Article
Chemistry, Physical
Marta Erminia Alberto, Bruna Clara De Simone, Tiziana Marino, Marirosa Toscano, Nino Russo
Summary: Thionation of carbonyl groups in known dyes has proven to enhance singlet oxygen production and shift the absorption band, suggesting a potential strategy for developing heavy-atom-free photosensitizers for photodynamic therapy (PDT). In this study, the effect of sulfur and selenium substitution for oxygen in the oxo-4-dimethylamino-1,8-naphthalimide molecule was investigated. The thio- and seleno-derivatives were found to allow for multiple intersystem crossing pathways, leading to increased singlet oxygen production. Moreover, the transition from a (1)pi pi* to a (1)n pi* state in the selenium derivative was crucial for reaching clinically useful regions of the spectrum. These findings suggest that selenium-for-oxygen substitution could be a promising strategy for developing more suitable PDT agents and advancing heavy-atom-free photosensitizers.
JOURNAL OF PHYSICAL CHEMISTRY A
(2022)
Review
Biochemistry & Molecular Biology
Alessandro Allegra, Alessandro Tonacci, Elvira Ventura Spagnolo, Caterina Musolino, Sebastiano Gangemi
Summary: Hypericum, widely used as a therapeutic cure for depression, skin wounds, and respiratory and inflammatory disorders, also demonstrates various biological actions such as anti-infective, anti-oxidant, and spasmolytic abilities. Recent studies have shown its potential in the treatment of pathological conditions like trigeminal neuralgia and cancer. In hematologic malignancies, Hypericum induces apoptosis in myeloid and lymphoid cells, and targets mediators of cell migration and angiogenesis. Furthermore, it downregulates proteins involved in leukemia cell resistance to chemotherapeutic agents, making it a potential candidate for tumor photodynamic therapy.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Physical
Sennur Ozcelik, Asiye Gok Yurttas, Muhammet U. Kahveci, Altug Mert Sevim, Ahmet Gul
Summary: A novel aza-BODIPY compound with phthalonitrile substituents was synthesized and characterized in this study. Its photophysical and photochemical properties were determined, and its potential for photodynamic therapy was explored through tests on breast cancer cells and normal healthy cells.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Chemistry, Physical
Valeria Butera, Gloria Mazzone, Hermann Detz
Summary: A new family of bis[pyrrolyl Ru(II)] triad scaffolds has been reported as efficient compounds for in vitro photodynamic therapy (PDT), with the complex carrying a pyrenyl group in the organic linker showing exceptional photosensitizing activity. This computational study based on DFT and TDA-TDDFT methods investigated the photochemical properties of this promising complex and compared it with a complex carrying a benzothiadiazole group. The influence of the organic chromophore and the role of the second [Ru(bpy)(2)](2+) moiety were evaluated.
Article
Chemistry, Medicinal
Yasunori Yamashita, Megumi Mae, Masayuki Oohira, Yukio Ozaki, Seigo Ohba, Izumi Asahina, Atsutoshi Yoshimura
Summary: This study evaluated the efficacy and safety of antimicrobial photodynamic therapy (a-PDT) in the maintenance phase. The findings suggest that a-PDT is more effective than scaling root planing (SRP) in improving periodontal status and can be a noninvasive treatment option, especially for patients with deeper periodontal pockets.
Article
Chemistry, Applied
Jae Moon Lee, Seongsoo Kang, Tae Gyu Hwang, Hong Mo Kim, Woo Sung Lee, Dongho Kim, Jae Pil Kim
Summary: This study investigates the photophysical and solvatochromic properties of BODIPY-based D-A complexes, and verifies the hypothesis that decreasing ΔE-ST can increase SOQY. By designing experiments under more controlled conditions, more accurate data was obtained. Materials with CT character exhibited higher SOQY.
Article
Oncology
Fangbiao Zhan, Ye Zhang, Qiang Zuo, Chaozheng Xie, Huanhuan Li, Ling Tian, Chunrong Wu, Zhiyu Chen, Chaohua Yang, Yang Wang, Qiaochu Li, Tao He, Haoyang Yu, Jian Chen, Jiangxia Xiang, Yunsheng Ou
Summary: This study reveals that ferroptosis and YAP knockdown can enhance the sensitivity of osteosarcoma cells to MPPa-PDT therapy.
PHOTODIAGNOSIS AND PHOTODYNAMIC THERAPY
(2022)
Article
Biochemistry & Molecular Biology
Kenta Yokoi, Yoshitaka Yasuda, Azusa Kanbe, Takehiro Imura, Shin Aoki
Summary: Photodynamic therapy (PDT) is a noninvasive cancer treatment method that uses photochemical excitation of photosensitizers (PSs) to generate reactive oxygen species (ROS) and induce cancer cell death. In clinical trials, red-near infrared light is preferred due to its deeper tissue penetration. To overcome this limitation, a PDT system using cyclometalated iridium(III) complexes with blue light excitation in a wireless power transmission (WPT) system was developed. This WPT-based PDT represents a potentially new method for treating tumors that are difficult to treat with previous PDT systems.
