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Bioactive Compounds in Cancer, Inflammation and Related Diseases
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Bioactive Compounds in Cancer, Inflammation and Related Diseases

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Bioactives and Nutraceuticals".

Deadline for manuscript submissions: closed (15 October 2023) | Viewed by 11764

Special Issue Editor

Prof. Dr. Guan-Jhong Huang

E-Mail Website
Guest Editor
Department of Chinese Pharmaceutical Sciences and Chinese Medicine Resources, College of Chinese Medicine, China Medical University, No.91, Hsueh-Shih Road, Taichung 40402, Taiwan
Interests: metabolic disorders; cancer; inflammation; oxidative stress; natural compounds; molecular signaling
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Inflammation is critically involved in host defenses against infectious agents and injury, but it also helps reduce damage to the body in many diseases, from viral infections and cancer to acute and chronic injury. Therefore, the discovery of inflammation-related biomarkers is the goal of many studies that focus on the pathogenesis, diagnosis, prognosis, and treatment of inflammation-related comorbidities. The purpose of this Special Issue is to publish research papers and reviews concerning biomarkers of inflammation-related diseases, with focus on the occurrence and progress of Chinese herbal medicines, foods or active ingredients in pathological conditions such as cancer, immune diseases, viral infections, cardiovascular-related diseases, etc. Molecular mechanisms in metabolic diseases and all other pathological states associated with inflammation are also of interest. In addition, an association with inflammation has also been found in infectious diseases such as COVID-19. Therefore, this knowledge should facilitate developing strategies to predict disease susceptibility, target and monitor treatments, and ultimately develop new approaches to prevent and treat diseases associated with inflammatory states.

Prof. Dr. Guan-Jhong Huang
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. There is an Article Processing Charge (APC) for publication in this open access journal. For details about the APC please see here. Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • oxidative disorders
  • inflammatory disorders
  • molecular signaling
  • bioactive compounds
  • cytokine

Related Special Issue

Published Papers (7 papers)

