Natural Products and Synthetic Analogs as a Source of Antitumor Drugs

Sharifi‐Rad, Javad; Ozleyen, Adem; Tumer, Tugba Boyunegmez; Adetunji, Charles Oluwaseun; Omari, Nasreddine El; Balahbib, Abdelaali; Taheri, Yasaman; Bouyahya, Abdelhakim; Martorell, Miquel; Martins, Natália; Cho, William C.

doi:10.3390/biom9110679

Cited by 139 publications

(85 citation statements)

References 271 publications

(269 reference statements)

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“…These ethnopharmacological uses of plants have guided scientific investigation for a large number of plant species, and has led to the identification of thousands of secondary metabolites, with desirable biological properties, including antioxidant, antimicrobial [34,35], anticancer [36,37], antidiabetic [38], anti-inflammatory [39] and neuroprotective properties [40].…”

Section: Ethnopharmacological Relevance Of Natural Compounds For Nddsmentioning

confidence: 99%

Impact of Natural Compounds on Neurodegenerative Disorders: From Preclinical to Pharmacotherapeutics

Sharifi‐Rad

Lankatillake

Dias

et al. 2020

JCM

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172

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Among the major neurodegenerative disorders (NDDs), Alzheimer’s disease (AD) and Parkinson’s disease (PD), are a huge socioeconomic burden. Over many centuries, people have sought a cure for NDDs from the natural herbals. Many medicinal plants and their secondary metabolites are reported with the ability to alleviate the symptoms of NDDs. The major mechanisms identified, through which phytochemicals exert their neuroprotective effects and potential maintenance of neurological health in ageing, include antioxidant, anti-inflammatory, antithrombotic, antiapoptotic, acetylcholinesterase and monoamine oxidase inhibition and neurotrophic activities. This article reviews the mechanisms of action of some of the major herbal products with potential in the treatment of NDDs according to their molecular targets, as well as their regional sources (Asia, America and Africa). A number of studies demonstrated the beneficial properties of plant extracts or their bioactive compounds against NDDs. Herbal products may potentially offer new treatment options for patients with NDDs, which is a cheaper and culturally suitable alternative to conventional therapies for millions of people in the world with age-related NDDs.

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Section: Ethnopharmacological Relevance Of Natural Compounds For Nddsmentioning

confidence: 99%

Impact of Natural Compounds on Neurodegenerative Disorders: From Preclinical to Pharmacotherapeutics

Sharifi‐Rad

Lankatillake

Dias

et al. 2020

JCM

Self Cite

172

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“…Thus, there is an urgent need for the discovery of novel therapeutic targets and effective anticancer agents for the treatment of patients with NSCLC. Natural resources are abundant, containing plentiful natural substances with potent antitumor efficacy (4). In recent years, these substances, such as oridonin and Celastrus orbiculatus have attracted attention worldwide due to their accessibility, and relatively low adverse effects (5,6).…”

Section: Resveratrol Modulates the Apoptosis And Autophagic Death Of mentioning

confidence: 99%

Resveratrol modulates the apoptosis and autophagic death of human lung adenocarcinoma A549 cells via a p53‑dependent pathway: Integrated bioinformatics analysis and experimental validation

Fan

Yang

et al. 2020

Int J Oncol

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Resveratrol (RSV) has been reported to exhibit cytotoxic activity in multiple types of malignant cells; however, the mechanisms underlying the antitumor effects of RSV in non-small-cell lung cancer (NSCLC) cells remain undetermined. Combining bioinformatics analysis with experimental validation, the present study aimed to examine the effects of RSV on the apoptosis and autophagy of A549 NSCLC cells, and to determine the potential underlying molecular mechanisms. Bioinformatics analysis was used to determine the differentially expressed genes (DEGs) and identify the enriched biological functions and pathways associated with these DEGs following RSV treatment. Cell viability was determined by MTT assay, and flow cytometry and TUNEL assay were used to evaluate cell apoptosis. Monodansylcadaverine staining combined with a transmission electron microscope were used to evaluate the extent of autophagy. The expression levels of apoptosis-, autophagy-, or pathway-associated molecular markers were measured by reverse transcription-quantitative PCR and/or western blot analysis. By bioinformatics analysis, a total of 1,031 DEGs were identified in the RSV-treated A549 cells, which were enriched in apoptosis-, or autophagy-related biological functions and the p53 signaling pathway. In validation experiments, RSV significantly reduced cell viability and initiated apoptosis, with an increase in the number of apoptotic cells; it also upregulated cleaved caspase-3 expression and Bax expression, and downregulated the Bcl-2 expression levels. Additionally, there was an increase in the accumulation of green dot-like structures, indicative of autophagic vesicles, observed under a fluorescence microscope, and an increase in the presence of autophagic vacuoles observed using a transmission electron microscope following RSV treatment. Furthermore, the expression levels of the autophagy-related proteins, LC3-II/LC3-I and Beclin-1, were increased and p62 expression was decreased. 3-methyladenine (3-MA), an inhibitor of autophagy, partially reversed the RSV-induced cytotoxic effects, but did not significantly alter the number of apoptotic cells. RSV elevated the p53 levels and decreased the phosphorylated (p-)Mdm2 and p-Akt levels. Pifithrin-α, an inhibitor of p53, partially reduced RSV-induced apoptosis and autophagy. On the whole, the results of the present study demonstrated that RSV initiates the apoptosis and autophagic death of A549 cells via the activation of the p53 signaling pathway, further highlighting the potential of RSV for the treatment of NSCLC.

