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The Journey of Natural Products: From Isolation Stage to Drug’s Approval in Clinical Trials Yehezkiel Steven Kurniawan; Tantiana Indriani; Hanif Amrulloh; Langit Cahya Adi; Arif Cahyo Imawan; Krisfian Tata Aneka Priyangga; Ervan Yudha
Bioactivities Vol. 1 No. 2 (2023): Bioactivities
Publisher : Pandawa Institute

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.47352/bioactivities.2963-654X.190

Abstract

Nature serves as an excellent inspiration for researchers in the fields of chemistry and medicine. Terrestrial or marine organisms produce billions of natural products with unique chemical and physical properties. Some of them have been used in traditional therapy for specific diseases since ancient times. Although their exact chemical structures have yet to be elucidated clearly in that time, investigations in medicinal chemistry have been well documented. Furthermore, utilizing natural products in drug design and development offers advantages such as high biocompatibility, low toxicity, fewer side effects, wide bioactivities, and large structure diversity. Nowadays, rational drug research using computer-aided drug design is well established to cut the long way of drug discovery and overcome the resistance cases and the increment in the number of active patients. This review will highlight some natural products to comprehensively understand their journey from unknown natural products, isolation, purification, characterization, in silico evaluation, bioactivity screening assay, drug modifications, in vitro investigation, in vivo examination, and clinical trial.
Fight for Cancer Diseases using Natural Compounds and Their Semisynthetic Derivatives Yehezkiel Steven Kurniawan; Kasta Gurning; Iksen Iksen; Ahmad Bikharudin
Bioactivities Vol. 2 No. 2 (2024): Bioactivities
Publisher : Pandawa Institute

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.47352/bioactivities.2963-654X.221

Abstract

Cancer stands as one of the deadliest diseases afflicting contemporary human societies, encompassing over 100 distinct forms, including oral, salivary glands, oropharynx, nasopharynx, hypopharynx, colorectal, liver, pancreas, lung, skin, breast, cervix, ovary, prostate, kidney, brain, thyroid, and leukemia cancers. At the cellular level, the uncontrolled growth of cancerous cells can disrupt the body's normal functions. Chemotherapy, a widely recognized cancer treatment, utilizes anticancer agents to target specific cancer cell lines effectively. Natural compounds are favored for their compatibility with the body, minimal harm to healthy cells, and easy extraction from natural sources. These natural compounds and their derivatives hold promise for cancer therapy, boasting diverse structural and pharmacological characteristics. Additionally, chemical modifications can enhance their anticancer properties. This review explores the anticancer potential of terpenoids, flavonoids, alkaloids, xanthones, and epoxides, as well as elucidates their molecular mechanisms, such as their antiproliferative, apoptotic, antiangiogenic, and antimetastatic actions. Furthermore, the effect of the functional group on the anticancer activity through the structure-activity relationship will be discussed in detail, supported by molecular docking and molecular dynamic simulations. Combining experimental in vitro and in vivo assays with computational in silico assays significantly helps us understand how we shall fight cancer diseases in the modern era.
Evaluation of The Anticancer Activity of Hydroxyxanthones Against Human Liver Carcinoma Cell Line Yehezkiel Steven Kurniawan; Nela Fatmasari; Jumina Jumina; Harno Dwi Pranowo; Eti Nurwening Sholikhah
Journal of Multidisciplinary Applied Natural Science Vol. 4 No. 1 (2024): Journal of Multidisciplinary Applied Natural Science
Publisher : Pandawa Institute

