Discovery, Development, and Design of Anthocyanins-Inspired Anticancer Agents-A Comprehensive Review

2021 ◽  
Vol 21 ◽  
Author(s):  
Sasadhar Majhi
Keyword(s):  
Secondary Metabolites ◽  
Anticancer Agents ◽  
Water Soluble ◽  
Commercial Application ◽  
Chemical Derivatization ◽  
Anticancer Activities ◽  
Bioactive Natural Products ◽  
Natural Colorants ◽  
Wide Range ◽  
Chemical Class

: Mother Nature is an indispensable source of bioactive natural products. Bioactive secondary metabolites have played a crucial role in the drug development and discovery process; mainly anticancer and antibiotic molecules are extensively enriched with molecules of natural origin. Anthocyanins are water-soluble secondary metabolites found in most species in the plant domain especially flowers, fruits, and tubers. These natural vacuolar pigments belong to the chemical class of phenolic moieties which are responsible for the shiny orange, red, blue, pink, and violet colors in the fruits, flowers, and vegetables. Chemically, anthocyanins comprise a core structure in the form of flavylium cation or 2-phenylbenzopyrylium and these natural colorants are polyhydroxy and polymethoxy analouges of this flavylium cation and can have sugar moieties or acylated groups linked at different positions. Currently, these molecules have raised a growing interest because of their wide range of colors, innocuous, beneficial health effects, and commercial application of these compounds in functional foods, nutraceuticals, pharmaceutical and cosmetic industries. However, interest in anthocyanin derivatives has noticeably enhanced in recent years due to their higher stability, improved bioavailability in biological matrices, and better use in food matrices and cosmetic products. Due to the enormous potential of natural anthocyanins and their derivatives this review tries to cover syntheses of anthocyanins and their analogues, chemical derivatization of anthocyanins, and anticancer activities such as breast, colorectal, leukemia, lung, prostate, and skin cancer of anthocyanins efficiently.

Synthesis and Antibacterial / Anticancer Activities of Compounds Containing Pyrazole Ring Linked to Piperazines

2020 ◽  
Vol 16 (4) ◽  
pp. 419-431
Author(s):  
Kishore K. Valluri ◽  
Tejeswara R. Allaka ◽  
IV Kasi Viswanath ◽  
Nagaraju PVVS
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Cancer Cell Line ◽  
Pyrazole Ring ◽  
Therapeutic Effects ◽  
Anticancer Activities ◽  
Human Colon Cancer ◽  
Parent Molecule ◽  
Wide Range

Background: Many pyrazole piperazine derivatives are known to exhibit a wide range, thus being attractive for the drug design and synthesis of interesting class of widely studied heterocyclic compounds. It is therefore necessary to devote continuing effort for the identification and development of New Chemical Entities (NCEs) as potential antibacterial and anticancer agents to address serious health problems. Methods: A series of new compounds containing pyrazole ring linked to a piperazine hydrochloride moiety were synthesized and screened for their antibacterial activity, cytotoxicity of novel scaffolds are described by variation in therapeutic effects of parent molecule. The structure variants were characterized by using a blend of spectroscopic 1H NMR, 13C NMR, IR, Mass and chromatographic techniques. Results: When tested for in vitro antibacterial and anticancer activities, several of these compounds showed good activities. The target compounds 9b, 9a and 9e exhibited a high degree of anticancer activity against human colon cancer cell line Caco-2 and human breast cancer cell line MDAMB231. Further, 9a, 9b, 9d, and 9h showed better activity towards four medically relevant organisms; Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Klebsiella Species compared to CPF. In the present investigation, cheminfomatics tools Molinspiration, 2003 and MolSoft, 2007 for the prediction of insilico molecular properties and drug likeness for the target compounds 9a-h was evaluated and positive results were observed. Conclusion: Our study revealed that the molecular framework presented here could be a useful template for the identification of novel small molecules as promising antibacterial/ anticancer agents.

Synthesis and characterization of a new series of thiadiazole derivatives as potential anticancer agents

2020 ◽  
Vol 26 (1) ◽  
pp. 6-13 ◽  
Author(s):  
Ulviye Acar Çevik ◽  
Derya Osmaniye ◽  
Serkan Levent ◽  
Begüm Nurpelin Sağlik ◽  
Betül Kaya Çavuşoğlu ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Biological Activities ◽  
Cancer Cell Line ◽  
Chemotherapeutic Agents ◽  
Anticancer Activities ◽  
Normal Tissues ◽  
H Nmr ◽  
Wide Range ◽  
Thiadiazole Derivatives ◽  
Low Efficiency

