Investigation of Lupeol as Anti-Melanoma Agent: An In Vitro-In Ovo Perspective

Bociort, Flavia; Macaşoi, Ioana; Marcovici, Iasmina; Motoc, Andrei Gheorghe Marius; Grosu, Cristina; Pînzaru, Iulia; Petean, Crina; Avram, Ștefana; Dehelean, Cristina

doi:10.3390/curroncol28060425

Cited by 9 publications

(5 citation statements)

References 48 publications

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“…Bociort et al evaluated lupeol as an anti-melanoma agent, noting that the compound induced morphological changes in A375 cancer cell lines at concentrations of 30 and 50 mM. As a result of these concentrations, rounding of cells was observed, which indicates the onset of cell death [3].…”

Section: Resultsmentioning

confidence: 99%

Evaluation of Oleanolic Acid, Doxorubicin and Their Association in the Treatment of Melanoma: Enhanced Efficacy and Antiangiogenic Potential

PUENEA

2023

FARMACIA

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As one of the most aggressive types of skin cancer, melanoma, remains a challenging malignancy to treat, necessitating continued research for more effective therapeutic approaches. This study examined the impact of oleanolic acid and doxorubicin individually and in combination on the viability of cells, morphological changes and antiangiogenic properties. Oleanolic acid, doxorubicin and a combination of both were used to treat melanoma cells -A375. The viability of the cells was assessed using MTT assay, and phase-contrast microscopy was used to observe morphological changes. To assess apoptotic alterations in the nuclei, Hoechst 33342 staining was applied to the nuclei. The antiangiogenic potential was evaluated using the hen's egg chorioallantoic membrane as a biological model. Cell viability was significantly reduced by both oleanolic acid and doxorubicin while cell morphology revealed distinct changes in shape and adherence, which are common to apoptotic processes. Apoptosis was confirmed as the underlying mechanism by the presence of condensation and fragmentation of the nuclei. It should be noted that the combination of oleanolic acid and doxorubicin had a more pronounced effect on cell viability and morphological changes associated with apoptosis. Furthermore, the assessment of antiangiogenic potential demonstrated that oleanolic acid, along with doxorubicin, was capable to inhibit the formation of new blood vessels. According to this study, both oleanolic acid and doxorubicin exhibit promising anti-melanoma properties, including a reduction in cell viability and induction of apoptosis. These effects are enhanced by their association, indicating a potential synergistic effect. A valuable insight has been gained into the therapeutic potential of combining oleanolic acid and doxorubicin in the treatment of melanoma in the present study. Efforts should be made to elucidate the underlying mechanisms of action of this combination as well as evaluate its safety and efficacy in preclinical and clinical settings to improve therapeutic outcomes. antiangiogenic a demonstrat că acidul oleanolic, împreună cu doxorubicina, a fost capabil să inhibe formarea de noi vase de sânge. Potrivit acestui studiu, atât acidul oleanolic, cât și doxorubicina prezintă proprietăți anti-melanom promițătoare, inclusiv o reducere a viabilității celulare și inducerea apoptozei. Aceste efecte sunt sporite de asocierea lor, indicând un potențial efect sinergic. În studiul de față s-a obținut o perspectivă valoroasă asupra potențialului terapeutic al combinării acidului oleanolic cu doxorubicina în tratamentul melanomului. Trebuie depuse eforturi pentru a elucida mecanismele de acțiune de bază ale acestei combinații, precum și pentru a evalua siguranța și eficacitatea acesteia în medii preclinice și clinice pentru a îmbunătăți rezultatele terapeutice.

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Section: Resultsmentioning

confidence: 99%

Evaluation of Oleanolic Acid, Doxorubicin and Their Association in the Treatment of Melanoma: Enhanced Efficacy and Antiangiogenic Potential

PUENEA

2023

FARMACIA

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“…Major phytosterols identifed are lup-20(29)-en-3-ol acetate (43.71), cyclolanost-24-en-3-ol acetate (19.98), β-amyrin (14.21), α-amyrin (7.30), betulin (3.52), and urs-12-en-28oic acid (2.43). Lupeol and its esters exhibited antioxidant [95,96], hypotensive [97,98], antihyperglycemic [99,100], antidyslipidemic [100], potent anti-infammatory activity [101,102], antiangiogenic [103], anticancer [104], and nephroprotective [105] activities. Lupeol and lupeol linoleate are also demostrated protective role against hepatic lipemicoxidative injury and lipoprotein peroxidation in experimental hypercholesterolemia [106].…”

Section: Discussionmentioning

confidence: 99%

Phytochemical Analysis, In Vitro Free Radical Scavenging, and LDL Protective Effects of Different Solvent Fractions of Calotropis procera (R.) Br. Root Bark Extract