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“…Currently, the identification of novel bioactive molecules with pharmacological effects is a promising strategy of research to combat several pathologies 1‐3 . Medicinal plants biosynthesize numerous bioactive compounds including terpenoids, flavonoids and alkaloids as secondary metabolites 1,4 .…”

Section: Introductionmentioning

confidence: 99%

“…Medicinal plants biosynthesize numerous bioactive compounds including terpenoids, flavonoids and alkaloids as secondary metabolites 1,4 . These metabolites in particularly essential oils (Eos) are endowed with important biological activities including anticancer, antimicrobial, antioxidant, anti‐parasitic, anti‐inflammatory and antidiabetic properties 3,5‐11 …”

Section: Introductionmentioning

confidence: 99%

Pharmacological investigation ofAjuga ivaessential oils collected at three phenological stages

Bouyahya

Omari

Belmehdi

et al. 2020

Flavour & Fragrance J

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Ajuga iva (A iva) is a medicinal plant used mainly in traditional medicine. This study was aimed to identify the volatile compounds of A iva essential oils (AIEO) at three developmental periods, and to evaluate their pharmacological properties. Chemical volatile compounds were identified by GC/MS analysis. Twenty‐eight volatile components were identified, belonging mainly to oxygenated monoterpenes and hydrocarbons monoterpenes. Carvacrol, octadecane, methyl chavicol were the major volatile components of AIEO at the three phenological stages. FRAP, DPPH and ABTS assays were adopted to estimate the antioxidant effects. AIEO at the vegetative stage exhibited important antioxidant effects with IC50 = 52.43 μg/mL (DPPH), IC50 = 115.22 μg/mL (FRAP), and, IC50 = 143.40 μg/mL (ABTS). The antidiabetic activity was evaluated in vitro by the inhibition of α‐amylase and α‐glucosidase. AIEO at the vegetative stage was the most active as an enzyme inhibitor of α‐amylase (IC50 = 101.727 μg/mL) and α‐glucosidase (IC50 = 86.93 μg/mL). The dermatoprotective effect was investigated by the in vitro inhibition of tyrosinase and elastase activities. AIEO at the vegetative stage showed the lowest IC50 inhibition values against tyrosinase (IC50 = 87.49 μg/mL) and elastase (IC50 = 192.21 μg/mL). Antifungal properties of AIEO were investigated on Trichophyton violaceum, T tonsurans and T mentagrophytes. The three EOs of A iva exhibited important inhibitions of the tested dermatophytes. The findings of this work showed that phenological stages affect significantly the volatile compounds of A iva, and these fluctuations influence mainly the biological properties. Moreover, further investigations concerning in vivo pharmacodynamic and pharmacokinetic investigations as well as clinical trials of these identified compounds could develop antidiabetic, dermatoprotective and anti‐dermatophyte drugs.

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Natural Products and Synthetic Analogs as a Source of Antitumor Drugs

Cited by 139 publications

References 271 publications

Impact of Natural Compounds on Neurodegenerative Disorders: From Preclinical to Pharmacotherapeutics

Impact of Natural Compounds on Neurodegenerative Disorders: From Preclinical to Pharmacotherapeutics

Resveratrol modulates the apoptosis and autophagic death of human lung adenocarcinoma A549 cells via a p53‑dependent pathway: Integrated bioinformatics analysis and experimental validation

Pharmacological investigation ofAjuga ivaessential oils collected at three phenological stages

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