AbstractCancer is one of the most common causes of death in the world. Despite the importance of combating cancer in healthcare systems and research centers, toxicity in normal tissues and the low efficiency of anticancer drugs are major problems in chemotherapy. Nowadays the aim of many medical research projects is to discover new safer and more effective anticancer agents. 1,3,4-Thiadiazole compounds are important fragments in medicinal chemistry because of their wide range of biological activities, including anticancer activities. The aim of this study was to determine the capacity of newly synthesized 1,3,4-thiadiazole compounds as chemotherapeutic agents. The structures of the obtained compounds were elucidated using 1H-NMR, 13C-NMR and mass spectrometry. Although the thiadiazole derivatives did not prove to be significantly cytotoxic to the tumour tissue cultures, compound 4i showed activity against the C6 rat brain cancer cell line (IC50 0.097 mM) at the tested concentrations.

scholarly journals Medicinal plants of the family Lamiaceae as functional foods – a review  

2016 ◽  
Vol 34 (No. 5) ◽  
pp. 377-390 ◽  
Author(s):  
K. Carović-Stanko ◽  
M. Petek ◽  
M. Grdiša ◽  
J. Pintar ◽  
D. Bedeković ◽  
...  
Keyword(s):  
Medicinal Plants ◽  
Secondary Metabolites ◽  
Bioactive Compounds ◽  
Functional Foods ◽  
Complex Mixture ◽  
Food Preservation ◽  
Anticancer Activities ◽  
Wide Range ◽  
The Family ◽  
Special Complex

Historically, species of the family Lamiaceae have enjoyed a rich tradition of use for flavouring, food preservation, and medicinal purposes, due to both their curative and their preventive properties. It is well known that each species has a special, complex mixture of bioactive compounds in which each component contributes to its overall bioactivity. Their value lays in the production of a wide range of secondary metabolites with potent antibacterial, antioxidant, anti-inflammatory, antimicrobial, antiviral, and anticancer activities. This review focuses on the Lamiaceae species and their secondary metabolites encompassing a wide array of beneficial functions and their applicability as sources of functional foods. It could help in addressing specific consumer needs as healthy diet is a part of the lifestyle that maintains or improves overall health.

scholarly journals Medicinal Potentialities of Plant Defensins: A Review with Applied Perspectives

Medicines ◽  
2019 ◽  
Vol 6 (1) ◽  
pp. 29 ◽  
Author(s):  
Nida Ishaq ◽  
Muhammad Bilal ◽  
Hafiz Iqbal
Keyword(s):  
Secondary Metabolites ◽  
Anticancer Agents ◽  
Genetically Modified Organisms ◽  
Defense Mechanism ◽  
Metal Tolerance ◽  
Biological Activities ◽  
Microbial Pathogens ◽  
Anticancer Activities ◽  
Eukaryotic Microorganisms ◽  
Plant Defensins

Plant-based secondary metabolites with medicinal potentialities such as defensins are small, cysteine-rich peptides that represent an imperative aspect of the inherent defense system. Plant defensins possess broad-spectrum biological activities, e.g., bactericidal and insecticidal actions, as well as antifungal, antiviral, and anticancer activities. The unique structural and functional attributes provide a nonspecific and versatile means of combating a variety of microbial pathogens, i.e., fungi, bacteria, protozoa, and enveloped viruses. Some defensins in plants involved in other functions include the development of metal tolerance and the role in sexual reproduction, while most of the defensins make up the innate immune system of the plants. Defensins are structurally and functionally linked and have been characterized in various eukaryotic microorganisms, mammals, plants, gulls, teleost species of fish, mollusks, insect pests, arachnidan, and crustaceans. This defense mechanism has been improved biotechnologically as it helps to protect plants from fungal attacks in genetically modified organisms (GMO). Herein, we review plant defensins as secondary metabolites with medicinal potentialities. The first half of the review elaborates the origin, structural variations, and mechanism of actions of plant defensins. In the second part, the role of defensins in plant defense, stress response, and reproduction are discussed with suitable examples. Lastly, the biological applications of plant defensins as potential antimicrobial and anticancer agents are also deliberated. In summary, plant defensins may open a new prospect in medicine, human health, and agriculture.

scholarly journals The Phylum Bryozoa as a Promising Source of Anticancer Drugs

Marine Drugs ◽  
2019 ◽  
Vol 17 (8) ◽  
pp. 477 ◽  
Author(s):  
Figuerola ◽  
Avila
Keyword(s):  
Secondary Metabolites ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Chemical Diversity ◽  
Anticancer Properties ◽  
Antitumor Compounds ◽  
Wide Range ◽  
Drug Synthesis ◽  
Low Toxicity ◽  
Promising Source

Recent advances in sampling and novel techniques in drug synthesis and isolation have promoted the discovery of anticancer agents from marine organisms to combat this major threat to public health worldwide. Bryozoans, which are filter-feeding, aquatic invertebrates often characterized by a calcified skeleton, are an excellent source of pharmacologically interesting compounds including well-known chemical classes such as alkaloids and polyketides. This review covers the literature for secondary metabolites isolated from marine cheilostome and ctenostome bryozoans that have shown potential as cancer drugs. Moreover, we highlight examples such as bryostatins, the most known class of marine-derived compounds from this animal phylum, which are advancing through anticancer clinical trials due to their low toxicity and antineoplastic activity. The bryozoan antitumor compounds discovered until now show a wide range of chemical diversity and biological activities. Therefore, more research focusing on the isolation of secondary metabolites with potential anticancer properties from bryozoans and other overlooked taxa covering wider geographic areas is needed for an efficient bioprospecting of natural products.