Kyada,

Rahamathulla,

Santani

et al. 2023

Journal of Food Biochemistry

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In the present study, the methanolic extract of Calotropis procera root bark was subjected to solvent-solvent partitioning using n-hexane fraction (HF), dichloromethane fraction (DMF), ethyl acetate fraction (EAF), and methanol fraction (MF). The resultant fractions were tested for antioxidant activity using in vitro radical scavenging assay. Preliminary phytochemical investigation revealed the presence of varying proportions of secondary metabolites in solvent fractions such as glycosides, flavonoids, triterpenoids, sterols, and polyphenolic compounds. The total phenolic content of EAF was 25.7 ± 3.12 mg TAE/g followed by 19.05 ± 3.29 mg TAE/g in DMF. The total flavonoid content was 13.69 ± 1.74 mg QUE/g in DMF and 11.4 ± 1.88 mg QUE/g in EAF. The EAF showed significant radical-scavenging activity against 1,1-diphenyl-2-picrylhydrazyl (DPPH, IC50 = 369.87 μg/mL), nitric oxide (IC50 = 317.46 μg/mL), hydrogen peroxide (H2O2 , IC50 = 396.85 μg/mL), and hydroxyl radicals (IC50 = 195.39 μg/mL). DMF was most effective in scavenging superoxide radicals (IC50 = 679.60 μg/mL), while greater metal chelating activity was exhibited by MF (IC50 = 614.73 μg/mL). Moreover, the total antioxidant activity for EAF was found to be 94.14 ± 9.114 mg AAE followed by DMF (68.10 ± 8.78 mg AAE). EAF also significantly reduced the formation of thiobarbituric acid reactive substances in a dose-dependent manner in CuSO4. The observed antioxidant effect might be attributed to the presence of secondary metabolites. Subsequent GC-MS analysis of EAF confirmed the presence of lupeol, α-amyrin, β-amyrin, and ursolic acid. The current investigation reveals that the high polyphenolic and antioxidant pentacyclic triterpenes in EAF of C. procera root bark methanol extract correlates with its good antioxidant activity and can provide protection against free radicals-induced damage in a variety of chronic health conditions.

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“…In addition, tanshinone IIA analog , kolaflavanone (KLF) (Alrazi et al, 2021), eugenol (Abdalla et al, 2020), and millepachine (Yan F et al, 2021), considered as potentially potent microtubule inhibitors, inhibit cell growth by interfering with the formation of microtubules. Epigallocatechin-3-gallate (EGCG) (Chen et al, 2019), lupeol (LUP) (Bociort et al, 2021), saikosaponin A (Cheng and Ying, 2021), and ononin (Gong et al, 2021) can significantly supress tumor angiogenesis.…”

Section: Discussionmentioning

confidence: 99%

Research Status and Hotspots of Anticancer Natural Products Based on the Patent Literature and Scientific Articles

Shen

2022

Front. Pharmacol.

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Background: The patent literature contains a large amount of information on the internal state of current industrial technologies that are not available in other literature studies. Scientific articles are the direct achievements of theoretical research in this field and can reveal how current theories in basic research have developed. In this study, the progress and status of natural anticancer products in this field were summarized, and the research hotspots were explored through the analysis of the relevant patent literature and scientific articles.Methods: Patent data were retrieved from the incoPat patent retrieval database, and paper data were retrieved from the Web of Science core set and PubMed. GraphPad Prism 8, Microsoft Excel 2010, and CiteSpace 5.8.R3 were used to perform visual processing. The analyzed patent literature includes the patent applicant type, country (or region), and technical subject. The analyzed scientific article includes academic groups, subject areas, keyword clustering, and burst detection.Results: A total of 20,435 patent families and 38,746 articles were collected by 4 January 2022. At present, antitumor drugs derived from natural products mainly include 1) apoptosis inducers such as curcumin, gallic acid, resveratrol, Theranekron D6, and gaillardin; 2) topoisomerase inhibitors such as camptothecins, scaffold-hopped flavones, podophyllotoxin, oxocrebanine, and evodiamine derivatives; 3) telomerase inhibitors such as camptothecin and isoquinoline alkaloids of Chelidonium majus, amentoflavone, and emodin; 4) microtubule inhibitors such as kolaflavanone, tanshinone IIA analog, eugenol, and millepachine; 5) immunomodulators such as fucoidan, myricetin, bergapten, and atractylenolide I; 6) tumor microenvironment regulators such as beta-escin and icaritin; 7) multidrug resistance reversal agents such as berberine, quercetin, and dihydromyricetin; and 8) antiangiogenic and antimetastatic agents such as epigallocatechin-3-gallate, lupeol, ononin, and saikosaponin A.Conclusion: Anticancer natural product technology was introduced earlier, but the later development momentum was insufficient. In addition, scientific research activities are relatively closed, and technical exchanges need to be strengthened. Currently, the development of medicinal plants and the research on the anticancer mechanism of natural active products are still research hotspots, especially those related to immune checkpoints, essential oils, and metastatic cancer. Theories of traditional Chinese medicine (TCM), such as “restraining excessiveness to acquire harmony,” “same treatment for different diseases,” “Meridian induction theory,” and “Fuzheng Quxie,” have important guiding significance to the research of anticancer mechanisms and the development of new drugs and can provide new ideas for this process.Systematic Review Registration: [https://sourceforge.net/projects/citespace/], identifier [000755430500001].

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Investigation of Lupeol as Anti-Melanoma Agent: An In Vitro-In Ovo Perspective

Cited by 9 publications

References 48 publications

Evaluation of Oleanolic Acid, Doxorubicin and Their Association in the Treatment of Melanoma: Enhanced Efficacy and Antiangiogenic Potential

Evaluation of Oleanolic Acid, Doxorubicin and Their Association in the Treatment of Melanoma: Enhanced Efficacy and Antiangiogenic Potential

Phytochemical Analysis, In Vitro Free Radical Scavenging, and LDL Protective Effects of Different Solvent Fractions of Calotropis procera (R.) Br. Root Bark Extract

Research Status and Hotspots of Anticancer Natural Products Based on the Patent Literature and Scientific Articles

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