Lupeol and its derivatives as anticancer and anti-inflammatory agents: Molecular mechanisms and therapeutic efficacy

Li, Kai; Zhang, Xumin; Xie, Long; Deng, Mao; Chen, Huijuan; Song, Jung Soo; Long, Jiaying; Li, Xiaofang; Jia, Luo

doi:10.1016/j.phrs.2020.105373

Cited by 106 publications

(68 citation statements)

References 159 publications

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“…[ 33 ] Although lupeol has been tested against different types of cancers, its mechanism has never been tested against Hep3B cells, particularly the resistant cells. [ 34 ]…”

Section: Discussionmentioning

confidence: 99%

Potential targeting of Hep3B liver cancer cells by lupeol isolated from Avicennia marina

ElDohaji

Fayed

Hamoda

et al. 2021

Archiv der Pharmazie

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Medicinal plants are valuable sources of different active constituents that are known to have important pharmacological activities including anticancer effects. Lupeol, a pentacyclic triterpenoid, present in many medicinal plants, has a wide range of biological activities. Although the anticancer activity of lupeol was reported, the published data are inconsistent and the clear mechanism of action has never been assigned. The current study aims at investigating the anticancer specificity and mechanism of lupeol isolated from Avicennia marina, which grows in the desert of the United Arab Emirates. The compound was purified by chromatography and identified by spectroscopy. Compared with a negative control, lupeol caused significant (p < .001) growth inhibitory activity on MCF‐7 and Hep3B parental and resistant cells by 45%, 46%, 72%, and 35%, respectively. The mechanism of action of lupeol was further explored by measuring its effect on key players in cancer development and progression, BCL‐2 anti‐apoptotic and BAX pro‐apoptotic proteins. Lupeol significantly (p < .01) downregulated BCL‐2 gene expression in parental and resistant Hep3B cells by 33 and 3.5 times, respectively, contributing to the induction of apoptosis in Hep3B cells, whereas it caused no effect on BAX. Furthermore, the immunoblotting analysis revealed that lupeol cleaved the executioner caspase‐3 into its active form. Interestingly, lupeol showed no significant effect on the proliferation of monocytes, whereas it caused an increase in the sub‐G1 population and a reduction in the apoptosis rates of monocytes at 48 and 72 h, indicative of no immuno‐inflammatory responses. Collectively, lupeol can be considered as promising effective and safe anticancer agent, particularly against Hep3B cancer cells.

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“…[ 33 ] Although lupeol has been tested against different types of cancers, its mechanism has never been tested against Hep3B cells, particularly the resistant cells. [ 34 ]…”

Section: Discussionmentioning

confidence: 99%

Potential targeting of Hep3B liver cancer cells by lupeol isolated from Avicennia marina

ElDohaji

Fayed

Hamoda

et al. 2021

Archiv der Pharmazie

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“…These compounds were known for its anticancer property in various malignant neoplasms. In breast cancer, lupeol acts by downregulating the Bcl-2 and bcl-XL protein expression which induces the apoptosis process in breast cancer cell line MCF-7 [69], it also reduces cell migration in non-small cell lung cancer [70,71]. Phytosterols such as Stigmasterol and beta sitosterol showed cytotoxic potential against breast cancer cell line [72]; the stigmasterol reduces the tumor development by activation of protein phosphatase 2A causing apoptosis in EAC induced mice via stimulation of antioxidant enzymes [73].…”

Section: Discussionmentioning

confidence: 99%

Phytochemical Screening, Toxicity Evaluation of Polycarpaea Corymbosa Lamk and Its Effect on Cancer Biomarkers of Ehrlich Ascites Carcinoma-Induced Mice Compared With the Reference Standard Drug 5- Fluorouracil