Design, Synthesis, SAR Study, Antimicrobial and Anticancer Evaluation of Novel 2-Mercaptobenzimidazole Azomethine Derivatives

2020 ◽  
Vol 20 (15) ◽  
pp. 1559-1571 ◽  
Author(s):  
Sumit Tahlan ◽  
Balasubramanian Narasimhan ◽  
Siong Meng Lim ◽  
Kalavathy Ramasamy ◽  
Vasudevan Mani ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Anticancer Agents ◽  
Benzimidazole Derivatives ◽  
Dilution Method ◽  
Anticancer Activities ◽  
Design Synthesis ◽  
Standard Drug ◽  
Wide Range ◽  
Sar Study

Background: Various analogues of benzimidazole are found to be biologically and therapeutically potent against several ailments. Benzimidazole when attached with heterocyclic rings has shown wide range of potential activities. So, from the above provided facts, we altered benzimidazole derivatives so that more potent antagonists could be developed. In the search for a new category of antimicrobial and anticancer agents, novel azomethine of 2-mercaptobenzimidazole derived from 3-(2- (1H-benzo[d]imidazol-2-ylthio)acetamido)benzohydrazide were synthesized. Results and Discussion: The synthesized analogues were characterized by FT-IR, 1H/13C-NMR and MS studies as well C, H, N analysis. All synthesized compounds were evaluated for in vitro antibacterial activity against Gram-positive (B. subtilis), Gram-negative (E. coli, P. aeruginosa, K. pneumoniae and S. typhi) strains and in vitro antifungal activity against C. albicans and A. niger strains by serial dilution method, the minimum inhibitory concentration (MIC) described in μM/ml. The in vitro anticancer activity of synthesized compounds was determined against human colorectal carcinoma cell line (HCT- 116) using 5-fluorouracil as standard drug. Conclusion: In general, most of the synthesized derivatives exhibited significant antimicrobial and anticancer activities. Compounds 8, 10, 15, 16, 17, 20 and 22 showed significant antimicrobial activity towards tested bacterial and fungal strains and compound 26 exhibited significant anticancer activity.

scholarly journals Plant Antimicrobial Peptides as Potential Anticancer Agents

2015 ◽  
Vol 2015 ◽  
pp. 1-11 ◽  
Author(s):  
Jaquelina Julia Guzmán-Rodríguez ◽  
Alejandra Ochoa-Zarzosa ◽  
Rodolfo López-Gómez ◽  
Joel E. López-Meza
Keyword(s):  
Antimicrobial Peptides ◽  
Anticancer Agents ◽  
Pathogenic Bacteria ◽  
Defense Mechanism ◽  
Immune Defense ◽  
Innate Immune ◽  
High Morbidity ◽  
Anticancer Activities ◽  
Innate Immune Defense ◽  
Wide Range

Antimicrobial peptides (AMPs) are part of the innate immune defense mechanism of many organisms and are promising candidates to treat infections caused by pathogenic bacteria to animals and humans. AMPs also display anticancer activities because of their ability to inactivate a wide range of cancer cells. Cancer remains a cause of high morbidity and mortality worldwide. Therefore, the development of methods for its control is desirable. Attractive alternatives include plant AMP thionins, defensins, and cyclotides, which have anticancer activities. Here, we provide an overview of plant AMPs anticancer activities, with an emphasis on their mode of action, their selectivity, and their efficacy.

scholarly journals The Understudied Phylum Bryozoa as a Promising Source of Anticancer Drugs

2019 ◽  
Author(s):  
Blanca Figuerola ◽  
Conxita Avila
Keyword(s):  
Secondary Metabolites ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Chemical Diversity ◽  
Anticancer Properties ◽  
Wide Range ◽  
Drug Synthesis ◽  
Low Toxicity ◽  
Promising Source ◽  
Excellent Source

Recent advances in sampling and novel techniques in drug synthesis and isolation have promoted the discovery of anticancer agents from marine organisms to combat this major threat to public health worldwide. Bryozoans, filter-feeding, sessile aquatic invertebrates often characterized by a calcified skeleton, are an excellent source of pharmacologically interesting compounds including well-known chemical classes such as alkaloids and polyketides. This review covers the literature for secondary metabolites isolated from marine cheilostome and ctenostome bryozoans that have shown potential as cancer drugs. Moreover, we highlight examples such as bryostatins, the most known class of marine-derived compounds from this animal phylum, which is advancing through anticancer clinical trials due to their low toxicity and antineoplastic activity. The bryozoan antitumour compounds discovered until now show a wide range of chemical diversity and biological activities. Therefore, more research focusing on the isolation of secondary metabolites with potential anticancer properties from bryozoans and other overlooked taxa covering wider geographic areas is needed for an efficient bioprospecting of natural products.

