicate that our formulations are non-toxic to normal cells. It is clear that this study would bring a new perspective to cancer therapy.

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Anticancer Activity of Triazolo-Thiadiazole Derivatives and Inhibition of AKT1 and AKT2 Activation

Pharmaceutics ◽

10.3390/pharmaceutics13040493 ◽

2021 ◽

Vol 13 (4) ◽

pp. 493

Author(s):

Dimitrios T. Trafalis ◽

Sofia Sagredou ◽

Panayiotis Dalezis ◽

Maria Voura ◽

Stella Fountoulaki ◽

...

Keyword(s):

Anticancer Activity ◽

Human Colon ◽

Tumor Xenograft ◽

Atp Binding Site ◽

Anticancer Properties ◽

Extensive Range ◽

Dependent Inhibition ◽

Ht 29

The fusion of 1,2,4-triazole and 1,3,4-thiadiazole rings results in a class of heterocycles compounds with an extensive range of pharmacological properties. A series of 1,2,4-triazolo[3,4-b]-1,2,4-thiadiazoles was synthesized and tested for its enzyme inhibition potential and anticancer activity. The results show that 1,2,4-triazolo[3,4-b]-1,2,4-thiadiazoles display potent anticancer properties in vitro against a panel of cancer cells and in vivo efficacy in HT-29 human colon tumor xenograft in CB17 severe combined immunodeficient (SCID) mice. Preliminary mechanistic studies revealed that KA25 and KA39 exhibit time- and concentration-dependent inhibition of Akt Ser-473 phosphorylation. Molecular modeling experiments indicated that 1,2,4-triazolo[3,4-b]-1,2,4-thiadiazoles bind well to the ATP binding site in Akt1 and Akt2. The low acute toxicity combined with in vitro and in vivo anticancer activity render triazolo[3,4-b]thiadiazoles KA25, KA26, and KA39 promising cancer therapeutic agents.

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A Nitrocarbazole as a New Microtubule-Targeting Agent in Breast Cancer Treatment

Applied Sciences ◽

10.3390/app11199139 ◽

2021 ◽

Vol 11 (19) ◽

pp. 9139

Author(s):

Maria Stefania Sinicropi ◽

Cinzia Tavani ◽

Camillo Rosano ◽

Jessica Ceramella ◽

Domenico Iacopetta ◽

...

Keyword(s):

Breast Cancer ◽

Anticancer Activity ◽

Breast Cancer Cell Lines ◽

Cellular Functions ◽

Anticancer Properties ◽

Cycle Arrest ◽

In Silico Studies ◽

Ic50 Values ◽

Mcf 7

Breast cancer is still considered a high-incidence disease, and numerous are the research efforts for the development of new useful and effective therapies. Among anticancer drugs, carbazole compounds are largely studied for their anticancer properties and their ability to interfere with specific targets, such as microtubule components. The latter are involved in vital cellular functions, and the perturbation of their dynamics leads to cell cycle arrest and subsequent apoptosis. In this context, we report the anticancer activity of a series of carbazole analogues 1–8. Among them, 2-nitrocarbazole 1 exhibited the best cytotoxic profile, showing good anticancer activity against two breast cancer cell lines, namely MCF-7 and MDA-MB-231, with IC50 values of 7 ± 1.0 and 11.6 ± 0.8 μM, respectively. Furthermore, compound 1 did not interfere with the growth of the normal cell line MCF-10A, contrarily to Ellipticine, a well-known carbazole derivative used as a reference molecule. Finally, in vitro immunofluorescence analysis and in silico studies allowed us to demonstrate the ability of compound 1 to interfere with tubulin organization, similarly to vinblastine: a feature that results in triggering MCF-7 cell death by apoptosis, as demonstrated using a TUNEL assay.

