PharmaciaPub Date : 2024-06-14DOI: 10.3897/pharmacia.71.e123848
Arkady Valentinovych Khromov, M. Zubairi, Hasan Mohammad Hasan Alhejoj, Z. Alshareeda, Omar Saleh Abdulkader
{"title":"Nanosense: Nonsurgical treatment of superficial cancer by (PLAN)","authors":"Arkady Valentinovych Khromov, M. Zubairi, Hasan Mohammad Hasan Alhejoj, Z. Alshareeda, Omar Saleh Abdulkader","doi":"10.3897/pharmacia.71.e123848","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e123848","url":null,"abstract":"Under current development is Nanosense, a medication designed for the nonsurgical treatment of superficial cancer via pulsed laser ablation of nanoparticles (PLAN). Nanosens is a stable dispersion of phthalocyanine zinc nanoparticles in a physiological solution. The technology for obtaining stable dispersions of zinc phthalocyanine ensures a shelf life of over two years. This article presents preliminary data from preclinical studies of the Nanosens formulation. Results were obtained on the effectiveness, pharmacokinetics, and biodistribution of the Nanosens drug in mice, as well as toxicity and allergy studies. When tested at therapeutic doses (1 TD = 7 mg/kg) ranging from 1 to 10 TD for acute toxicity and from 1 to 30 TD for chronic toxicity, no signs of intoxication leading to death were observed in animals. However, at the maximum dose, individual organs and tissues exhibited a blue coloration.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":1.1,"publicationDate":"2024-06-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141341626","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
PharmaciaPub Date : 2024-06-14DOI: 10.3897/pharmacia.71.e123794
Huda Ghassan Hameed, H. Sahib, Zahraa Sabbar Omran
{"title":"Investigating the anti-carcinogenic potential action of 1,2,3 triazole core compounds: impact of introducing an aldehyde or Nitro group, integrating cell line studies, and in silico ADME and protein target prediction","authors":"Huda Ghassan Hameed, H. Sahib, Zahraa Sabbar Omran","doi":"10.3897/pharmacia.71.e123794","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e123794","url":null,"abstract":"The development of novel chemotherapeutic drugs begins with the suppression of cancer and angiogenesis. Ringed compounds with one or more heteroatoms are known as heterocyclic compounds. In organic chemistry and the pharmaceutical sector, heterocyclic compounds containing nitrogen atoms are valuable. In pharmaceutical chemistry, molecules containing a 1,2,3-triazole skeleton are particularly favored. They have great stability, making it simple to bind them to biomolecular targets. In this work, two 1,2,3-triazole scaffolds containing new chemical entities were assessed using the MTT assay against two malignant (MCF-7 and HCT116) and one normal (HUVECs) cell lines with the goal of creating a new leading prodrug for cancer treatment. The ligands were well characterized by FTIR and 1HNMR. In silico ADMET studies show acceptable pharmacokinetic properties. With the aid of the ligands’ SWISS target protein prediction, the in silico binding to target proteins was examined. The two compounds exhibited a dose-dependent cytotoxic effect, with the H4 compound demonstrating a favorable selectivity index against MCF-7 breast cancer, indicating its potential as a leading compound for anticancer prodrugs.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":1.1,"publicationDate":"2024-06-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141345355","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
PharmaciaPub Date : 2024-06-13DOI: 10.3897/pharmacia.71.e127441
Hiba R. Kamal, T. A. Allwsh
{"title":"Evaluating the effect of vitamin D3 supplementation on DKK-3 serum for third-stage chronic kidney patients","authors":"Hiba R. Kamal, T. A. Allwsh","doi":"10.3897/pharmacia.71.e127441","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e127441","url":null,"abstract":"Vitamin D3 helps to reduce oxidative stress levels, as does Dickkopf-3 (DKK-3) glycoprotein, which is released in the kidney’s tubular membrane during stress and helps promote tubulointerstitial fibrosis. The aim is to investigate how vitamin D supplementation affects serum DKK-3 levels and biochemical indicators of renal function in CKD patients in stage III. The study had inclusion criteria for 180 participants of both sexes, aged between 20 and 35 years. They were divided into 3 groups: 60 healthy participants as control, 60 CKD patients in stage III (without vitamin D3 supplements), and 60 others (with three months of 5,000 IU of weekly vitamin D3 supplements). DKK-3 levels in serum, vitamin D3, and parathyroid hormone were examined, and kidney function was tested. Findings indicated a significant increase in levels of DKK-3 serum for patients in the 2 and 3 groups with CKD compared with control. Additionally, outcomes revealed significantly lower DKK-3 (41%) in the third group of patients who took vitamin D compared to the second group (120%) without vitamin D supplements. There was also an improvement in several kidney functions for the third group, and the relationships revealed a significant inverse association between the levels of vitamin D3 and serum DKK3. Also, there is a significant inverse association with urea and creatinine levels; additionally, there is a significant positive association with glomerular filtration rate and calcium. In conclusion, DKK-3 may be a potential biomarker for the development of CKD. Furthermore, vitamin D administration improved kidney function and DKK-3 levels in individuals with stage III CKD. As a result, vitamin D can assist in reducing the development of chronic kidney disease.