Drug Target Insights

Colorectal cancer incidences continue to increase annually, worldwide. Herbal plants with antiproliferative properties received research interest as agents that can be adjuvant therapies with chemotherapy drugs to enhance their efficacy and reverse drug resistance.

Thembelihle Nxasana

Innocensia Mangoato

Patriciah Masiu

Abhay Mishra

Motlalepula Matsabisa

Investigating the combinatory effect of Sclerocarya birrea with doxorubicin against selected colorectal cancer cell lines

研究非洲沙棘与多柔比星联合作用对选定结直肠癌细胞系的抑制效果

Objectives: To assess through an indirect treatment comparison (ITC) the potential benefit of faricimab over the anti-vascular endothelial growth factor (VEGF) real-life scenario, hereby defined standard of care (SoC), in Italy, that is, aflibercept, bevacizumab, and ranibizumab, in patients with neovascular age-related macular degeneration (nAMD) naïve to any anti-VEGF treatment. Methods: Individual patient-level data from the phase III clinical trials TENAYA and LUCERNE (faricimab cohort) and the real-world study RADIANCE (RADIANCE cohort) were used. Efficacy was evaluated with changes in best corrected visual acuity (BCVA) and central subfield thickness (CST) from baseline to 1 year (week 52 in the RADIANCE and week 48 in the faricimab cohorts, respectively). Propensity score-based inverse probability of treatment weighting was utilized to balance cohorts and mitigate bias due to potential confounding. Sensitivity analyses were performed to evaluate treatment differences adjusted for the number of injections. Results: The ITC included 513 patients treated with faricimab and 263 patients treated with SoC. At 1 year, faricimab showed a greater mean BCVA gain (treatment difference +5.4 letters, p&lt;0.001) and CST reduction (treatment difference −71.8 μm, p&lt;0.001) compared to SoC. Sensitivity analyses confirmed the robustness of results, showing a BCVA improvement of +4.0 letters and a CST reduction of −71.5 μm in favor of faricimab. Conclusions: Despite the limitations due to the use of ITC and the comparison between clinical trials and real-world cohorts, the present analysis suggests potential benefits in terms of vision gain and CST reduction in naïve nAMD patients treated with faricimab compared with SoC in a real-world setting.

Carlotta Galeone

Federica Turati

Massimo Nicolò

Mariacristina Parravano

Stela Vujosevic

Laura Bianchino

Emilia Sicari

Paolo Lanzetta

Faricimab versus the standard of care for neovascular age-related macular degeneration in Italy: an indirect treatment comparison

意大利新生血管性年龄相关性黄斑变性的Faricimab与标准治疗间接比较

Background: Edible fruits and resins provide various benefits to mankind including potential medicinal applications. This study aimed to determine the cytotoxicity, selectivity, and clonogenicity of fruits and exudates of certain Saudi medicinal plants (Anethum graveolens (BEP-09), Opuntia ficus-indica (L.) Miller (BEP-10), Boswellia serrata Roxb. ex Colebr. (BEP-11), and Commiphora myrrha (BEP-12)) against human liver adenocarcinoma (HepG2). Methods: Initial cytotoxicity and cell line selectivity against different cell lines were screened using MTT assay. The most promising extract was subjected to gas chromatography-mass spectrometry (GC-MS) analysis to determine the main phytoconstituents. Clonogenicity was checked for the most active extract. Results: The selected plants’ fruits and resins possess a significant cytotoxic activity estimated as IC50. The fruit of BEP-10 was found to be the most active extract against liver cancer cells (IC50 = 2.82) comparable to both doxorubicin (IC50 = 1.40) and camptothecin (IC50 = 1.11). It showed a selectivity index of 4.47 compared to the normal human foetal lung fibroblast (MRC5) cells. BEP-10 showed a dose-dependent clonogenic effect against HepG2 cells comparable to the effect of doxorubicin. The GC-MS chromatogram of BEP-10 extract revealed the presence of eight small polar molecules, representing 73% of the total identified compounds and the rest three molecules (27%) were non-polar constituents. The furan derivatives represent the chief components in BEP-10 (16.3%), while the aldehyde 5-(hydroxymethyl)-2-furancarboxaldehyde was found to be the main molecule (13.2%). Conclusion: The fruits of BEP-10 have a potential cytotoxic effect particularly against HepG2. The identified phytoconstituents in the tested plant extract might contribute to the investigated cytotoxic activity.