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In vitro anticancer activity of Astaxanthin

World Journal of Biology Pharmacy and Health Sciences ◽

10.30574/wjbphs.2021.5.3.0110 ◽

2021 ◽

Vol 5 (3) ◽

pp. 033-037

Author(s):

Uma Nath U ◽

Ravi. R ◽

Sundara Ganapathy ◽

Lal Prasanth

Keyword(s):

Anticancer Activity ◽

Tumor Volume ◽

Hematological Parameters ◽

Ehrlich Ascites Carcinoma ◽

High Dose ◽

Ehrlich Ascites ◽

Shrimp Shell ◽

Shrimp Shell Waste ◽

Wbc Count

This study was designed to determine the in vitro anticancer potential of the Astaxanthin isolated from shrimp shell waste (ETC) against Ehrlich Ascites Carcinoma (EAC) induced cancer in swiss albino mice. The anticancer activity was assessed using in vitro cytotoxicAity, mean survival time, tumor volume and hematological studies. The reliable criteria for evaluating the potential of any anticancer agent is the prolongation of lifespan of the animal and decrease in WBC count of blood. The high dose of ETC (200 mg/kg, orally) significantly reduced the tumor growth which was demonstrated by increased lifespan of the mice and restoration of hematological parameters. ETC was also found to be cytotoxic in the in vitro parameter which shows that ETC possesses significant anticancer potential.

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In-Vitro Antioxidant, Antibacterial and Anticancer properties of Leaf Extract Annona Muricata

International Journal of Advanced Science and Engineering ◽

10.29294/ijase.8.1.2021.2119-2126 ◽

2021 ◽

Vol 8 (1) ◽

Keyword(s):

Antioxidant Activity ◽

Anticancer Activity ◽

Antioxidant Activities ◽

Extraction Procedure ◽

Radical Scavenging ◽

Antibacterial Activities ◽

Diffusion Method ◽

Annona Muricata ◽

Anticancer Properties

Annona muricata is one of the important herbal plant that are widely used to treat antidiabetic, anti-inflammatory, insecticidal, antimalarial, anticancer, antibacterial and antioxidant activities. In the present study, extraction procedure was carried out in few step processes method. The extract contains high percentage of steroid, alkaloid, flavonoid, phenolic and saponin. The extract was used to study the antioxidant activity; antibacterial activities and anticancer activity by standard methods. The antioxidant activity was studied by using radical scavenging DPPH, FRAP and H2O2 method and disc diffusion method. The results of antibacterial activity of the following bacteria’s such as Pseudomonas, Staphylococcus, Bacillus, E.coli shows the maximum zone of inhibition against Staphylococcus aureus which is around 1.7 cm. The anticancer activity was carried out by MTT assay using Hep-G2 as cell line and results are reported in the paper.

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High-dose vitamin C enhances cancer immunotherapy

Science Translational Medicine ◽

10.1126/scitranslmed.aay8707 ◽

2020 ◽

Vol 12 (532) ◽

pp. eaay8707 ◽

Cited By ~ 17

Author(s):

Alessandro Magrì ◽

Giovanni Germano ◽

Annalisa Lorenzato ◽

Simona Lamba ◽

Rosaria Chilà ◽

...

Keyword(s):

Immune System ◽

Vitamin C ◽

Clinical Evidence ◽

High Dose ◽

Dependent Manner ◽

Cancer Cell Growth ◽

Mutational Burden ◽

Cancer Types ◽

High Doses ◽

High Dose Vitamin

Vitamin C (VitC) is known to directly impair cancer cell growth in preclinical models, but there is little clinical evidence on its antitumoral efficacy. In addition, whether and how VitC modulates anticancer immune responses is mostly unknown. Here, we show that a fully competent immune system is required to maximize the antiproliferative effect of VitC in breast, colorectal, melanoma, and pancreatic murine tumors. High-dose VitC modulates infiltration of the tumor microenvironment by cells of the immune system and delays cancer growth in a T cell–dependent manner. VitC not only enhances the cytotoxic activity of adoptively transferred CD8 T cells but also cooperates with immune checkpoint therapy (ICT) in several cancer types. Combination of VitC and ICT can be curative in models of mismatch repair–deficient tumors with high mutational burden. This work provides a rationale for clinical trials combining ICT with high doses of VitC.