Article
Oncology
Wen Sun, Xiaoyu Ma, Yunxia Wang, Guosheng Yang, Jiping Liao, Yuan Cheng, Guangfa Wang
Summary: This study finds that moderate doses of photodynamic therapy (PDT) are more effective than low or high doses in treating non-small cell lung cancer (NSCLC). These experimental data are of great significance for improving lung cancer treatment protocols.
PHOTODIAGNOSIS AND PHOTODYNAMIC THERAPY
(2023)
Article
Pharmacology & Pharmacy
Nadire Oezenver, Thomas Efferth
Summary: Oxidative stress is crucial in carcinogenesis and treatment response, and antioxidant genes play important roles in chemotherapy and radiotherapy resistance. This study investigated the role of 205 antioxidant genes in 21 different tumor types and identified 84 genes whose expression was significantly correlated with overall survival. Renal clear cell carcinoma, renal papillary cell carcinoma, and hepatocellular carcinoma were the tumor types most frequently associated with antioxidant gene expression and worse overall survival. Additionally, 17 genes were found to be overexpressed in tumors and may serve as druggable targets.
Article
Biology
Onat Kadioglu, Faranak Bahramimehr, Mona Dawood, Nuha Mahmoud, Mohamed Elbadawi, Xiaohua Lu, Yagmur Buelbuel, Jana Agnieszka Schulz, Lisa Kraemer, Marie-Kathrin Urschel, Zoe Kuenzli, Leila Abdulrahman, Fadwa Aboumaachar, Lajien Kadalo, Le Van Nguyen, Sara Shaidaei, Nawal Thaher, Kathrin Walter, Karolin Christiane Besler, Andreas Spuller, Markus Munder, Henry Johannes Greten, Thomas Efferth
Summary: RNA-sequencing is utilized to develop individualized therapy concepts for cancer patients based on their tumor-specific mutational profiles. In this study, drugs and inhibitors were identified through virtual drug screening of FDA-approved drugs and mining the Drug Gene Interaction (DGI) database for missense mutated proteins in 35 tumors. The approach offers new treatment options for patients with refractory tumors that do not respond to standard chemotherapy.
COMPUTERS IN BIOLOGY AND MEDICINE
(2023)
Article
Medicine, Research & Experimental
Jasmin Taubenschmid-Stowers, Michael Orthofer, Anna Laemmerer, Christian Krauditsch, Marianna Rozsova, Christian Studer, Daniela Loetsch, Johannes Gojo, Lisa Gabler, Matheus Dyczynski, Thomas Efferth, Astrid Hagelkruys, Georg Widhalm, Andreas Peyrl, Sabine Spiegl-Kreinecker, Dominic Hoepfner, Shan Bian, Walter Berger, Juergen A. Knoblich, Ulrich Elling, Moritz Horn, Josef M. Penninger
Summary: The natural compound Artemisinin is widely used as an antimalarial drug and has potential for anticancer therapy. Through screening with yeast and haploid stem cells, it has been discovered that the porphyrin biosynthesis pathway is crucial for the cytotoxicity of Artemisinin. In various human brain tumor models, a combination treatment of Artemisinin and the porphyrin enhancer 5-aminolevulinic acid sensitizes and kills brain tumor cells.
EMBO MOLECULAR MEDICINE
(2023)
Article
Chemistry, Applied
Inas Y. Younis, Rana M. Ibrahim, Ali. M. El-Halawany, Mohamed-Elamir F. Hegazy, Thomas Efferth, Engy Mohsen
Summary: In this study, LC-QTOF-MS and multivariate statistical tools were used to analyze the composition differences of dragon fruit peel and pulp from Egypt, Germany, Philippines, and China. It was found that dragon fruits from China and Egypt were the most distinct due to their high betalains content. Moreover, different extracts from dragon fruit showed different activities as inhibitors of alpha-glucosidase and AGE formation, as well as antioxidants.
Article
Biochemistry & Molecular Biology
Matteo Rosellini, Petri Turunen, Thomas Efferth
Summary: Plastic in oceans degrades into microplastics and nanoplastics, posing various problems for marine organisms. Recent findings show that microplastics can be found in human blood, breast milk, and placenta, suggesting their ability to enter the human body with unknown effects. Additionally, plastic contains compounds with potential impact on human health, such as plasticizers and antioxidants. This study investigates the interaction between plastic-related compounds and two cellular transporters involved in detoxification of xenobiotics. The results provide evidence that certain plastic compounds can inhibit these transporters and increase their toxic potential.
Article
Biochemistry & Molecular Biology
Luay. J. J. Rashan, Nadire Oezenver, Joelle. C. C. Boulos, Mona Dawood, Wynand. P. P. Roos, Katrin Franke, Ioannis Papasotiriou, Ludger. A. A. Wessjohann, Heinz-Herbert Fiebig, Thomas Efferth
Summary: A study found that a cold-water leaf extract called Breastin from Nerium oleander L. has potential as an anticancer agent, inhibiting the growth of multiple cancer cell lines and bypassing some traditional drug resistance mechanisms. The study also showed that protein expression profiles can be used to predict the sensitivity of tumor cells to Breastin constituents.
