Recent Advancements in the Development of Anti-Breast Cancer Synthetic Small Molecules

Elkaeed, Eslam B.; Salam, Hayam A. Abd El; Sabt, Ahmed; Al-Ansary, Ghada H.; Eldehna, Wagdy M.

doi:10.3390/molecules26247611

Cited by 12 publications

(6 citation statements)

References 127 publications

(152 reference statements)

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“…Choe and his coworkers (2020) [42] discovered that OPE has anticancer activities against breast cancer. The apoptosis system was defective, and there was unregulated growth in cancerous cells, while as in the case of malignant cells, cell proliferation was prevented by cell division with natural extracts.…”

Section: Anticancer Propertiesmentioning

confidence: 99%

Nutritional Profile, Phytochemical Compounds, Biological Activities, and Utilisation of Onion Peel for Food Applications: A Review

et al. 2022

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The majority of the by products formed during onion processing remain unutilized, yet they are rich in bioactive compounds and phytochemicals. Onions are a very valuable vegetable. Onion chemical compounds are incredibly diverse, and they work through a variety of pharmacological mechanisms to prevent disease. Although the mechanism of the action of the chemicals found in onions has been studied, there is still room for further reformulating of nutrient supplements and pharmaceutical treatments thanks to a growing interest in sustainable resource utilisation and circular economy. This review focuses on the primary bioactive components found in onion peel and skin, particularly total phenolics, quercetin, total flavonoids, and their derivatives, as well as their therapeutic uses such as cardioprotective, anticancer, neuroprotective, antiobesity, antidiabetic, and antibacterial constituents. This review article noted that onion peel is a valuable agricultural byproduct that has a variety of biologically active compounds so it can be used as a health-regulating ingredient, particularly in the biomedical and pharmacological domains.

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Section: Anticancer Propertiesmentioning

confidence: 99%

Nutritional Profile, Phytochemical Compounds, Biological Activities, and Utilisation of Onion Peel for Food Applications: A Review

et al. 2022

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“…Due to BC heterogeneity, the first-line treatment of the disease typically involves one or multiple chemotherapeutics having distinct modes of action such as antimetabolites, immunotherapeutics, hormonal/endocrine drugs, DNA alkylating agents, ion modulators, antimitotic agents, etc. [ 4 , 5 ]. The long-term survival of breast cancer patients depends on the tumor subtype, stage at the time of diagnosis, specific tumor markers, and the effectiveness of treatment.…”

Section: Introductionmentioning

confidence: 99%

Tuning of the Anti-Breast Cancer Activity of Betulinic Acid via Its Conversion to Ionic Liquids

Ossowicz-Rupniewska,

Klebeko,

Georgieva

et al. 2024

Pharmaceutics

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Betulinic acid (BA) is a natural pentacyclic triterpene with diverse biological activities. However, its low water solubility limits its pharmaceutical application. The conversion of pharmaceutically active molecules into ionic liquids (ILs) is a promising strategy to improve their physicochemical properties, stability, and/or potency. Here, we report the synthesis and characterization of 15 novel ILs containing a cation ethyl ester of a polar, non-polar, or charged amino acid [AAOEt] and an anion BA. Except for [ValOEt][BA], we observed preserved or up to 2-fold enhanced cytotoxicity toward hormone-dependent breast cancer cells MCF-7. The estimated IC50 (72 h) values within the series varied between 4.8 and 25.7 µM. We found that the most cytotoxic IL, [LysOEt][BA]2, reduced clonogenic efficiency to 20% compared to that of BA. In addition, we evaluated the effect of a 72 h treatment with BA or [LysOEt][BA]2, the most cytotoxic compound, on the thermodynamic behavior of MCF-7 cells. Based on our data, we suggest that the charged amino acid lysine included in the novel ILs provokes cytotoxicity by a mechanism involving alteration in membrane lipid organization, which could be accompanied by modulation of the visco–elastic properties of the cytoplasm.

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“…In order to reduce the aggressiveness of breast cancer and to prevent cancer cell multiplication, invasion and metastasis, it is urgently necessary to create more effective and safe treatments. [6][7][8][9] Cancer cells possess the ability to self-renew and can develop all types of cells. Hemostasis, embryogenesis, and proper development are all largely regulated by several signaling cascades.…”

Section: Introductionmentioning

confidence: 99%

Ligand Based Multi-Targeted Molecular Docking Analysis o f Terpenoid Phytoconstituents as Potential Chemotherapeutic Agents Against Breast Cancer: An In Silico Approach

Raju,

Kumar,

Sekar

et al. 2023

JOPCR

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Breast cancer is one of the most common cancers in women all around the world and is a dominant cause of deaths occurring all around the globe. The available potent drugs for breast cancer show adverse effects and resistance and are found to be ineffective in patients. The high cost of currently available cancer therapy and certain limitations of current treatment make it necessary to search for novel, cost-effective and efficient methods of cancer treatment. Phytochemicals are directly involved in treatment or precursors to synthesize useful drugs. Therefore, in the current investigation, 500 terpenoid phytoconstituents and five proteins associated with breast cancer including EGFR, ERα, HER2, NF-κB and Topo IIa were selected from various databases. Selected compounds were screened for their molecular properties based on Lipinski's rule of five resulting in 235 compounds exclusion. Drug-likeness and PAINS alert properties were predicted using pkCSM and SwissADME web servers which led to the omission of 43 compounds. The remaining 222 compounds were screened to predict their ADMET properties and based on these results, 117 compounds were selected to predict the anti-breast cancer potential. Finally, 73 compounds, which showed anti-breast cancer activity prediction, were virtually screened and the top four best-scoring compounds were selected as lead-like molecules and docked with the five respective breast cancer targets. The results showed that the top four lead-like molecules exhibited greater binding affinity and lesser toxicity than the standard drugs namely 4–Hydroxytamoxifen, Daunorubicin, Erlotinib and Lapatinib. Keywords: ADMET, Breast cancer, Chemotherapeutic agents, In silico analysis, Molecular docking, Terpenoids

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Recent Advancements in the Development of Anti-Breast Cancer Synthetic Small Molecules

Cited by 12 publications

References 127 publications

Nutritional Profile, Phytochemical Compounds, Biological Activities, and Utilisation of Onion Peel for Food Applications: A Review

Nutritional Profile, Phytochemical Compounds, Biological Activities, and Utilisation of Onion Peel for Food Applications: A Review

Tuning of the Anti-Breast Cancer Activity of Betulinic Acid via Its Conversion to Ionic Liquids

Ligand Based Multi-Targeted Molecular Docking Analysis o f Terpenoid Phytoconstituents as Potential Chemotherapeutic Agents Against Breast Cancer: An In Silico Approach

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