In Vitro and in Silico Analysis of Antilipase, Antioxidant, and Optimization of Granule Effervescent from Peronema canescens Jack
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Abstract
Obesity results from prolonged energy imbalance, with anti-obesity treatment targeting pancreatic lipase inhibition. Peronema canescens Jack. (PC) known as Sungkai, has traditionally been used to treat various ailments. This study aimed to assess PC antioxidant and antilipase activities and optimize effervescent granule formulations. Phytochemical screening and thin-layer chromatography (TLC) were performed, followed by antioxidant analysis using 2,2-diphenyl-1-picrylhydazyl (DPPH) and pancreatic antilipase activity, using the p-NPB substrate, were employed. The ethanol fraction of PC demonstrated potent antioxidant activity (IC50 = 47.27 mg/mL), while the insoluble fraction showed the highest pancreatic antilipase activity (67.65%). Gas chromatography-mass spectrometry (GC-MS) identified active compounds, including dimethyl tetracycline, 2-methoxy-5H-indolo[2,3-b] quinoxaline, and trilaurin, with molecular docking study indicating dimethyl tetracycline was the most effective antilipase candidate, binding to the pancreatic receptor (PDB ID: 1LPB). This compound also met Lipinski’s Rule of Five and ADMET (Absorption, Distribution, Metabolism, Excretion, and Toxicity), suggesting favorable pharmacokinetics and safety. Evaluation of effervescent granules included angle of repose, bulk density, and tapped density. Optimization of tartaric and citric acid concentration using Design Expert 13 yielding two optimal formulas: Formula 1 with 13.16% tartaric acid and 0.84% citric acid, and Formula 2 with 13.21% tartaric acid and 0.80% citric acid. PC leaves have the potential to be an antioxidant and anti-obesity and can be developed into effervescent formula.
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References
1. Ministry of Health RI. Riskesdas 2018. Ministry of Health RI. 2018;53(9):1689–1699.
Liu TT, Liu XT, Chen QX, Shi Y. Lipase Inhibitors for Obesity: A Review. Biomed and Pharm. 2020;128(110314): 1-9.
Ladeska V, Elya B, Hanafi M, Kusmardi, Rohmat SS. Pharmacognostic Evaluation and Antioxidant Activities of Tetracera indica (Christm. and Panz.) Merr. Hayati. 2024;31(5):836–853.
Romiti GF, Corica B, Raparelli V, Basili S, Cangemi R. The interplay between antioxidants and the immune system: A promising field, still looking for answers. Nutrients. 2020;12(6):10–13.
5. Li S, Pan J, Hu X, Zhang Y, Gong D, Zhang G. Kaempferol inhibits the activity of pancreatic lipase and its synergistic effect with Orlistat. J Funct Foods. 2020;72(104041) : 1-11.
6. Douglas IJ, Langham J, Bhaskaran K, Brauer R, Smeeth L. Orlistat and the risk of acute liver injury: Self controlled case series study in UK Clinical Practice Research Datalink. British Med J. 2013;346(7906):1–9.
Rahardhian MRR, Susilawati Y, Sumiwi A, Muktiwardoyo M, Muchtaridi M, Sumiwi SA. A Review Of Sungkai (Peronema Canescens): Traditional Usage, Phytoconstituent, And Pharmacological Activities. Int J. App Pharm. 2022;14(Special issue 5):15–23.
Chike-Ekwughe A, John-Africa LB, Adebayo AH, Ogunlana OO. Evaluation of the In vitro and In silico Pancreatic Lipase Inhibitory Activity of Ethanol Leaf Extract of Tapinanthus cordifolius and its Effect on Oral Glucose Tolerance in Mice. Trop J Nat Prod Res. 2024;8(8):8168–8175.
Rahardhian MRR, Susilawati Y, Musfiroh I, Febriyanti RM, Muchtaridi, Sumiwi SA. In Silico Study of Bioactive Compounds From Sungkai (Peronema Canescens) As Immunomodulator. Int J. App Pharm. 2022;14(Special Issue 4):135–141.
Indriastuti M, Astuti AF, Anna L Yusuf, Akbar F, Kurnia R R. Optimization of Formula Preparation of Effervescent Granules of Moringa Leaf Extract (Moringa oleifera L.). Med Sains : JIK. 2023;8(2):519–528.
Yang HY, Tae J, Seo YW, Kim YJ, Im HY, Choi GD. Novel pyrimidoazepine analogs as serotonin 5-HT2A and 5-HT 2C receptor ligands for the treatment of obesity. Eur J Med Chem. 2013;63:558–569.
Dedic N, Wang L, Hajos-Korcsok E, Hecksher-Sørensen J, Roostalu U, Vickers SP. TAAR1 agonists improve glycemic control, reduce body weight and modulate neurocircuits governing energy balance and feeding. Mol Metab. 2024;80 (101883): 1-14.