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":1.1,"publicationDate":"2024-06-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141346169","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
PharmaciaPub Date : 2024-06-13DOI: 10.3897/pharmacia.71.e126316
Suryanto Suryanto, L. Tumewu, Hilkatul Ilmi, A. Hafid, Suciati Suciati, A. Widyawaruyanti
{"title":"Antimalarial activity of Cratoxyarborenone E, a prenylated xanthone, isolated from the leaves of Cratoxylum glaucum Korth","authors":"Suryanto Suryanto, L. Tumewu, Hilkatul Ilmi, A. Hafid, Suciati Suciati, A. Widyawaruyanti","doi":"10.3897/pharmacia.71.e126316","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e126316","url":null,"abstract":"This research aims to discover active compounds from the leaf extract from Cratoxylum glaucum using the bioassay-guided isolation method. The multistage extraction of C. glaucum leaves was conducted using n-hexane, dichloromethane, and methanol. The LDH assay was employed to analyze antimalarial activity, and the Resazurin assay was used to measure cytotoxicity values. The structure of the active isolates was determined using spectroscopic techniques. The compound 1 was successfully isolated from the dichloromethane extract of C. glaucum leaves (Cg.FD) and confirmed as a prenylated xanthone namely cratoxyarborenone E. The in vitro antimalarial activity showed an IC50 value of 5.82 ± 0.04 μM, the cytotoxicity assay exhibited a CC50 value of 20.74 ± 0.04 µM, and the SI value was determined to be 3.56. Our research demonstrates that cratoxyarborenone E was first reported from Cg.FD and shows promise as a prospective candidate for new antimalarial drugs.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":1.1,"publicationDate":"2024-06-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141345462","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
PharmaciaPub Date : 2024-06-10DOI: 10.3897/pharmacia.71.e122169
Imen Ben Haj Yahia, Olfa Baccouri, Maroua Jalouli, Nadia Boujelbene, Md Ataur Rahman, A. Harrath, Ines Zidi
{"title":"The small phytomolecule resveratrol: A promising role in boosting tumor cell chemosensitivity","authors":"Imen Ben Haj Yahia, Olfa Baccouri, Maroua Jalouli, Nadia Boujelbene, Md Ataur Rahman, A. Harrath, Ines Zidi","doi":"10.3897/pharmacia.71.e122169","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e122169","url":null,"abstract":"Resveratrol (RES), chemically known as trans-3,5,4′-trihydroxystilbene, is a polyphenolic molecule that occurs naturally and is produced by a variety of plants in response to being stimulated by diverse stimuli. It possesses a wide range of biological activities and provides a multitude of health benefits, including anti-tumor, cardioprotective, anti-inflammatory, and antioxidant characteristics. According to the findings of research on the bioavailability of RES, oral administration results in a high level of absorption. However, research has demonstrated that the administration of RES through gavage or intravenous administration produces more favorable results than the administration of RES through oral administration. As a result, more research has been carried out to address the rapid metabolism of RES. This has been accomplished through the utilization of novel formulation methodologies, metabolic regulation, and the analysis of potential interactions with other dietary variables. Through the process of triggering apoptosis, RES has been proposed as a possible agent for reversing drug resistance and improving the therapeutic potential of chemotherapy. Additionally, RES exhibits promising antiproliferative properties when paired with chemotherapeutic medicines, which enhances the overall function of these treatments. It is vital to do additional research to shed light on the beneficial role that RES plays in the context of cancer therapy, even though there have been few clinical trials that combine RES with anticancer medications.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":1.1,"publicationDate":"2024-06-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141363365","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
PharmaciaPub Date : 2024-06-07DOI: 10.3897/pharmacia.71.e122666
