Plant secondary metabolites as lead compounds for the production of potent drugs

Srivastav, Vijay Kumar; Egbuna, Chukwuebuka; Tiwari, Mayank

doi:10.1016/b978-0-12-817890-4.00001-9

Cited by 12 publications

(13 citation statements)

References 33 publications

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“…Our review identified a considerable number of reports (77 studies) published in the last two decades, with an increasing trend over recent years. In fact, phytochemicals have great pharmaceutical significance due to their diverse structures (with more than 100,000 being described so far) and their pharmacological properties ( Srivastav et al, 2020 ), and have already made an important contribution to cancer treatments ( Ashraf, 2020 ). Our review also showed that carvacrol and its thymol isomer are capable of restraining growth and combating different tumor strains in vitro .…”

Section: Discussionmentioning

confidence: 99%

Antitumor Effects of Carvacrol and Thymol: A Systematic Review

et al. 2021

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Background: It is estimated that one in five people worldwide faces a diagnosis of a malignant neoplasm during their lifetime. Carvacrol and its isomer, thymol, are natural compounds that act against several diseases, including cancer. Thus, this systematic review aimed to examine and synthesize the knowledge on the antitumor effects of carvacrol and thymol.Methods: A systematic literature search was carried out in the PubMed, Web of Science, Scopus and Lilacs databases in April 2020 (updated in March 2021) based on the PRISMA 2020 guidelines. The following combination of health descriptors, MeSH terms and their synonyms were used: carvacrol, thymol, antitumor, antineoplastic, anticancer, cytotoxicity, apoptosis, cell proliferation, in vitro and in vivo. To assess the risk of bias in in vivo studies, the SYRCLE Risk of Bias tool was used, and for in vitro studies, a modified version was used.Results: A total of 1,170 records were identified, with 77 meeting the established criteria. The studies were published between 2003 and 2021, with 69 being in vitro and 10 in vivo. Forty-three used carvacrol, 19 thymol, and 15 studies tested both monoterpenes. It was attested that carvacrol and thymol induced apoptosis, cytotoxicity, cell cycle arrest, antimetastatic activity, and also displayed different antiproliferative effects and inhibition of signaling pathways (MAPKs and PI3K/AKT/mTOR).Conclusions: Carvacrol and thymol exhibited antitumor and antiproliferative activity through several signaling pathways. In vitro, carvacrol appears to be more potent than thymol. However, further in vivo studies with robust methodology are required to define a standard and safe dose, determine their toxic or side effects, and clarify its exact mechanisms of action.This systematic review was registered in the PROSPERO database (CRD42020176736) and the protocol is available at https://www.crd.york.ac.uk/prospero/display_record.php?RecordID=176736.

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Section: Discussionmentioning

confidence: 99%

Antitumor Effects of Carvacrol and Thymol: A Systematic Review

et al. 2021

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“…Moreover, oleanolic, ursolic and tirucallic acids have been long-recognized to have anti-inflammatory and antihyperlipidemic properties in vivo test [ 49 , 50 ], as well as 3-oxo -tirucalla-8,24-dien-21-oic acid, which also reports anti-proliferative activities [ 51 ]. In a recent study, oleanolic and ursolic acid have also shown in silico putative activity against the main protease of the SARS-CoV-2 responsible for coronavirus disease (COVID-19), suggesting further investigations for their potential antiviral activity [ 52 , 53 , 54 ].…”

Section: Discussionmentioning

confidence: 99%

Quali–Quantitative Characterization of Volatile and Non-Volatile Compounds in Protium heptaphyllum (Aubl.) Marchand Resin by GC–MS Validated Method, GC–FID and HPLC–HRMS2

