scholarly journals Putative Anticancer Compounds from Plant-Derived Endophytic Fungi: A Review

Molecules ◽  
2022 ◽  
Vol 27 (1) ◽  
pp. 296
Author(s):  
Md. Hridoy ◽  
Md. Zobayer Hossain Gorapi ◽  
Sadia Noor ◽  
Nargis Sultana Chowdhury ◽  
Md. Mustafizur Rahman ◽  
...  
Keyword(s):  
Cost Effectiveness ◽  
Antitumor Activity ◽  
Genetic Engineering ◽  
Endophytic Fungi ◽  
Anticancer Agents ◽  
Host Plants ◽  
Purification And Characterization ◽  
Anticancer Compounds ◽  
Comprehensive Review ◽  
Lung Cancers

Endophytic fungi are microorganisms that exist almost ubiquitously inside the various tissues of living plants where they act as an important reservoir of diverse bioactive compounds. Recently, endophytic fungi have drawn tremendous attention from researchers; their isolation, culture, purification, and characterization have revealed the presence of around 200 important and diverse compounds including anticancer agents, antibiotics, antifungals, antivirals, immunosuppressants, and antimycotics. Many of these anticancer compounds, such as paclitaxel, camptothecin, vinblastine, vincristine, podophyllotoxin, and their derivatives, are currently being used clinically for the treatment of various cancers (e.g., ovarian, breast, prostate, lung cancers, and leukemias). By increasing the yield of specific compounds with genetic engineering and other biotechnologies, endophytic fungi could be a promising, prolific source of anticancer drugs. In the future, compounds derived from endophytic fungi could increase treatment availability and cost effectiveness. This comprehensive review includes the putative anticancer compounds from plant-derived endophytic fungi discovered from 1990 to 2020 with their source endophytic fungi and host plants as well as their antitumor activity against various cell lines.

Bioactive Secondary Metabolites from Endophytic Fungi

2020 ◽  
Vol 27 (11) ◽  
pp. 1836-1854 ◽  
Author(s):  
Elena Ancheeva ◽  
Georgios Daletos ◽  
Peter Proksch
Keyword(s):  
Secondary Metabolites ◽  
Endophytic Fungi ◽  
Host Plants ◽  
Biological Activities ◽  
Cytotoxic Agents ◽  
Special Focus ◽  
Plant Metabolites ◽  
Direct Production ◽  
Bioactive Secondary Metabolites ◽  
Fungal Genes

Background: Endophytes represent a complex community of microorganisms colonizing asymptomatically internal tissues of higher plants. Several reports have shown that endophytes enhance the fitness of their host plants by direct production of bioactive secondary metabolites, which are involved in protecting the host against herbivores and pathogenic microbes. In addition, it is increasingly apparent that endophytes are able to biosynthesize medicinally important “phytochemicals”, originally believed to be produced only by their host plants. Objective: The present review provides an overview of secondary metabolites from endophytic fungi with pronounced biological activities covering the literature between 2010 and 2017. Special focus is given on studies aiming at exploration of the mode of action of these metabolites towards the discovery of leads from endophytic fungi. Moreover, this review critically evaluates the potential of endophytic fungi as alternative sources of bioactive “plant metabolites”. Results: Over the past few years, several promising lead structures from endophytic fungi have been described in the literature. In this review, 65 metabolites are outlined with pronounced biological activities, primarily as antimicrobial and cytotoxic agents. Some of these metabolites have shown to be highly selective or to possess novel mechanisms of action, which hold great promises as potential drug candidates. Conclusion: Endophytes represent an inexhaustible reservoir of pharmacologically important compounds. Moreover, endophytic fungi could be exploited for the sustainable production of bioactive “plant metabolites” in the future. Towards this aim, further insights into the dynamic endophyte - host plant interactions and origin of endophytic fungal genes would be of utmost importance.

