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Indonesian Journal of Medical Chemistry and Bioinformatics

Abstract

Background: Breast cancer remains a major global health burden. Particularly in Indonesia, limitations of conventional chemotherapy, such as severe side effect, toxicity, and high cost, indicating the necessitate the development of alternative therapeutic agents. Peperomia pellucida, a medicinal plant rich in bioactive phytochemicals, has shown promising anticancer potential; however, its cytotoxic activity against MCF-7 breast cancer cells and the influence of solvent polarity remains underexplored. This study aimed to evaluate the cytotoxic effects of P. pellucida leaf extracts which are prepared using different polarity of solvents (ethanol, ethyl acetate, and n-hexane).

Method: Dried leaf powder of P. pellucida was extracted via maceration, and the resulting extracts were tested against MCF-7 cells using the MTT assay. Cells were exposed to concentrations ranging from 3.125 µg/mL to 400 µg/mL, and cytotoxicity was expressed as IC₅₀ values derived from linear regression analysis.

Results: The ethanol extract exhibited the the strongest cytotoxic activity (IC₅₀ = 10.68 µg/mL), followed by the ethyl acetate extract (IC50=17.81µg/mL), while the n-hexane extract showed weak activity (IC50 = 62.73 µg/mL). The superior activity of the ethanol extract is attributed to its broader phytochemical profile, including flavonoids, alkaloids, tannins, and triterpenoids, which may act synergistically to induce apoptosis and inhibit proliferation.

Conclusion: P. pellucida demonstrates solvent-dependent cytotoxic activity, with ethanol extract showing the highest potential as a candidate for breast cancer therapy. Further studies are required to elucidate its molecular mechanisms.

Bahasa Abstract

Latar belakang: Kanker payudara masih menjadi masalah kesehatan global. Khususnya di Indonesia, keterbatasan kemoterapi konvensional, seperti efek samping yang berat, toksisitas yang tinggi, dan biaya yang mahal, menunjukkan perlunya pengembangan agen terapeutik alternatif. Peperomia pellucida, tanaman obat yang kaya akan senyawa fitokimia bioaktif, telah menunjukkan potensi antikanker yang menjanjikan. Namun, aktivitas sitotoksiknya terhadap sel kanker payudara MCF-7 serta pengaruh polaritas pelarut masih belum banyak diteliti. Penelitian ini bertujuan untuk mengevaluasi efek sitotoksik ekstrak daun P. pellucida yang disiapkan menggunakan pelarut dengan polaritas berbeda (etanol, etil asetat, dan n-heksana). 

Metode: Serbuk daun kering P. pellucida diekstraksi melalui metode maserasi, dan ekstrak yang dihasilkan diuji terhadap sel MCF-7 menggunakan metode MTT. Sel dipaparkan ekstrak P.pellucida pada berbagai konsentrasi mulai dari 3,125 µg/mL hingga 400 µg/mL, dan aktivitas sitotoksik dinyatakan sebagai nilai IC₅₀ yang diperoleh dari analisis regresi linier.

Hasil: Ekstrak etanol menunjukkan aktivitas sitotoksik paling kuat (IC₅₀ = 10,68 µg/mL), diikuti oleh ekstrak etil asetat (IC₅₀ = 17,81 µg/mL), sedangkan ekstrak n-heksana menunjukkan aktivitas paling lemah (IC₅₀ = 62,73 µg/mL). Aktivitas sitotoksik tertinggi pada ekstrak etanol dikaitkan dengan profil fitokimianya yang lebih luas, meliputi kandungan flavonoid, alkaloid, tanin, dan triterpenoid, yang berpotensi bekerja secara sinergis dalam menginduksi apoptosis dan menghambat proliferasi sel.    

Simpulan: P. pellucida menunjukkan aktivitas sitotoksik yang bergantung pada jenis pelarut, dengan ekstrak etanol memiliki potensi tertinggi sebagai kandidat bagi terapi kanker payudara. Penelitian lebih lanjut diperlukan untuk mengungkap mekanisme molekuler yang mendasarinya.

References

1.        Bhatt, S.; Gething, P.W.; Brady, O.J.; Messina, J.P.; Farlow, A.W.; Moyes, C.L.; Drake, J.M.; Brownstein, J.S.; Hoen, A.G.; Sankoh, O.; et al. The Global Distribution and Burden of Dengue. Nature 2013, 496, 504–507, doi:10.1038/nature12060.

2.        World Health Organization Dengue and Severe Dengue ; Geneva, 2020;

3.        Achee, N.L.; Gould, F.; Perkins, T.A.; Reiner, R.C.; Morrison, A.C.; Ritchie, S.A.; Gubler, D.J.; Teyssou, R.; Scott, T.W. A Critical Assessment of Vector Control for Dengue Prevention. PLoS Negl. Trop. Dis. 2015, 9, e0003655, doi:10.1371/journal.pntd.0003655.

4.        Brady, O.J.; Golding, N.; Pigott, D.M.; Kraemer, M.U.G.; Messina, J.P.; Reiner Jr, R.C.; Scott, T.W.; Smith, D.L.; Gething, P.W.; Hay, S.I. Global Temperature Constraints on Aedes Aegypti and Ae. Albopictus Persistence and Competence for Dengue Virus Transmission. Parasit. Vectors2014, 7, 338, doi:10.1186/1756-3305-7-338.