Ali Hendi Alghamdi

Aimun A E Ahmed

Mahadi Bashir

Haidar Abdalgadir

Asaad Khalid

Mohamed E Abdallah

Riyad Almaimani

Bassem Refaat

Ashraf N Abdalla

Cytotoxic activity, selectivity, and clonogenicity of fruits and resins of Saudi medicinal plants against human liver adenocarcinoma

沙特药用植物果实和树脂对人肝腺癌的细胞毒性活性、选择性和克隆形成能力

Multidrug-resistant (MDR) extended-spectrum beta-lactamase (ESBL)-producing bacterial isolates have emerged as a global threat to human health. Little is known about the overall prevalence of multidrug resistance profile and ESBL-producing gram-negative bacilli (GNB) in Ethiopia. Therefore, this meta-analysis was performed to produce proportional estimates of multidrug resistance and ESBL-producing GNB in Ethiopia.&#x0D; A web-based search was conducted in PubMed, Google Scholar, Research Gate, Scopus and other databases. Articles published till 2019 on the prevalence and antimicrobial resistance profiles of ESBL-producing GNB in Ethiopia were included in the study. Relevant data were extracted and statistical analysis was performed using comprehensive meta-analysis version 3.3.0 software. Publication bias was analyzed and presented with funnel plots.&#x0D; In this meta-analysis, the overall proportional estimate of ESBL-producing GNB was 48.9% (95% confidence interval [CI]: 0.402, 0.577). The pooled proportional estimates of ESBL-producing Klebsiella pneumoniae, Escherichia coli and other GNB were 61.8%, 41.2% and 42.9%, respectively. Regarding antimicrobial resistance profiles against selected drugs, the pooled proportional estimates of resistance against amoxicillin-clavulanic acid, trimethoprim-sulfamethoxazole, cefotaxime, ceftazidime, tetracycline, gentamicin and ciprofloxacin was 79.0%, 78.4%, 78.0%, 72.4%, 72.7%, 58.9% and 43.8%, respectively. The pooled proportional estimates of MDR isolates were found to be 82.7% (95% CI: 0.726, 0.896), which are relatively high as compared to other countries. This highlights a need for active surveillance systems which can help understand the actual epidemiology of ESBL, aid in formulating national guidelines for proper screening of ESBL and support developing standardized approaches for managing patients colonized with ESBL

Mengistu Abayneh

Teshale Worku

Prevalence of multidrug-resistant and extended-spectrum beta-lactamase (ESBL)-producing gram-negative bacilli: A meta-analysis report in Ethiopia

埃塞俄比亚多重耐药和产超广谱β-内酰胺酶（ESBL）革兰氏阴性杆菌的流行情况：一项Meta分析报告

Salbutamol and terbutaline are short-acting β2 adrenergic agonists that produce bronchial smooth muscle relaxation and are widely used in obstructive pulmonary diseases. Nevertheless, their use has been the cause of a paradoxical bronchoconstriction, which is a rare and potentially serious adverse reaction. The aim of this study is to report a case of paradoxical bronchoconstriction caused by β2 adrenergic agonists.This case is about a 50-year-old asthmatic patient who describes a history of repeated acute asthma attacks after salbutamol inhalation or terbutaline nebulization. A double-blind crossover study was performed over 3 days, in order to compare the effects of each bronchodilator. Forced expiratory volume in 1 second (FEV1), forced vital capacity (FVC), and maximal expiratory flow 25-75 (MEF25-75) were measured.On the first day, a bronchoconstriction caused by deep and repeated inhalations was eliminated. On the second day, an airway obstruction was confirmed by a decrease in FEV1 at 40% from baseline values after nebulization of a standard dose of terbutaline. On the third day, a spirometry was performed before and after nebulization of a standard dose of ipratropium bromide, and there were no significant changes in the spirometric parameters. Finally the patient was discharged with a written warning mentioning the danger of salbutamol and terbutaline use.Salbutamol and terbutaline are generally well-tolerated β2 adrenergic agonists. Nevertheless, in rare cases, these substances can cause a paradoxical bronchoconstriction. Doctors must therefore remain vigilant about its side effect and possibly investigate each case.