Cytotoxic Activity and DNA Binding Property of New Aminopyrimidine Derivatives

2020 ◽  
Vol 17 (5) ◽  
pp. 640-654
Author(s):  
Hamidreza Akrami ◽  
Bibi Fatemeh Mirjalili ◽  
Omidreza Firuzi ◽  
Azadeh Hekmat ◽  
Ali Akbar Saboury ◽  
...  
Keyword(s):  
Cell Lines ◽  
Anticancer Agents ◽  
Lymphoblastic Leukemia ◽  
Cd Spectroscopy ◽  
Myelogenous Leukemia ◽  
Breast Adenocarcinoma ◽  
Binding Property ◽  
Anticancer Compounds ◽  
Calf Thymus ◽  
Dna Binding Property

Background: Chromene and anilinopyrimidine heterocyclics are attractive anticancer compounds that have inspired many researchers to design novel derivatives bearing improved anticancer activity. Methods: A series of pyrimidine-fused benzo[f]chromene derivatives 6a-x were synthesized as anticancer hybrids of 1H-benzo[f]chromenes and anilinopyrimidines. The inhibitory activity of the synthesized compounds 6a-x against cell viability of human chronic myelogenous leukemia (K562), human acute lymphoblastic leukemia (MOLT-4) and human breast adenocarcinoma (MCF-7) cell lines was evaluated using MTT assay. The interaction of the most promising compound with calf-thymus DNA was also studied using spectrometric titrations and Circular Dichroism (CD) spectroscopy. Results: Most compounds showed promising activity against tested cell lines. Among them, 2,4- dimethoxyanilino derivative 6g exhibited the best profile of activity against tested cell lines (IC50s = 1.6-6.1 μM) with no toxicity against NIH3T3 normal cell (IC50 >200 μM). The spectrometric studies exhibited that compound 6g binds to DNA strongly and may change DNA conformation significantly, presumably via a groove binding mechanism. Conclusion: The results of this study suggest that the prototype compound 6g can be considered as a novel lead compound for the design and discovery of novel anticancer agents.

scholarly journals Novel Marine Compounds: Anticancer or Genotoxic?

2004 ◽  
Vol 2004 (2) ◽  
pp. 93-98 ◽  
Author(s):  
Jamal M. Arif ◽  
Amal A. Al-Hazzani ◽  
Muhammed Kunhi ◽  
Fahad Al-Khodairy
Keyword(s):  
Clinical Trials ◽  
Anticancer Agents ◽  
Screening Tests ◽  
Tumor Xenograft ◽  
Anticancer Compounds ◽  
Early Exit ◽  
Marine Compounds ◽  
Xenograft Models ◽  
Pharmaceutical Industries ◽  
Carcinogenesis Models

In the past several decades, marine organisms have generously gifted to the pharmaceutical industries numerous naturally bioactive compounds with antiviral, antibacterial, antimalarial, anti-inflammatory, antioxidant, and anticancer potentials. But till date only few anticancer drugs (cytarabine, vidarabine) have been commercially developed from marine compounds while several others are currently in different clinical trials. Majority of these compounds were tested in the tumor xenograft models, however, lack of anticancer potential data in the chemical- and/or oncogene-induced pre-initiation animal carcinogenesis models might have cost some of the marine anticancer compounds an early exit from the clinical trials. This review critically discusses importance of preclinical evaluation, failure of human clinical trials with certain potential anticancer agents, the screening tests used, and choice of biomarkers.