Violeta Getova-Kolarova, A. Zlatareva, Ivo Kumanov
{"title":"Exploring the nexus of trust, information sources, and vaccination intent: a study of HPV awareness and general practitioner influence","authors":"Violeta Getova-Kolarova, A. Zlatareva, Ivo Kumanov","doi":"10.3897/pharmacia.71.e122666","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e122666","url":null,"abstract":"This study delves into the intricate interplay between trust in personal doctors (GPs), sources of information about recommended vaccines, and the willingness to vaccinate against human papillomavirus (HPV) and other recommended vaccines. The analysis revealed a positive and statistically significant correlation between HPV awareness and the willingness to vaccinate. Notably, awareness concerning HPV is high, with 35.6% of all respondents expressing readiness to receive the HPV vaccine. The study identified the personal doctor as the predominant source of vaccine-related information. The identified correlations underscore the influence of medical professionals in guiding vaccine uptake choices and the necessity for targeted communication strategies aimed at enhancing vaccine acceptance.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":1.1,"publicationDate":"2024-06-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141372432","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
PharmaciaPub Date : 2024-06-07DOI: 10.3897/pharmacia.71.e126100
Mariana Bacelova, T. Stankova, A. Alakidi, A. Bivolarska, V. Petkova
{"title":"A retrospective look at the impact of smoking on glycemic control and thyroid status in patients with type 1 diabetes (T1DM)","authors":"Mariana Bacelova, T. Stankova, A. Alakidi, A. Bivolarska, V. Petkova","doi":"10.3897/pharmacia.71.e126100","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e126100","url":null,"abstract":"Smoking is one of the factors that can affect serum glucose in patients with type 1 diabetes (T1DM). Control of T1DM is associated with achieving glycated hemoglobin [HbA1c] levels of approximately 7%, which leads to reduced long-term cardiovascular risk. Thyroid hormones can also affect blood sugar levels. Therefore, appropriate control of diabetes can reduce the risk of developing thyroid disorders and vice versa. The aim of the study is to determine whether smoking affects glycemic control and thyroid function in established type 1 diabetes mellitus (T1DM). Materials and methods: A heterogeneous group of 73 patients aged 39±13 years were examined: men 49 (65.3%), women 24 (32%) with T1DM upon admission to the endocrinology department “St. Georgi” (Plovdiv); smokers 25; non-smokers 48. The following were investigated: blood glucose profile (BGP): serum glucose (mmol/L) at 6, 12, 17, 21, 24 hours; HBA1c (%); FT4 pmol/L; TSH mIU/L; TC: total cholesterol mmol/L; HDL-C mmol/L; LDL-C mmol/L; TAG mmol/L; BMI kg/m2 on admission to the ward. Results: In smokers compared to non-smokers, we found statistically significant, p<0.05: increased fasting serum glucose at 6 hours (15.59±6 mmol/L vs 9.67±3.3 mmol/L); decreased BMI (23.21±4.62 kg/m2 vs 26.16±4.79 kg/m2); HDL-C (1.05±0.35 mmol/L vs 1.57±0.43 mmol/L); as well as increased TSH (1.84±0.99 mIU/L vs 0.85±0.94 mIU/L). HBA1c at admission to the clinic showed no significant difference in smokers compared to non-smokers (9.15±1.66% vs. 10.07±1.98%, p=0.574). Conclusion: Smoking worsens glycemic control and thyroid function in patients with T1DM.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":1.1,"publicationDate":"2024-06-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141373967","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
PharmaciaPub Date : 2024-06-07DOI: 10.3897/pharmacia.71.e121674
Ni Made Rika Trismayanti, K. Handono, Dian Handayani, U. Kalsum, Ettie Rukmigarsari
{"title":"Pathway analysis of the effect of virgin coconut oil on suppressing colonic mucosal inflammation and clinical symptoms in ulcerative colitis","authors":"Ni Made Rika Trismayanti, K. Handono, Dian Handayani, U. Kalsum, Ettie Rukmigarsari","doi":"10.3897/pharmacia.71.e121674","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e121674","url":null,"abstract":"Ulcerative colitis (UC) is an inflammatory disease of the large intestine characterized by ulceration and diffuse mucosal damage. Virgin coconut oil (VCO), with its anti-inflammatory properties, emerges as a potential preventive solution for UC. VCO can be an alternative because it has relatively few side effects compared to chemical drugs. This study aims to determine the effect of VCO on suppressing colonic mucosal inflammation and clinical symptoms of UC through pathway analysis. A model grounded in equations within path analysis emerges as a superior framework compared to regression for elucidating the collective impact of PPAR-γ expression, NF-κB p65 expression, the quantity of M1 and M2 macrophages, the M1/M2 macrophage ratio, as well as TNF-α, IL-6, and IL-10 levels, and the MCHI score on DAI in UC model mice. Achieving an R2y9 value of 0.998 vastly surpasses the R2 value of 0.252 attained through regression analysis. This R2y9 value denotes that the cumulative influence of the mentioned variables on DAI stands at an impressive 99.8%. Drawing from the outcomes of pathway analysis, it is evident that VCO exhibits anti-inflammatory properties in UC model mice. To advance this understanding, future investigations could focus on refining VCO into a medicinal formulation suitable for commercial consumption.