Palaniswamy

2021

Asian J Pharm Clin Res

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Objective: The current investigation focuses on the study of efficacy of whole plant of Polycarpaea corymbosa Lamk in Ehrlich ascites carcinoma (EAC) inoculated Swiss albino mice. Methods: The whole plant of P. corymbosa Lamk (WPC) was extracted with solvents of increasing polarity and their percentage yields were calculated. The major phytoconstituents present in the plant extracts were determined by standard chemical tests. Tumor was induced in mice by intraperitoneal injection of EAC cells (1×106 cells/mouse). The in vivo antitumor effect of extracts was assessed by monitoring the mean survival time, tumor volume, effect on hematological parameters, determination of lysosome specific cancer markers (cathepsin-D), β-D glucuronidase and acid phosphatase, liver marker enzymes (5’-nuclotidase and lactate dehydrogenase), membrane bound ATPase (Na+/K+ ATPase and Mg2+ ATPase), DNA, and RNA content. Results: The percentage yield obtained were 9.87%w/w, 7.88%w/w, and 16.56% w/w for petroleum ether, ethyl acetate, and ethanol extract, respectively. The phytochemical screenings of those extracts were performed. The order of activity of extracts was ethanol extract > ethyl acetate > petroleum ether. Among the extracts, Ethanol extract of P. corymbosa Lamk. showed a significant increase in life span and decrease in viable cancer cell number and tumor volume. The protective effect of the extract on the hemopoietic system at the dose 200mg∕kg was noted. The alterations in the hematological profile, lysosome-specific cancer markers, liver-specific cancer markers, and membrane-bound ATPases DNA and RNA were restored. Conclusion: The ethanolic extract of P. corymbosa Lamk. possesses in vivo anticancer activity when compared to the tumor control group.

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“…Compound 1 has antiinflammatory, anticancer, antioxidant, and antimicrobial activities. [36][37][38] Meanwhile, compound 2 has shown antihypertensive, antioxidant, anticancer, antiaging, and neuroprotective activities. 39,40 Compound 3 has antiallergic, antifungal, antioxidant, antiplasmodial, and ovicidal properties.…”

Section: Antimycobacterial Activitymentioning

confidence: 99%

Antimycobacterial Activity of the Extract and Isolated Compounds From the Stem Bark of Zanthoxylum leprieurii Guill. and Perr.

Oloya

Namukobe

Heydenreich

et al. 2021

Natural Product Communications

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Zanthoxylum leprieurii Guill. and Perr. (Rutaceae) stem bark is used locally in Uganda for treating tuberculosis (TB) and cough-related infections. Lupeol (1), sesamin (2), trans-fagaramide (3), arnottianamide (4), ( S)-marmesinin (5), and hesperidin (6) were isolated from the chloroform/methanol (1:1) extract of Z. leprieurii stem bark. Their structures were elucidated using spectroscopic techniques and by comparison with literature data. Furthermore, the extract and isolated compounds were subjected to antimycobacterial activity. The extract exhibited moderate activity against the susceptible (H37Rv) TB strain, but weak activity against the multidrug resistant (MDR)-TB strain with minimum inhibitory concentrations (MICs) of 586.0 and 1172.0 μg/mL, respectively. Compound 3 (trans-fagaramide) showed significant antimycobacterial activity against the susceptible (H37Rv) TB strain (MIC 6 μg/mL), but moderate activity against the MDR-TB strain (MIC 12.2 μg/mL). Compounds 2, 5, 6, and 1 showed moderate activities against the susceptible (H37Rv) strain (MIC 12.2-98.0 μg/mL) and moderate to weak activities against the MDR-TB strain (MIC 24.4-195.0 μg/mL). This study reports for the first time the isolation of compounds 1 to 6 from the stem bark of Z leprieurii. trans-Fagaramide (3) may present a vital template in pursuit of novel and highly effective TB drugs.

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Lupeol and its derivatives as anticancer and anti-inflammatory agents: Molecular mechanisms and therapeutic efficacy

Cited by 106 publications

References 159 publications

Potential targeting of Hep3B liver cancer cells by lupeol isolated from Avicennia marina

Potential targeting of Hep3B liver cancer cells by lupeol isolated from Avicennia marina

Phytochemical Screening, Toxicity Evaluation of Polycarpaea Corymbosa Lamk and Its Effect on Cancer Biomarkers of Ehrlich Ascites Carcinoma-Induced Mice Compared With the Reference Standard Drug 5- Fluorouracil

Antimycobacterial Activity of the Extract and Isolated Compounds From the Stem Bark of Zanthoxylum leprieurii Guill. and Perr.

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