5.        Bowman, L.R.; Donegan, S.; McCall, P.J. Is Dengue Vector Control Deficient in Effectiveness or Evidence?: Systematic Review and Meta-Analysis. PLoS Negl. Trop. Dis. 2016, 10, e0004551, doi:10.1371/journal.pntd.0004551.

6.        Maciel-de-Freitas, R.; Avendanho, F.C.; Santos, R.; Sylvestre, G.; Araújo, S.C.; Lima, J.B.P.; Martins, A.J.; Coelho, G.E.; Valle, D. Undesirable Consequences of Insecticide Resistance Following Aedes Aegypti Control Activities Due to a Dengue Outbreak. PLoS One 2014, 9, e92424, doi:10.1371/journal.pone.0092424.

7.        Ranson, H.; Lissenden, N. Insecticide Resistance in African Anopheles Mosquitoes: A Worsening Situation That Needs Urgent Action to Maintain Malaria Control. Trends Parasitol. 2016, 32, 187–196, doi:10.1016/j.pt.2015.11.010.

8.        Mostafalou, S.; Abdollahi, M. Pesticides and Human Chronic Diseases: Evidences, Mechanisms, and Perspectives. Toxicol. Appl. Pharmacol.2013, 268, 157–177, doi:10.1016/j.taap.2013.01.025.

9.        Mnif, W.; Hassine, A.I.H.; Bouaziz, A.; Bartegi, A.; Thomas, O.; Roig, B. Effect of Endocrine Disruptor Pesticides: A Review. Int. J. Environ. Res. Public Health 2011, 8, 2265–2303, doi:10.3390/ijerph8062265.

10.       Isman, M.B. Botanical Insecticides, Deterrents, and Repellents in Modern Agriculture and an Increasingly Regulated World. Annu. Rev. Entomol.2006, 51, 45–66, doi:10.1146/annurev.ento.51.110104.151146.

11.       Bioactivity of Sweet Flag (Acorus Calamus Linnaeus) Essential Oils against Spodoptera Litura Fabricius (Lepidoptera: Noctuidae). J. Trop. Life Sci. 2016, 6, 86–90, doi:10.11594/jtls.06.02.04.

12.       Rajput, S.B.; Tonge, M.B.; Karuppayil, S.M. An Overview on Traditional Uses and Pharmacological Profile of Acorus Calamus Linn. (Sweet Flag) and Other Acorus Species. Phytomedicine 2014, 21, 268–276, doi:10.1016/j.phymed.2013.09.020.

13.       Senthilkumar, A.; Venkatesalu, V. Larvicidal Potential of Acorus Calamus L. Essential Oil against Filarial Vector Mosquito Culex Quinquefasciatus (Diptera: Culicidae). Asian Pac. J. Trop. Dis. 2012, 2, 324–326, doi:10.1016/S2222-1808(12)60070-X.

14.       Benelli, G.; Mehlhorn, H. Declining Malaria, Rising of Dengue and Zika Virus: Insights for Mosquito Vector Control. Parasitol. Res. 2016, 115, 1747–1754, doi:10.1007/s00436-016-4971-z.

15.       Zhao, Y.; Li, J.; Cao, G.; Zhao, D.; Li, G.; Zhang, H.; Yan, M. Ethnic, Botanic, Phytochemistry and Pharmacology of the Acorus L. Genus: A Review. Molecules 2023, 28, doi:10.3390/molecules28207117.

16.       Hemingway, J.; Hawkes, N.J.; McCarroll, L.; Ranson, H. The Molecular Basis of Insecticide Resistance in Mosquitoes. Insect Biochem. Mol. Biol.2004, 34, 653–665, doi:10.1016/j.ibmb.2004.03.018.

17.       Liu, N.; Li, M.; Gong, Y.; Liu, F.; Li, T. Cytochrome P450s--Their Expression, Regulation, and Role in Insecticide Resistance. Pestic. Biochem. Physiol. 2015, 120, 77–81, doi:10.1016/j.pestbp.2015.01.006.

18.       Trott, O.; Olson, A.J. AutoDock Vina: Improving the Speed and Accuracy of Docking with a New Scoring Function, Efficient Optimization, and Multithreading. J. Comput. Chem. 2010, 31, 455–461, doi:10.1002/jcc.21334.

19.       Liu, Y.; Yang, X.; Gan, J.; Chen, S.; Xiao, Z.-X.; Cao, Y. CB-Dock2: Improved Protein-Ligand Blind Docking by Integrating Cavity Detection, Docking and Homologous Template Fitting. Nucleic Acids Res. 2022, 50, W159–W164, doi:10.1093/nar/gkac394.

20.       WG, B. Chapter 5: Insecticide Resistance Monitoring; Microplate Enzyme Activity Assays. In:            Benedict, M.Q. (Ed.), Methods in Anopheles Research, 4th Ed; 4th ed.; Centers for Disease Control and            Prevention: Atlanta, 2014;

21.       Balmert, N.J.; Rund, S.S.C.; Ghazi, J.P.; Zhou, P.; Duffield, G.E. Time-of-Day Specific Changes in Metabolic Detoxification and Insecticide Resistance in the Malaria Mosquito Anopheles Gambiae. J. Insect Physiol. 2014, 64, 30–39, doi:10.1016/j.jinsphys.2014.02.013.

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