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":1.1,"publicationDate":"2024-06-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141372825","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
PharmaciaPub Date : 2024-06-06DOI: 10.3897/pharmacia.71.e123549
Phuvamin Suriyaamporn, Boonnada Pamornpathomkul, Pawaris Wongprayoon, T. Rojanarata, T. Ngawhirunpat, P. Opanasopit
{"title":"The artificial intelligence and design of experiment assisted in the development of progesterone-loaded solid-lipid nanoparticles for transdermal drug delivery","authors":"Phuvamin Suriyaamporn, Boonnada Pamornpathomkul, Pawaris Wongprayoon, T. Rojanarata, T. Ngawhirunpat, P. Opanasopit","doi":"10.3897/pharmacia.71.e123549","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e123549","url":null,"abstract":"The application of Artificial Intelligence (AI) has the potential to revolutionize the formulation development of nanomedicine. This study investigated the physicochemical characteristics of progesterone-loaded solid-lipid nanoparticles (PG-SLNs) produced through an emulsification–ultrasonication process, with a focus on demonstrating the efficacy of this controlled preparation method via the Design of Experiments (DoE) and Artificial Neural Networks (ANN). Critical quality factors, including stearic acid, medium chain triglycerides (MCT), Pluronic F-127, and the amount of propylene glycol (PG), were explored using DoE to streamline experimental setups. The concentration of stearic acid was identified as a crucial factor influencing PG-SLN physicochemical properties, impacting particle size (PS), polydispersity index (PDI), zeta potential (ZP), and %drug loading (%DL). Optimal conditions for PS, PDI, ZP, and %DL were identified. DoE revealed acceptable values across multiple runs, and the ANN model demonstrates high prediction accuracy, surpassing Response Surface Methodology (RSM). The selected PG-SLN formulation was tested for transdermal drug delivery, showing improved permeation compared to PG suspension. Loading with limonene further enhances transdermal drug delivery, attributed to limonene’s role as a penetration enhancer. Moreover, the selected PG-SLN formulation was found to be safe and non-toxic to neuronal cells. The combination of DoE and ANN was proposed to enhance predictive ability. This research highlights the potential of PG-SLNs in transdermal drug delivery, emphasizing the role of limonene as a safe and effective enhancer. The study contributes to the growing interest in applying AI tools in pharmaceutical and biomedical fields for improved predictive modeling.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":1.1,"publicationDate":"2024-06-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141378356","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
PharmaciaPub Date : 2024-06-06DOI: 10.3897/pharmacia.71.e121943
Hristina Zlatanova-Tenisheva, S. Vladimirova
{"title":"Experimental screening for analgesic and anti-inflammatory effect of novel compounds with a pyrrole heterocycle","authors":"Hristina Zlatanova-Tenisheva, S. Vladimirova","doi":"10.3897/pharmacia.71.e121943","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e121943","url":null,"abstract":"The pyrrole heterocycle is found in the chemical structure of numerous drugs with various effects, and it has a reasonably high tolerance and safety profile. The objectives of our study were to assess the analgesic and anti-inflammatory efficacy of six novel compounds with pyrrolic structures. Methods: All trials were carried out on 6-week-old male Wistar rats. Animal pain models using thermal (paw withdrawal, tail-flick) and chemical stimuli (formalin test) were used to examine antinociception. A carrageenan-induced paw edema model was used to assess anti-inflammatory activity. Results: Significant differences between the experimental groups were observed in both early and late phase of the formalin test. Conclusions: The six novel pyrrolic compounds have analgesic action against chemical stimuli in experimental conditions. They do not possess anti-inflammatory activity, or antinociceptive properties against thermal stimuli.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":1.1,"publicationDate":"2024-06-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141380401","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}