Khadija Ayed

Islam Latifa Hadi Khalifa

Salma Mokaddem

Saloua Ben Khamsa Jameleddine

Paradoxical bronchoconstriction caused by β2-adrenoceptor agonists

β2-肾上腺素受体激动剂引起的矛盾性支气管收缩

Levofloxacin, a fluoroquinolone, is an extensively used antibiotic effective against both positively and negatively staining bacteria. It works by inhibiting bacterial topoisomerase type II and topoisomerase type IV, resulting in impaired DNA synthesis and bacterial cell death. Eryptosis is another term for apoptotic cell death of erythrocyte marked by cell shrinkage, phosphatidylserine (PS) flipping, and membrane blebbing.

Hafiz Muhammad Aslam

Azka Sohail

Ammara Shahid

Maham Abdul Bari Khan

None Muhammad Umar Sharif

Razia Kausar

Samia Nawab

Waqas Farooq

Dr. Kashif Jilani

Majeeda Rasheed

Levofloxacin induces erythrocyte contraction leading to red cell death

左氧氟沙星诱导红细胞收缩导致红细胞死亡

Objective: Cancer or neoplasm is a cosmopolitan catastrophe that results in more than 20 million new cases and 10 million deaths every year. Some factors lead to carcinogenesis like infectious diseases. Parasites like Toxoplasma gondii, by its components, could modulate the cancer system by inducing apoptosis. The objective of this investigation is to assess the potential of peptides derived from T. gondii in combating cancer by examining their effects on Caco-2, Hep-G2, and HT29 cell lines. Materials and methods: Candidate peptide by its similarity to anticancer compounds was predicted through the computer-based analysis/platform. The impact of the peptide on cell viability, cell proliferation, and gene expression was evaluated through the utilization of MTT assay, flow cytometry, and real-time polymerase chain reaction (PCR) methodologies. Results: The cell viability rate exhibited a significant decrease (p &lt; 0.001) across all cell lines when exposed to a concentration of ≤160 μg. Within the 48-hour timeframe, the half maximal inhibitory concentration (IC50) for HT29 and Hep-G2 cell lines was determined to be 107.2 and 140.6 μg/mL, respectively. Notably, a marked decrease in the expression levels of Bcl2 and APAF1 genes was observed in both the Hep-G2 and HT29 cell lines. Conclusion: These findings indicate that the T. gondii peptide affected cancer cell mortality and led to changes in the expression of genes associated with apoptosis.

Firooz Shahrivar

Javid Sadraei

Majid Pirestani

Ehsan Ahmadpour

Enhancement of apoptosis in Caco-2, Hep-G2, and HT29 cancer cell lines following exposure to Toxoplasma gondii peptides

弓形虫肽暴露后Caco-2、Hep-G2和HT29癌细胞系凋亡增强

Abbreviation	Drug Target Insights
Journal Impact	2.16
Quartiles(Global)	PHARMACOLOGY & PHARMACY(Q3)

ISSN	1177-3928
h-index	16

Publication Information	Publisher: AboutScience Srl，Publishing cycle: ，Journal Type: journal，Open Access Journals: Yes
Basic data	Year of publication: 2011，Proportion of original research papers: 81.82%，Self Citation Rate:5.00%， Gold OA Rate: 93.10%
Journal Fees	$Details
Average review cycle	8 weeks

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Investigating the combinatory effect of Sclerocarya birrea with doxorubicin against selected colorectal cancer cell lines

Faricimab versus the standard of care for neovascular age-related macular degeneration in Italy: an indirect treatment comparison

Cytotoxic activity, selectivity, and clonogenicity of fruits and resins of Saudi medicinal plants against human liver adenocarcinoma

Prevalence of multidrug-resistant and extended-spectrum beta-lactamase (ESBL)-producing gram-negative bacilli: A meta-analysis report in Ethiopia

Paradoxical bronchoconstriction caused by β2-adrenoceptor agonists

Faricimab versus the standard of care for neovascular age-related macular degeneration in Italy: an indirect treatment comparison

Investigating the combinatory effect of Sclerocarya birrea with doxorubicin against selected colorectal cancer cell lines

Cytotoxic activity, selectivity, and clonogenicity of fruits and resins of Saudi medicinal plants against human liver adenocarcinoma

Levofloxacin induces erythrocyte contraction leading to red cell death

Enhancement of apoptosis in Caco-2, Hep-G2, and HT29 cancer cell lines following exposure to Toxoplasma gondii peptides