13. Suharsanti R, Wahyuono S, Yuniarti N, Astuti P. Molecular Docking of Lipase Inhibitory Activities , Pharmacokinetics and Toxicity Prediction of Chemical Constituents from Curcuma aeruginosa Roxb Rhizome. Int J. Pharm Res and App. 2024;9(2):162–174.
14. Rahardhian MRR, Suharsanti R, Sugihartini N, Lukitaningsih E. In vitro assessment of total phenolic, total flavonoid and sunscreen activities of crude ethanolic extract of belimbing wuluh (Averrhoa bilimbi) fruits and leaves. J. Glob Pharm Tech. 2019;11(4):308–313.
15. Syofyan, S, Almahdy, A, Wulandari, A, Alen, Y, Diliarosta, S, Kurniawan, H, Noverial, N, Putra, P.P, Dillasamola, D. Effects of Ethanol Extract of Sungkai (Peronema canescens Jack.) on Fertility of Female Wistar Mice (Mus musculus L.). Trop J Nat Prod Res. 2023;7(5):2863–2866.
16. Suharsanti R, Sugihartini N, Lukitaningsih E, Rahardhian MRR. Effect of Different Solvent on Total Phenolic, Total Flavonoid, and Sun Protection Factor of Belimbing Wuluh (Averrhoa bilimbi linn.) Fruits Fraction. J. Glob Pharm Tech. 2019;11(1):154–162.
17. Suharsanti R, Sugihartini N, Lukitaningsih E, Rahardhian MRR. Potency Of Belimbing Wuluh (Averrhoa Bilimbi) As Antioxidat And Tyrosinase Inhibitor For Skin Whitening Product. J. Pharm Res. 2019;8(4):151–154.
18. 2.Liu TT, Liu XT, Chen QX, Shi Y. Lipase Inhibitors for Obesity: A Review. Biomed and Pharm. 2020;128(110314): 1-9.
19. Falodun A, Siraj R, Choudhary MI. GC-MS Insecticidal Leaf essential oil of P. staudtii Hutch and Dalz (Icacinaceae). Trop J. Pharm Res. 2009; 82:139-143.
20. Puspitasari YE, Alfikri MA, Sitanggang R, Tambunan JE, Hardoko H. In Silico Analysis of Phenolic Compounds from Ceriops decandra Griff. Leaves and Molecular Interaction as Anti Diabetes. Sci and Tech Ind. 2023;8(4):542–553.
21. Molyneux P. The Use of the Stable Free Radical Diphenylpicryl-hydrazyl (DPPH) for Estimating Antioxidant Activity. Songkla J. Sci and Tech. 2004, 26(2) : 211-219.
22. Alias N, Leow TC, Ali MSM, Tajudin AA, Salleh AB, Zaliha RN, Rahman RA. Anti-obesity Potential of Selected Tropical Plants via Pancreatic Lipase Inhibition. Adv Obes Weight Manag Control. 2017;6(4): 122-131.
23. Halliwell B, Gutteridge JMC. Free Radicals in Biology and Medicine. Free Radicals in Bio and Med. 2015
24. Fernández A, Madrigal-Santillán E, Bautista M, Esquivel-Soto J, Morales-González Á, Esquivel-Chirino C. Inflammation, oxidative stress, and obesity. Int J Mol Sci. 2011;12(5):3117–3132.
25. Suharsanti, Wahyuono S, Yuniarti N, Astuti P. Antioxidant Activity and Pancreatic Lipase Inhibition of Curcuma aeruginosa Roxb Rhizome Fractions. J. Bio. 2024;9(11):228–243.
26. Shah RB, Tawakkul MA, Khan MA. Comparative Evaluation of flow for pharmaceutical powders and granules. AAPS Pharm Sci Tech. 2008;9(1):250–258.
27. Rani KC, Parfati N, Muarofah D, Sacharia SN. Meniran (Phyllanthus niruri L.) Herbal Effervescent Granule Formulation with Variations of Suspending Agent Xanthan Gum, CMC-Na, and Combination CMC-Na-Microcrystalline Cellulose RC- 591. J. Sci Pharm.and Clin. 2020;7(1):39-51.
28. Aulton M. Pharmaceutics: the Science of Dosage Form Design. 2nd ed. Edinburgh: Churchill Livingstone; 2002.
29. Lee, R. E. Effervescent Tablets : Key Facts About A Unique, Effective Dossage Form. CSC Publishing; 2004.
30. Mutiah R, Briliana MSD, Ahmad ARA, Fauziyah B, Janaloka NA, Suryadinata A. Network Pharmacology and Component Analysis Integrated Study to Uncovers the Molecular Mechanisms of Lansium parasiticum Bark Extract in Colon Cancer Treatment. Sci and Tech Ind. 2024;9(2):314–324.
31.Okolie NP, Falodun A, Oluseyi D. Evaluation of the Antioxidant Activity of Root Extract of Pepper Fruit (Dennetia Tripetala), and It’s Potential for the Inhibition of Lipid Peroxidation. Afr J. of Trad Compl and Altern Med. 2014;11(3):221–227.