Advancements in the Use of Platinum Complexes as Anticancer Agents

2021 ◽  
Vol 21 ◽  
Author(s):  
Rajiv Sharma ◽  
Vikram Jeet Singh ◽  
Pooja A Chawla
Keyword(s):  
Anticancer Agents ◽  
Biomedical Applications ◽  
Clinical Importance ◽  
Platinum Complexes ◽  
Water Soluble ◽  
Platinum Compounds ◽  
Anticancer Compounds ◽  
Cellular Resistance ◽  
Anti Cancer ◽  
Target Effects

Background: The platinum (II) complexes as anticancer agents have been well explored for the development of novel analogs. Yet, none of them achieved clinical importance in oncology. At present, anticancer compounds containing platinum (II) complexes have been employed in the treatment of colorectal, lung, and genitourinary tumors. Among the platinum-based anticancer drugs, Cisplatin (cis-diamine dichloroplatinum (II), cis-[Pt(NH3)2Cl2]) is one of the most potent components of cancer chemotherapy. The nephrotoxicity, neurotoxicity and ototoxicity, and platinum compounds associated resistant cancer are some major disadvantages. Objective: With the rapidly growing interest in platinum (II) complexes in tumor chemotherapy, researchers have synthesized many new platinum analogs as anticancer agents that show better cytotoxicity, and less off-target effects with less cellular resistance. This follows the introduction of oxaliplatin, water-soluble carboplatin, multinuclear platinum and newly synthesized complexes, etc. Method: This review emphasizes recent advancements in drug design and development, the mechanism of platinum (II) complexes, their stereochemistry, current updates, and biomedical applications of platinum-based anticancer agents. Conclusion: In the last few decades, the popularity of platinum complexes as potent anti-cancer agents has risen as scientists have synthesized many new platinum complexes that exhibit better cytotoxicity coupled with less off-target effects.

Naturally occurring heterocyclic anticancer compounds

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Shashi Kiran Misra ◽  
Kamla Pathak
Keyword(s):  
Anticancer Agents ◽  
Topoisomerase I ◽  
Heterocyclic Ring ◽  
Cytotoxic Action ◽  
Extrinsic Pathway ◽  
Anticancer Compounds ◽  
Halichondrin B ◽  
Naturally Occurring ◽  
Microbial Infections ◽  
Almost All

Abstract Naturally occurring heterocyclic scaffolds are key ingredients for the development of various therapeutics employed for biomedical applications. Heterocyclic pharmacophores are widely disseminated and have been befallen in almost all categories of drugs for the alleviation of myriad ailments including diabetes, neurodegenerative, psychiatric, microbial infections, disastrous cancers etc. Countless fused heterocyclic anticancerous templates are reported to display antimetabolite, antioxidant, antiproliferative, cytostatic etc. pharmacological actions via targeting different signaling pathways (cell cycle, PI-3kinase/Akt, p53, caspase extrinsic pathway etc.), overexpressive receptors (EGRF, HER2, EGF, VEGF etc.) and physiological enzymes (topoisomerase I and II, cyclin dependent kinase etc.). A compiled description on various natural sources (plants, microbes, marine) containing anticancer agents comprising heterocyclic ring specified with presence of nitrogen (vincristine, vinblastine, indole-3-carbinol, meridianins, piperine, lamellarins etc.), oxygen (paclitaxel, halichondrin B, quercetin, myricetin, kaempferol etc.) and sulphur atoms (brugine, fucoidan, carrageenan etc.) are displayed here along with their molecular level cytotoxic action and therapeutic applications.

Potency of Endophytic Fungi Isolated from Medicinal Plants in Egypt as a Resource for Anticancer Compounds

2020 ◽  
pp. 113-131
Author(s):  
Ahmed M. Abdel-Azeem ◽  
Sherif M. Zaki ◽  
Fatma M. Salem ◽  
Waleed F. Khalil ◽  
Sherif Y. Saleh
Keyword(s):  
Medicinal Plants ◽  
Endophytic Fungi ◽  
Anticancer Compounds

scholarly journals ISOLASI CENDAWAN ENDOFIT DARI AKAR WANGI (Vetiveria zizanioides L.) DAN POTENSINYA SEBAGAI ANTIMIKROBA