Article
Pharmacology & Pharmacy
Mohamed Elbadawi, Joelle C. Boulos, Mona Dawood, Min Zhou, Waseem Gul, Mahmoud A. ElSohly, Sabine M. Klauck, Thomas Efferth
Summary: The proto-oncogenic transcription factor c-MYC is a key player in tumorigenesis, cellular proliferation, and cell death control. This study aimed to investigate the anticancer activity and molecular mechanisms of the artemisinin dimer isoniazide in drug-sensitive and multidrug-resistant leukemia cells. The compound showed potent growth inhibitory activity, good binding with c-MYC, downregulated c-MYC expression, and induced DNA damage, apoptosis, and autophagy.
Editorial Material
Nutrition & Dietetics
Haroon Khan, Thomas Efferth, Silvia Tejada
FRONTIERS IN NUTRITION
(2023)
Article
Integrative & Complementary Medicine
Laetitia M. Youmbi, Yves S. D. Makong, Armelle T. Mbaveng, Simplice B. Tankeo, Ghislain W. Fotso, Bruno L. Ndjakou, Jean D. Wansi, Veronique P. Beng, Norbert Sewald, Bonaventure T. Ngadjui, Thomas Efferth, Victor Kuete
Summary: This study aimed to identify the cytotoxic constituents of Brucea antidysenterica and demonstrate their mode of induction of apoptosis on cancer cell lines. The results showed that Brucea antidysenterica and its constituents have potential antiproliferative effects and can induce apoptosis through caspase activation, alteration of mitochondrial membrane potential, and increased reactive oxygen species levels.
BMC COMPLEMENTARY MEDICINE AND THERAPIES
(2023)
Article
Biochemistry & Molecular Biology
Julia Schaefer, Vincent Julius Kloesgen, Ejlal A. Omer, Onat Kadioglu, Armelle T. Mbaveng, Victor Kuete, Andreas Hildebrandt, Thomas Efferth
Summary: Cancer therapy is often hindered by drug resistance and severe side effects. Phytochemicals are a valuable resource for developing less toxic drugs. Bioinformatics can simplify the drug development process. This study analyzed 375 phytochemicals and identified six compounds with potential anticancer activity and P-gp inhibition.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Plant Sciences
Anand Kar, Durgesh Mahar, Sagarika Biswas, Debolina Chakraborty, Thomas Efferth, Sunanda Panda
Summary: This study aimed to evaluate the effect of Ficus religiosa leaf extract in ameliorating hypothyroidism in rats and identify the major bioactive compounds responsible for this activity. The results showed that FL extract could improve hypothyroidism, and the major compounds betulinic acid, chlorogenic acid, and quinic acid may increase thyroid hormone levels by interacting with thyroid hormone receptor and TSH receptor through molecular docking analysis.
JOURNAL OF ETHNOPHARMACOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Min Zhou, Joelle C. Boulos, Ejlal A. Omer, Sabine M. Klauck, Thomas Efferth
Summary: The aim of this study was to investigate the molecular modes of action of a 1,2,4-oxadiazole derivative (ZINC15675948) as a c-MYC inhibitor. It was found that ZINC15675948 strongly bound to c-MYC and downregulated its expression. In both leukemia and breast cancer cells, ZINC15675948 affected signaling pathways downstream of c-MYC through inducing DNA damage, cell cycle arrest, and apoptosis.
Article
Chemistry, Multidisciplinary
Assia I. Drif, Bharathi Avula, Ikhlas A. Khan, Thomas Efferth
Summary: This study investigated the inhibitory activities of secondary metabolites from chamomile against COX2, an enzyme involved in inflammation and cancer development. It also evaluated the cytotoxicity of these compounds on cancer cell lines. Myricetin, a compound found in chamomile tea, was further studied to determine its effects on tumor cells and its potential as a therapeutic agent. Overall, this study provides insight into the molecular mechanisms of chamomile secondary metabolites and their potential in cancer prevention or treatment.
APPLIED SCIENCES-BASEL
(2023)
Article
Oncology
Joelle C. Boulos, Manik Chatterjee, Letian Shan, Thomas Efferth
Summary: Hematological neoplasms are difficult to cure, and new treatment approaches targeting c-MYC are needed. In this study, adapalene, an FDA-approved drug, was identified as a potential c-MYC inhibitor, providing hope for the development of new anticancer medications. Adapalene showed cytotoxicity against multiple myeloma cells and decreased c-MYC expression and transcriptional activity, resulting in cell cycle arrest, DNA damage, and induction of apoptosis and autophagy.
Article
Integrative & Complementary Medicine
Valaire Y. Matieta, Armelle T. Mbaveng, Guy R. Sado Nouemsi, Simplice B. Tankeo, Gabriel T. Kamsu, Paul Nayim, Alain M. Lannang, Ilhami Celik, Thomas Efferth, Victor Kuete
Summary: This study found that Bauhinia thonningii and its constituents have promising cytotoxic effects on human cancer cell lines, without causing toxicity in rats.
BMC COMPLEMENTARY MEDICINE AND THERAPIES
(2023)