Cytotoxic and Antibiotic Potential of Secondary Metabolites from the Lichen Umbilicaria muhlenbergii

2020 ◽  
Vol 21 (14) ◽  
pp. 1516-1527
Author(s):  
Lyndon Letwin ◽  
Ladislav Malek ◽  
Zacharias Suntres ◽  
Lew Christopher
Keyword(s):  
Secondary Metabolites ◽  
Crude Extract ◽  
Cellular Proliferation ◽  
Chemical Constituents ◽  
Positive Control ◽  
Anticancer Activities ◽  
Bioactive Natural Products ◽  
Cycle Arrest ◽  
Set Up ◽  
Mcf 7

Objective: Lichens are emerging as a promising natural source of bioactivities of pharmaceutical interest. The present study aims to contribute to the knowledge of the lichen Umbilicaria muhlenbergii as a potential source of pharmaceutically relevant anticancer and antibiotic lichen chemicals. Methods: The crude acetone extract of U. muhlenbergii exhibited 13.3 μg mL-1 cytotoxic activity (EC50) against breast cancer cells (MCF-7), as compared to a cisplatin positive control with EC50 of 5.8 μg mL-1. The antibiotic activity of the crude extract against a gram-positive Staphylococcus aureus was 22.5 μg mL-1 as MIC. Using silica gel 60 (SG60) column chromatography, the crude extract was then separated into eight fractions, which were further evaluated for their anticancer activities against MCF-7 cells. By means of propidium iodide flow cytometry, two of the eight SG60 fractions were found to cause cell cycle arrest in MCF-7 cells (73.14% of cells) at the G2 phase, which is indicative of apoptosis and inhibition of cellular proliferation. Results: Identification of chemical constituents present in these two SG60 fractions was carried out with Thin-Layer Chromatography (TLC) and a lichen metabolite database (Wintabolites). The two fractions (SG60-5 and SG60-6) were found to contain compounds belonging to the chemical families depsides, depsidones, anthraquinones, and xanthones. Discussion: The SG60-5 and SG60-6 fractions were further fractionated with Sephadex LH-20. Over 15% of the 46 LH-20 fractions obtained from the SG60-5 fraction caused 100% cell death, whereas 32% of the LH-20 fractions derived from SG60 6 fraction reduced cell survival to below 20%. Conclusion: This work extends the evaluation of the cytotoxic and antibiotic activities of lichen secondary metabolites to the species U. muhlenbergii. It presents encouraging results of pharmaceutical interest that set up lichens as an effective source of new bioactive natural products. Further investigations are underway to reveal the full biopharmaceutical potential of U. muhlenbergii.

scholarly journals (Z)-5-(3′,4′-Bis(benzyloxy)benzylidene)furan-2(5H)-one

Molbank ◽  
10.3390/m1193 ◽  
2021 ◽  
Vol 2021 (1) ◽  
pp. M1193
Author(s):  
Angelica Artasensi ◽  
Giovanna Baron ◽  
Giulio Vistoli ◽  
Giancarlo Aldini ◽  
Laura Fumagalli
Keyword(s):  
Natural Products ◽  
Secondary Metabolites ◽  
Good Yield ◽  
Biological Activities ◽  
The Novel ◽  
One Pot ◽  
Natural Form ◽  
Bioactive Natural Products ◽  
Beneficial Effects ◽  
Wide Range

Over the years secondary metabolites have been considered as lead molecules both in their natural form and as templates for medicinal chemistry. Some secondary metabolites such as polyphenols and flavan-3-ols exert beneficial effects after a modification by the microbiota. Synthetic precursors of some of these modified compounds, in turn, carried a γ-alkylidenebutenolide moiety which characterizes a large class of bioactive natural products endowed with a wide range of biological activities. For these reasons stereoselective preparation of γ-alkylidenebutenolide continues to be an important issue for organic chemists. Our objective is to synthetize the novel compound (Z)-5-(3′,4′-bis(benzyloxy)benzylidene)furan-2(5H)-one in a stereocontrolled-one-pot reaction. The product was obtained in good yield. Furthermore, the theoretical investigation of the transition states suggests a new procedure to achieve Z-isomer of β-unsubstituted γ-alkylidenebutenolide.

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