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Astrid Widhowaty Santoso,1,* Eri Amalia,2,* Kartika Indah Sari,3 Veni Takarini,4 Irna Sufiawati5,* 1Oral Medicine Residency Program, Faculty of Dentistry, Universitas Padjadjaran, Bandung, Indonesia; 2Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Universitas Padjadjaran, Bandung, Indonesia; 3Department of Oral Biology, Faculty of Dentistry, Universitas Padjadjaran, Bandung, Indonesia; 4Department of Dental Material Science and Technology, Faculty of Dentistry, Universitas Padjadjaran, Bandung, Indonesia; 5Department of Oral Medicine, Faculty of Dentistry, Universitas Padjadjaran, Bandung, Indonesia*These authors contributed equally to this workCorrespondence: Irna Sufiawati, Department of Oral Medicine, Faculty of Dentistry, Universitas Padjadjaran, Jalan Sekeloa No. 1, Bandung, West Java, 40132, Indonesia, Tel +62-22-2504985, Email irna.sufiawati@unpad.ac.idIntroduction: Oral mucosal wounds present significant clinical challenges due to their susceptibility to infection, inflammation, and delayed healing. The limitation of standard anti-inflammatory drugs (both steroidal and non-steroidal) highlights the urgent need for plant-derived alternative therapies. Granola potato (Solanum tuberosum L.) from Pangalengan, West Java, Indonesia, has shown promise due to its bioactive compounds. However, its potential for wound healing and anti-inflammatory effects, specifically for oral mucosal wounds, remains largely unexplored.Purpose: To evaluate the wound healing and anti-inflammatory activity of Granola potato peel ethanol extract (GPPEE) on the oral mucosa of Wistar rats based on histopathological analysis.Materials and Methods: Forty-eight Wistar rats were wounded on the palatal mucosa using a 4 mm punch biopsy and subsequently divided into four groups: placebo gel, 0.1% triamcinolone acetonide ointment (TCA), 4% GPPEE gel, and 6% GPPEE gel. The rats were euthanized on days 0, 1, 3, 7, and 14. Histopatholo

Faradila Tiarasanti,1,&ast; Irna Sufiawati,1,&ast; Eri Amalia,2 Kartika Indah Sari,3 Cucu Zubaedah,4 Veni Takarini5 1Department of Oral Medicine, Faculty of Dentistry, Padjadjaran University, Bandung, Indonesia; 2Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Padjadjaran University, Bandung, Indonesia; 3Department of Oral Biology, Faculty of Dentistry, Padjadjaran University, Bandung, Indonesia; 4Department of Dental Public Health, Faculty of Dentistry, Padjadjaran University, Bandung, Indonesia; 5Department of Dental Material Science and Technology, Faculty of Dentistry, Padjadjaran University, Bandung, Indonesia&ast;These authors contributed equally to this workCorrespondence: Irna Sufiawati, Department of Oral Medicine, Faculty of Dentistry, Padjadjaran University, Jalan Sekeloa No. 1, Bandung, West Java, 40132, Indonesia, Tel +62-22-2504985, Email irna.sufiawati@fkg.unpad.ac.idPurpose: Phenolic compounds with antioxidant, antimicrobial, and anti-inflammatory properties have been identified in potatoes (Solanum tuberosum L.; Solanaceae), which may potentially contribute to wound healing. The study aimed to evaluate the effect of potato peel extract gel Granola variety on oral gingival wound healing in Wistar Rats.Methods: This research was a true experimental in vivo study, involving 30 male Wistar rats, aged 12– 14 weeks and weighing approximately 150 to 200 grams. Surgical vertical incisions, each 3 mm in length, were made on the mandibular gingiva. The test group consisted of six subgroups, each comprising 5 rats. The negative control group received a base gel, while treatment groups were given 1% povidone-iodine solution, 0.1% triamcinolone acetonide oral paste, and 2%, 4%, and 6% potato peel extract gel. Wound lengths were measured on days 3, 7, and 14 to evaluate the healing process. Statistical analysis used the ANOVA test, a p-value of < 0.05 was considered statistically significant.Results: All experiment