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.47352/jmans.2774-3047.165

Abstract

Nowadays, cancer is one of the most fatal diseases in developed and developing countries. Therefore, it is an urgent need to find more effective anticancer drugs among the recent commercially available standard drugs. Xanthone derivatives have been researched as anticancer drugs due to their ease of synthesis and structure modification, as well as their excellent anticancer activity. In this work, the in vitro anticancer activity of hydroxyxanthones against the human liver carcinoma cell line (HepG2) was evaluated. Among the twenty-two hydroxyxanthones, 1,3,6,8-tetrahydroxyxanthone was found as the most active anticancer agent with an IC50 value of 9.18 μM, which was better than doxorubicin as the standard drug. From the molecular docking studies against topoisomeraseIIα and two c-KIT protein kinases, 1,3,6,8-tetrahydroxyxanthone yielded strong binding energy in a range of -25.48 to -30.42 kJ/mol. The 1,3,6,8-tetrahydroxyxanthone could bind on the active site of these protein receptors through hydrogen bonds with key amino acid residues (Glu640, Cys673, Gln767, Met769, Asp810, and Asp831), as well as nitrogen bases (Adenine12 and Guanine13), thus leading to the death of HepG2 cancer cells through the apoptosis mechanism.
Catalytic Reduction of 4-Nitrophenol and Methylene Blue with Silver Nanoparticles Decorated with Drymoglossum piloselloides Extract Awalul Fatiqin; Rokiy Alfanaar; Sudarman Rahman; Yahya Febrianto; Shesanthi Citrariana; Mu’afa Purwa Arsana; Thathit Suprayogi; Yehezkiel Steven Kurniawan
Journal of Multidisciplinary Applied Natural Science Vol. 4 No. 2 (2024): Journal of Multidisciplinary Applied Natural Science
Publisher : Pandawa Institute

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.47352/jmans.2774-3047.210

Abstract

Drymoglossum piloselloides is one of the epiphytic plants that is commonly found in Southeast Asia region. In this study, the ethanol extract of D. piloselloides plant has been used in the green synthesis of silver nanoparticles. The synthesized silver nanoparticles were characterized by ultraviolet-visible (UV-Vis) spectrophotometry, X-ray diffraction (XRD),Fourier-transform infrared (FTIR) spectroscopy, and transmission electron microscopy (TEM) measurements. The UV-Vis spectrum of silver nanoparticles showed a maximum wavelength at 453 nm. The XRD measurement showed the silver nanoparticles peaks at 38.38°, 44.60°, 64.76°, and 77.62°. The FTIR spectra provided evidence of the interaction between silver and chemicals in the plant extract as a weak signal at 682 cm-1. Meanwhile, TEM revealed an average size of 12.63nm. The synthesised silver nanoparticles were utilised for the reduction of 4-nitrophenol with a conversion percentage of up to 100% with a reduction reaction rate constant of 7.104 s-1. In addition, methylene blue was also successfully reduced with the synthesised silver nanoparticles as the catalyst with a reduction reaction rate constant (k) of 21.150 s-1. This study highlights the superior advantage of utilizing ethanolic extract of D. piloselloides to prepare silver nanoparticles with promising catalytic reduction purposes.
Evaluation of Xanthone and Cinnamoylbenzene as Anticancer Agents for Breast Cancer Cell Lines through In Vitro and In Silico Assays Yehezkiel Steven Kurniawan; Hanif Amrulloh; Ervan Yudha; Nela Fatmasari; Faris Hermawan; Anggit Fitria; Harno Dwi Pranowo; Eti Nurwening Sholikhah; Jumina Jumina
Journal of Multidisciplinary Applied Natural Science Vol. 5 No. 1 (2025): Journal of Multidisciplinary Applied Natural Science
Publisher : Pandawa Institute

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.47352/jmans.2774-3047.231

Abstract

Breast cancer is a severe global disease for women as the number of deaths increases annually. Therefore, attempts to find new anticancer agents are critical and inevitable. In this work, we report the investigation on the anticancer activity of xanthone and cinnamoylbenzene compounds against two breast cancer cell lines, i.e., T47D and MCF-7, through experimental in vitro and theoretical in silico assays. Xanthone and cinnamoylbenzene exhibit anticancer activity with a half-maximal inhibitory concentration (IC50) of 136.7–194.3 and 235.8–262.4 µg/mL against T47D and MCF-7 cancer cells, respectively. Cinnamoylbenzene generates less cytotoxicity to normal Vero cells with a selectivity index of 1.095–2.102. The molecular docking studies agree with the experimental data in which cinnamoylbenzene is more active against T47D with an IC50 of 136.7 µg/mL due to Topoisomerase II inhibition through π-π stacked interactions with Adenine12 and Guanine13 nitrogen bases. Meanwhile, xanthone is more active against MCF-7 with an IC50 of 235.8 µg/mL due to EGFR inhibition through van der Waals interaction and hydrogen bond with Glutamic acid767 and Methionine769 amino acid residues, respectively. Additionally, the pharmacokinetic parameters of xanthone and cinnamoylbenzene are predicted through absorption, distribution, metabolism, excretion, and toxicity (ADMET) analysis, and they show better suitability than doxorubicin as the commercial anticancer drug.