1930 ◽  
Vol 8 (01) ◽  
pp. 115-121
Author(s):  
Israwati Harahap ◽  
Elsie
Keyword(s):  
Escherichia Coli ◽  
Endophytic Fungi ◽  
Host Plants ◽  
Vetiveria Zizanioides ◽  
Surface Sterilization ◽  
Anti Oxidant ◽  
In Vitro Inhibition ◽  
Fungal Extracts ◽  
Antimicrobial Potency

Endophytic fungi are microorganisms living in healthy tissue of their host plants without causing disease. Endophytic fungi live in every plant, including Vetiveria zizanioides L. medicinal plant intracellulary and/or intercellulary. This plant was screened pharmacologically for antibacterial, antifungal, anticataleptic, analgesic and anti-inflammatory, rheumatism, anti oxidant and anti arthritic activity. This research aimed to isolation endophytic fungi from V. zizanioides L. and to screening their antimicrobial potency against microflora Escherichia coli, Staphylococcus aureus, and Candida albicans. Endophytic fungi isolation from V. zizanioides L. was done by surface sterilization method. A total of 33 isolates were recovered from 88 leaves and 88 root segments. Based on antimicrobial activitytest, most of the fungal extracts showed in vitro inhibition of microbes growth.

scholarly journals Endophytic Fungi as Alternative and Reliable Sources for Potent Anticancer Agents

10.5772/67797 ◽  
2017 ◽  
Author(s):  
Edwin O. Omeje ◽  
Joy E. Ahomafor ◽  
Theophilus U. Onyekaba ◽  
Philip O. Monioro ◽  
Ibekwe Nneka ◽  
...  
Keyword(s):  
Endophytic Fungi ◽  
Anticancer Agents

Design, Synthesis, Molecular Docking and Biological Studies of New Heterocyclic Compounds Derived from -Diketonesas Novel EGFR and Pim-1 Inhibitors Endowed with Antitumor Activity

2022 ◽  
Vol 22 ◽  
Author(s):  
Rafat Milad Mohareb ◽  
Noha M. Asaad Bagato ◽  
Ibrahim Taha Radwan
Keyword(s):  
Molecular Docking ◽  
Antitumor Activity ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Diethyl Malonate ◽  
Binding Mode ◽  
Binding Modes ◽  
Binding Interactions ◽  
Biological Studies

Background: Cancer is a disease illustrated by a shift in the controlled mechanisms that control both cell proliferation and differentiation. It is regarded as a prime health problem worldwide, leading cause of human death-rate exceeded only by cardiovascular diseases. Many reported work was concerned with the discovery of new antitumor compounds this encourage us to synthesis new anticancer agents. Objective: In this work, we are aiming to synthesize target molecules from 1,3-dicarbonyl compounds through many heterocyclization reactions. Method: The reaction of either 4-methylaniline (1a) or 1-naphthylamine (1b) with diethyl malonate (2) gave the anilide derivatives 3a and 3b, respectively. The latter products underwent a series of heterocyclization reactions to give the pyridine, pyran andthiazole derivatives which confirmed with the required spectral data. Results: Thein-vitro antitumor evaluations of the newly synthesized products against four cancer cell lines MCF-7, NCI-H460, SF-268 and WI 38 as normal cell line were screened and the data revealed that compounds 11a, 18b, 18c and 20d showed high antitumor activity and 20dindividualize with potential antitumor activity towards cell lines with lowest cytotoxicity effect. Both EGFR and PIM-1 enzyme inhibition were investigated for the compound 20d and his inhibition effect was promising for each enzyme showing IC50=45.67 ng and 553.3 ng for EGFR and PIM-1, respectively. Conclusion: Molecular docking results of compound 20d showed a strong binding interactions on both enzymes, where, good binding modes obtained on case of EGFR, which closely similar to the binding mode of standard Erlotinib. While, 20d showed complete superimposition binding interactions with VRV-cocrystallized ligand of PIM-1 that may expounds the in-vitro antitumor activity.

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