et al. 2021

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Protium heptaphyllum (Aubl.) Marchand (PH) trees are endemic to the tropical region of South America, mostly Brazil. Antibacterial, antinociceptive, anti-inflammatory, anxiolytic, antidepressant and anti-hyperlipidemic/anti-hypercholesterolemic effects were reported for its resinous exudate Protiumheptaphyllum resin (PHR). This work aims to provide a qualitative and quantitative consistent chemical profiling of the major constituents of this resin and two extracts enriched in acid (acidic triterpene concentrated extract, ATCE) and neutral triterpenes (α and β-amyrin concentrated extract, AMCE). GC–MS/GC–FID was used for volatile terpene fraction, a validated GC–MS method was developed for quantification of neutral α and β-amyrin and HPLC–APCI HRMS2 was used for acidic triterpenes analysis. The chemical investigation reported 29 molecules, including 14 volatile terpenes, 6 neutral triterpenes and 11 acid triterpenes. The most abundant compounds were α-amyrin (251.28 g kg−1, 123.98 g kg−1 and 556.82 g kg−1 in PHR, ATCE and AMCE, respectively), β-amyrin (172.66 g kg−1, 95.39 g kg−1 and 385.58 g kg−1 in PHR, ATCE and AMCE, respectively), 3-oxo-tirucalla-7,24-dien-21-oic acid (80.64 g kg−1, 157.10 g kg−1 and 15.31 g kg−1 in PHR, ATCE and AMCE, respectively) and 3α-hydroxy-tirucalla-8,24-dien-21-oic acid (77.71 g kg−1, 130.40 g kg−1 and 11.64 g kg−1 in PHR, ATCE and AMCE, respectively). Results showed specific enrichment of acidic and neutral triterpenoids in the two respective extracts.

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“…Nonetheless, plants and plant-derived compounds are low-cost and less toxic when compared with conventional treatment. Plants are an established source of novel drug candidates, the majority of existing drugs and phytoleads have their origin in plants (Srivastav et al, 2020). They have also been reported to demonstrate inhibition of Akt protein and modulation of the Akt/mTOR pathway (Nitulescu et al, 2018;Srivastav et al, 2020).…”

Section: Backg Rou N Dmentioning

confidence: 99%

“…Plants are an established source of novel drug candidates, the majority of existing drugs and phytoleads have their origin in plants (Srivastav et al, 2020). They have also been reported to demonstrate inhibition of Akt protein and modulation of the Akt/mTOR pathway (Nitulescu et al, 2018;Srivastav et al, 2020). The anti-neoplastic properties of Azadirachta indica (neem) have been reported (Agrawal et al, 2020), it is been shown to modulate the tumor microenvironments, attenuate the proliferation of tumor cells (Agrawal et al, 2020).…”

Section: Backg Rou N Dmentioning

confidence: 99%

Terpenoids from Azadirachta indica are potent inhibitors of Akt: Validation of the anticancer potentials in hepatocellular carcinoma in male Wistar rats

Akinloye

Lawal

et al. 2020

J. Food Biochem.

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Hepatocellular carcinoma (HCC) is the commonest primary malignancy with poor patient prognosis and a high mortality rate. In this study, phytochemicals characterized from Azadirachta indica were screened against the catalytic site of Akt, and the anticancer potentials of the extracted leads (terpenoids) were determined in hepatocellular carcinoma in male Wistar rats. The lead compounds are terpenoids; hence, the extraction of terpenoids from A. indica. Gas chromatography-mass spectrometry (GCMS) was employed for the characterization of the extract. Diethylnitrosamine (DEN)-induced hepatocellular carcinoma in male Wistar rats were treated with the terpenoids extract. The hit, lupeol demonstrates inhibition of Akt and is a potential drug candidate. The terpenoids extract downregulate Akt mRNA and demonstrated anti-Akt downstream signaling effects; anti-inflammatory, anti-angiogenesis, proapoptotic, and cell cycle arrest, it also demonstrated cellular regeneration, hepatoprotection, antioxidant potentials, and cellular repairs in hepatocellular carcinoma in male Wistar rats. Practical applications Hepatocellular Carcinoma (HCC) is the most common primary malignancy with poor patient prognosis and a high mortality rate. Akt, a serine/threonine kinase is at the crossroad of cell survival, the progression of the cell cycle, cell signaling, cell growth, cell division, and inactivation of pro-apoptotic factors. The inhibition of Akt is an effective therapeutic strategy against HCC. In this study, terpenoids from Azadirachta indica are potent inhibitors of Akt and hitherto demonstrate anticancer potentials. A. indica leaves are readily available globally and more also it is readily cultivated in African and Asia, continents with the highest prevalence of HCC. A. indica terpenoids extract demonstrate anti-HCC potentials and hence should be exploited in this regard.

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Plant secondary metabolites as lead compounds for the production of potent drugs

Cited by 12 publications

References 33 publications

Antitumor Effects of Carvacrol and Thymol: A Systematic Review

Antitumor Effects of Carvacrol and Thymol: A Systematic Review

Quali–Quantitative Characterization of Volatile and Non-Volatile Compounds in Protium heptaphyllum (Aubl.) Marchand Resin by GC–MS Validated Method, GC–FID and HPLC–HRMS2

Terpenoids from Azadirachta indica are potent inhibitors of Akt: Validation of the anticancer potentials in hepatocellular carcinoma in male Wistar rats

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