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Journal : JURNAL FARMASI DAN ILMU KEFARMASIAN INDONESIA

Antimalarial Potential of Fraction 5 from Ethanolic Leaves Extract of Artocarpus Altilis Einstenia Kemalahayati; Hilkatul Ilmi; Agriana Rosmalina Hidayati; Marsih Wijayanti; Lidya Tumewu; Suciati; Achmad Fuad Hafid; Aty Widyawaruyanti
JURNAL FARMASI DAN ILMU KEFARMASIAN INDONESIA Vol. 10 No. 2 (2023): JURNAL FARMASI DAN ILMU KEFARMASIAN INDONESIA
Publisher : Universitas Airlangga

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.20473/jfiki.v10i22023.184-192

Abstract

Background: Artocarpus altilis leaf extract (AAL.E) was separated by VLC, and six fractions were obtained. Fraction 5 (AAL.E.5) showed antimalarial activity with an IC50 value of 3.71 µg/mL. Objective: This study aimed to determine the antimalarial activity of AAL.E.5 subfractions against P. falciparum, the mechanism of action against Plasmodium Falciparum Malate quinone oxidoreductase (PfMQO), and the active substances. Methods: The AAL.E.5 was separated by open-column chromatography and eluted with chloroform-methanol gradient elution in order of increasing polarity. The antimalarial activity of all subfractions was assessed using a lactate dehydrogenase (LDH) assay against P. falciparum and the mechanism of action of the PfMQO enzyme. The profiles of the most active subfractions were analyzed using High-Performance Liquid Chromatography (HPLC). Results: The separation of fraction 5 (AAL.E.5) yielded 11 subfractions (AAL.E.5.1–AAL.E.5.11). Screening antimalarial activity at 10 μg/mL in this subfraction showed that only five subfractions (AAL.E.5.6-AAL. E.5.10) inhibited P. falciparum and two subfractions (AAL.E.5.6 and AAL.E.5.10) inhibited the PfMQO enzyme. Only subfraction 6 (AAL.E.5.6) inhibited both, with IC50 values of 6.609 µg/mL and 20.34 µg/mL. The thin layer chromatography profile of AAL.E.5.6 revealed reddish-orange spots, indicating the presence of flavonoid compounds, and was also presumed from the UV-visible to HPLC chromatogram for band I in the 300 – 400 nm range and band II in the 240–285 nm range. Conclusion: Subfraction 6 has antimalarial activity against P. falciparum and is thought to have a mechanism of action in PfMQO. Based on the TLC, HPLC, and UV-Vis spectra, subfraction 6 was assumed to be a flavonoid.
In Silico Analgesic and Toxicity Analysis of Modified Paracetamol on COX-2 Receptor (PDB ID: 3LN1) Hidayah, Nurul; Lina Permatasari; Agriana Rosmalina Hidayati; Handa Muliasari
JURNAL FARMASI DAN ILMU KEFARMASIAN INDONESIA Vol. 11 No. 3 (2024): JURNAL FARMASI DAN ILMU KEFARMASIAN INDONESIA
Publisher : Universitas Airlangga

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.20473/jfiki.v11i32024.312-324

Abstract

Background: Paracetamol is often used as the main analgesic in Indonesia. The use of more than 4 g/day or a single dose above 10 g can cause hepatotoxicity. This can be overcome by modifying the structure through a computer-aided drug design (CADD) approach, particularly molecular docking, which aims to produce compounds with greater potency and fewer side effects. Objective: This study aimed to determine the analgesic activity and toxicity of paracetamol derivatives modified using the Topliss method. Methods: Analgesic activity was tested by molecular docking of the COX-2 receptor (PDB ID 3LN1) using AutoDock Tool 4.2 and toxicity testing using pkCSM and Protox Online Tool. Results: The results of docking showed that the free binding energy values ​​for test compounds 1 to 5 are -10.59 kcal/mol, -10.17 kcal/mol, -8.79 kcal/mol, -10.01 kcal/mol, and -9.32 kcal/mol, respectively, with corresponding inhibition constants of 17.29 nM, 35.21 nM, 360.88 nM, 46.36 nM, and 146.65 nM. These values are lower than paracetamol, which has a free binding energy of -6.21 kcal/mol and an inhibition constant of 28,043 nM. The results showed that the test compound was more stable in ligand-receptor binding. Toxicity tests showed that all the test compounds and paracetamol belonged to toxicity class IV. The test compound had an LD50 value of 1551 mg/kg, which was higher than that of paracetamol (338 mg/kg), indicating better effectiveness. Conclusions: Compound 2 was predicted to have the best biological activity and potential as an alternative to paracetamol.
Co-Authors Abdillah, Lalu Khairi Achmad Fuad Hafid Achmad Fuad Hafid Agustini, Nur Indah Aini, Siti Rahmatul Aliefman Hakim Amira Amira Amni Hamid Anggit L. Sunarwidhi Anggit Listyacahyani Sunarwidhi Anindiya, Naya Wahyu Anisa Febriani Ariani, Fitri Aryana, Baiq Putri Aty Widyawaruyanti Aty Widyawaruyanti Aulia, Dia Ul Avida In Amy Baiq Ihda Nanda Safriyana Baiq Ridho Amalia Bayani, Faizul Cahyani, Dina Fathia Candra Eka Puspitasari Dedianto Hidajat Devanus lahardo Dewi Suryani Dia Ul Aulia Djoko Agus Purwanto Dyke Gita Wirasisya Dyke Gita Wirasisya Dyke Gita Wirasisya Einstenia Kemalahayati Firman Wicaksana Hafizah, Gina Tasya Rizka Hajrin, Wahida Handa Muliasari Handa Muliasari Haryanto, Wahyu Hidayati, Regina Tria Hidayaturrohman, Achmad Hilkatul Ilmi Hilkatul Ilmi Iman Surya Pratama Iman Surya Pratama Pratama Indah Permata Sari Indra Purnomo Indriani, Zulfia Ika Julia Harpina Kadar Riansyah Khairatun, Laziza Iklima Kurniasih Sukenti Lidya Tumewu Lina Permatasari Lisnasari, Baiq Risky Wahyu Mahacita Andanalusia Mahacita Andanalusia Marsih Wijayanti Maylisa Natalia Corry Muhamad Haikhal Muhammad Amir Hasan Muhammad Robby Rizky Mukhlishah, Neneng Rachmalia Izzatul Muktiali, Abdul Hamid Muliasari, Handa Muthia Cenderadewi, Muthia Narendrani Sasmitaning Edhi Neneng Rachmalia Izzatul Mukhlishah Nisa Isneni Hanifa NURUL HIDAYAH Permatasari, Lina Permatasari, Ni Made Ayu Dinda Pramudya, Muhammad Zaidan Pratama, Iman Surya Pratiwi, Eskarani Tri Prianggawe, Prianggawe Pujiarohman, Pujiarohman Purnomo, Indra Purwitasari, Neny Putri Nuryana Raissa, Talitha Hasna Ramadhan, Muhammad Rafi Bintang Retno Widyowati Riadi, Putri Oktaviati Riesta Primaharinastiti Risnata, Richa Poetri rizki, alpa alfi Rizkika, Adila Safriyana, Baiq Ihda Nanda Sasvania, Anisa Siti Rahmatul Aini Suciati Suciati Suciati Suciati Sukardiman Sukardiman sulistanti, Erly Sunarwidhi, Anggit Listyacahyani suryani, Bunga Tri Widiandani Wahida Hajrin Wardani, Ray Haerul Windah Anugrah Subaidah Wirasisya, Dyke Gita Yayuk Andayani Yunita Yunita Zahra, Nisrina