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Selenium Anticancer Properties and Impact on Cellular Redox Status

Antioxidants ◽

10.3390/antiox9010080 ◽

2020 ◽

Vol 9 (1) ◽

pp. 80 ◽

Cited By ~ 6

Author(s):

Lolita Kuršvietienė ◽

Aušra Mongirdienė ◽

Jurga Bernatonienė ◽

Jurgita Šulinskienė ◽

Inga Stanevičienė

Keyword(s):

Anticancer Activity ◽

Antioxidant Activities ◽

Chemotherapeutic Agents ◽

Redox Activity ◽

Biological Functions ◽

Cellular Redox ◽

Selenium Compounds ◽

Anticancer Properties ◽

Redox Active ◽

The Impact

(1) Background: In this review, we provide information published in recent years on the chemical forms, main biological functions and especially on antioxidant and prooxidant activities of selenium. The main focus is put on the impact of selenoproteins on maintaining cellular redox balance and anticancerogenic function. Moreover, we summarize data on chemotherapeutic application of redox active selenium compounds. (2) Methods: In the first section, main aspects of metabolism and redox activity of selenium compounds is reviewed. The second outlines multiple biological functions, asserted when selenium is incorporated into the structure of selenoproteins. The final section focuses on anticancer activity of selenium and chemotherapeutic application of redox active selenium compounds as well. (3) Results: optimal dietary level of selenium ensures its proper antioxidant and anticancer activity. We pay special attention to antioxidant activities of selenium compounds, especially selenoproteins, and their importance in antioxidant defence. It is worth noting, that data on selenium anticancer properties is still contraversive. Moreover, selenium compounds as chemotherapeutic agents usually are used at supranutritional doses. (4) Conclusions: Selenium play a vital role for many organism systems due to its incorporation into selenoproteins structure. Selenium possesses antioxidant activity at optimal doses, while at supranutritional doses, it displays prooxidant activity. Redox active selenium compounds can be used for cancer treatment; recently special attention is put to selenium containing nanoparticles.

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A phase II trial of pharmacological ascorbate, gemcitabine, and nabpaclitaxel for metastatic pancreatic cancer.

Journal of Clinical Oncology ◽

10.1200/jco.2020.38.4_suppl.tps791 ◽

2020 ◽

Vol 38 (4_suppl) ◽

pp. TPS791-TPS791

Author(s):

Pashtoon Murtaza Kasi ◽

Kellie Bodeker ◽

Daniel James Berg ◽

Chandrikha Chandrasekharan ◽

Saima Sharif ◽

...

Keyword(s):

Oxidative Stress ◽

Pancreatic Cancer ◽

Clinical Trial ◽

Cancer Cells ◽

Objective Response ◽

Plasma Concentrations ◽

High Dose ◽

Resectable Pancreatic Cancer ◽

Pancreatic Cancer Cells ◽

Production Of Hydrogen

TPS791 Background: FOLFIRINOX or gemcitabine/nab-paclitaxel are both frontline chemotherapy options for patients with metastatic pancreas cancer. For most who cannot tolerate the triplet, the latter doublet is the preferred option. Through previous work by our group, pharmacologic ascorbate is known to synergize with gemcitabine; preliminary in vitro data from our group suggests a similar synergistic response with paclitaxel. Though ascorbate has been utilized in cancer therapy, few robust trials have investigated intravenous delivery of ascorbate to deliver plasma concentrations that are cytotoxic to tumor cells. Our prior studies have demonstrated ascorbate induces oxidative stress and cytotoxicity in pancreatic cancer cells; this cytotoxicity appears to be greater in tumor vs. normal cells. We hypothesize that production of hydrogen peroxide mediates the increased susceptibility of pancreatic cancer cells to ascorbate-induced metabolic oxidative stress, resulting in improved treatment outcomes, which has led to the development of the clinical trial (NCT02905578). Methods: All participants receive gemcitabine (1000 mg/m2 weekly) and nab-paclitaxel (125 mg/m2) on cycle days 1, 8, and 15 of a 28-day cycle. Participants are randomized to ± pharmacologic ascorbate (75-gram infusion 3x weekly) in addition to chemotherapy. Study therapy continues until tumor progression. The primary objective is to determine overall survival in patients when treated with combination gemcitabine, nab-Paclitaxel and high-dose ascorbic acid compared to gemcitabine and nab-paclitaxel in patients with non-resectable pancreatic cancer. Secondary objectives include determining objective response rate as well as progression free survival using RECIST 1.1 criteria employing a blinded reviewer for RECIST measurements. The study opened to accrual in 2018 with a goal of enrolling 65 participants. Oversight.Study is conducted under IND 105715 (J. Cullen, sponsor). The University of Iowa Biomedical IRB (IRB-01) serves as the IRB of record. Clinical trial information: NCT02905578.

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