Eri Amalia,1– 3 Ajeng Diantini,1 Erwahyuni Endang Prabandari,4 Danang Waluyo,4 Anas Subarnas1 1Department of Pharmacology and Clinical Pharmacy, Faculty of Pharmacy, Universitas Padjadjaran, Jatinangor, Indonesia; 2Department of Pharmacology, Faculty of Science and Technology, Department of Pharmacy, Muhammadiyah University, Bandung, Indonesia; 3Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Universitas Padjadjaran, Jatinangor, Indonesia; 4Research Center for Vaccine and Drug, National Research and Innovation Agency, Bogor, IndonesiaCorrespondence: Eri Amalia, Department of Pharmaceutics and Pharmaceutical Technology, Laboratory Building 1, Faculty of Pharmacy, Universitas Padjadjaran. Jl. Raya Bandung-Sumedang km.21. Jatinangor, West Java, 45363, Indonesia, Email amalia_eri@yahoo.co.id; amalia@unpad.ac.idIntroduction: A combination of chemotherapy agents is the best choice in breast cancer treatment to increase the patient survival rate. 5-fluorouracil (5-FU) is one of the drugs applied in combination with other drugs to control and delay development of cancer cells. Nevertheless, the occurrence of multidrug resistance and dose-limiting cytotoxicity have limited the efficacy of 5-FU treatment. Therefore, the discovery of new anti-breast cancer drugs should be pursued.Objective: To study potency of a promising naturally derived compound, caffeic acid phenethyl ester (CAPE), for breast cancer treatment in single and combination with 5-FU.Methods: Cytotoxicity of CAPE, 5-FU, and 5-FU+CAPE was studied by in vitro MTT experiment in MCF-7 cell line, and RT-PCR analysis was used to evaluate the change in gene expression due to the treatment. Moreover, an enzymatic assay and molecular docking analysis were applied to evaluate the possible mechanism of substance-induced apoptosis.Results: The study revealed that a single treatment of CAPE showed cytotoxicity with IC50 6.6 ± 1.0 μM and 6.5 ± 2.9 μM at 24 h and 48 h, respectively. Meanwh

Dihydroorotate dehydrogenase (DHODH) is a mitochondrial monotopic membrane protein that plays an essential role in the pyrimidine de novo biosynthesis and electron transport chain pathways. In Eimeria tenella, an intracellular apicomplexan parasite that causes the most severe form of chicken coccidiosis, the activity of pyrimidine salvage pathway at the intracellular stage is negligible and it relies on the pyrimidine de novo biosynthesis pathway. Therefore, the enzymes of the de novo pathway are considered potential drug target candidates for the design of compounds with activity against this parasite. Although, DHODHs from E. tenella (EtDHODH), Plasmodium falciparum (PfDHODH), and human (HsDHODH) show distinct sensitivities to classical DHODH inhibitors, in this paper,we identify ferulenol as a potent inhibitor of both EtDHODH and HsDHODH. Additionally, we report the crystal structures of EtDHODH and HsDHODH in the absence and presence of ferulenol. Comparison of these enzymes showed that despite similar overall structures, the EtDHODH has a long insertion in the N-terminal helix region that assumes a disordered configuration. In addition, the crystal structures revealed that the ferulenol binding pocket of EtDHODH is larger than that of HsDHODH. These differences can be explored to accelerate structure-based design of inhibitors specifically targeting EtDHODH., Genes, 11(12), art.no.1468; 2020

Human dihydroorotate dehydrogenase (HsDHODH) is a key enzyme of pyrimidine de novo biosynthesis pathway. It is located on the mitochondrial inner membrane and contributes to the respiratory chain by shuttling electrons to the ubiquinone pool. We have discovered ascofuranone (1), a natural compound produced by Acremonium sclerotigenum, and its derivatives are a potent class of HsDHODH inhibitors. We conducted a structure-activity relationship study and have identified functional groups of 1 that are essential for the inhibition of HsDHODH enzymatic activity. Furthermore, the binding mode of 1 and its derivatives to HsDHODH was demonstrated by co-crystallographic analysis and we show that these inhibitors bind at the ubiquinone binding site. In addition, the cytotoxicities of 1 and its potent derivatives 7, 8, and 9 were studied using human cultured cancer cells. Interestingly, they showed selective and strong cytotoxicity to cancer cells cultured under microenvironment (hypoxia and nutrient-deprived) conditions. The selectivity ratio of 8 under this microenvironment show the most potent inhibition which was over 1000-fold higher compared to that under normal culture condition. Our studies suggest that under microenvironment conditions, cancer cells heavily depend on the pyrimidine de novo biosynthesis pathway. We also provide the first evidence that 1 and its derivatives are potential lead candidates for drug development which target the HsDHODH of cancer cells living under a tumor microenvironment., Frontiers in Pharmacology, 9, art.no.997; 2018