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Research

Jump to: Review

16 pages, 3270 KiB  
Article
Radiosensitizing Effect of Dextran-Coated Iron Oxide Nanoparticles on Malignant Glioma Cells
by Nhan Hau Tran, Vyacheslav Ryzhov, Andrey Volnitskiy, Dmitry Amerkanov, Fedor Pack, Aleksander M. Golubev, Alexandr Arutyunyan, Anastasiia Spitsyna, Vladimir Burdakov, Dmitry Lebedev, Andrey L. Konevega, Tatiana Shtam and Yaroslav Marchenko
Int. J. Mol. Sci. 2023, 24(20), 15150; https://doi.org/10.3390/ijms242015150 - 13 Oct 2023
Viewed by 848
Abstract
The potential of standard methods of radiation therapy is limited by the dose that can be safely delivered to the tumor, which could be too low for radical treatment. The dose efficiency can be increased by using radiosensitizers. In this study, we evaluated [...] Read more.
The potential of standard methods of radiation therapy is limited by the dose that can be safely delivered to the tumor, which could be too low for radical treatment. The dose efficiency can be increased by using radiosensitizers. In this study, we evaluated the sensitizing potential of biocompatible iron oxide nanoparticles coated with a dextran shell in A172 and Gl-Tr glioblastoma cells in vitro. The cells preincubated with nanoparticles for 24 h were exposed to ionizing radiation (X-ray, gamma, or proton) at doses of 0.5–6 Gy, and their viability was assessed by the Resazurin assay and by staining of the surviving cells with crystal violet. A statistically significant effect of radiosensitization by nanoparticles was observed in both cell lines when cells were exposed to 35 keV X-rays. A weak radiosensitizing effect was found only in the Gl-Tr line for the 1.2 MeV gamma irradiation and there was no radiosensitizing effect in both lines for the 200 MeV proton irradiation at the Bragg peak. A slight (ca. 10%) increase in the formation of additional reactive oxygen species after X-ray irradiation was found when nanoparticles were present. These results suggest that the nanoparticles absorbed by glioma cells can produce a significant radiosensitizing effect, probably due to the action of secondary electrons generated by the magnetite core, whereas the dextran shell of the nanoparticles used in these experiments appears to be rather stable under radiation exposure. Full article
(This article belongs to the Special Issue Bioactive Compounds in Cancer, Inflammation and Related Diseases)
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15 pages, 3388 KiB  
Article
Anisomeles indica Extracts and Their Constituents Suppress the Protein Expression of ACE2 and TMPRSS2 In Vivo and In Vitro
by Yu-Ru Chen, Wen-Ping Jiang, Jeng-Shyan Deng, Ya-Ni Chou, Yeh-Bin Wu, Hui-Ju Liang, Jaung-Geng Lin and Guan-Jhong Huang
Int. J. Mol. Sci. 2023, 24(20), 15062; https://doi.org/10.3390/ijms242015062 - 11 Oct 2023
Viewed by 1303
Abstract
Coronavirus disease 2019 (COVID-19), stemming from severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has had a profound global impact. This highly contagious pneumonia remains a significant ongoing threat. Uncertainties persist about the virus’s effects on human health, underscoring the need for treatments and [...] Read more.
Coronavirus disease 2019 (COVID-19), stemming from severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has had a profound global impact. This highly contagious pneumonia remains a significant ongoing threat. Uncertainties persist about the virus’s effects on human health, underscoring the need for treatments and prevention. Current research highlights angiotensin-converting enzyme 2 (ACE2) and transmembrane protease serine 2 (TMPRSS2) as key targets against SARS-CoV-2. The virus relies on ACE2 to enter cells and TMPRSS2 to activate its spike protein. Inhibiting ACE2 and TMPRSS2 expression can help prevent and treat SARS-CoV-2 infections. Anisomeles indica (L.) Kuntze, a medicinal plant in traditional Chinese medicine, shows various promising pharmacological properties. In this study, ethanolic extracts of A. indica were examined both in vivo (250 and 500 μM) and in vitro (500 μM). Through Western blotting analysis, a significant reduction in the expression levels of ACE2 and TMPRSS2 proteins was observed in HepG2 (human hepatocellular carcinoma) cells and HEK 293T (human embryonic kidney) cell lines without inducing cellular damage. The principal constituents of A. indica, namely, ovatodiolide (5 and 10 μM), anisomlic acid (5 and 10 μM), and apigenin (12.5 and 25 μM), were also found to produce the same effect. Furthermore, immunohistochemical analysis of mouse liver, kidney, and lung tissues demonstrated a decrease in ACE2 and TMPRSS2 protein expression levels. Consequently, this article suggests that A. indica and its constituents have the potential to reduce ACE2 and TMPRSS2 protein expression levels, thus aiding in the prevention of SARS-CoV-2 infections. Full article
(This article belongs to the Special Issue Bioactive Compounds in Cancer, Inflammation and Related Diseases)
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20 pages, 6447 KiB  
Article
Water Extract from Brown Strain of Flammulina velutipes Alleviates Cisplatin-Induced Acute Kidney Injury by Attenuating Oxidative Stress, Inflammation, and Autophagy via PI3K/AKT Pathway Regulation
by Ya-Ni Chou, Min-Min Lee, Jeng-Shyan Deng, Wen-Ping Jiang, Jaung-Geng Lin and Guan-Jhong Huang
Int. J. Mol. Sci. 2023, 24(11), 9448; https://doi.org/10.3390/ijms24119448 - 29 May 2023
Cited by 1 | Viewed by 1345
Abstract
One of the most popular edible mushrooms in the world, Flammulina velutipes, has been shown to possess pharmacological properties such as anti-inflammatory and antioxidant properties. However, the potential activity of the brown strain of F. velutipes, a hybrid between the white [...] Read more.
One of the most popular edible mushrooms in the world, Flammulina velutipes, has been shown to possess pharmacological properties such as anti-inflammatory and antioxidant properties. However, the potential activity of the brown strain of F. velutipes, a hybrid between the white and yellow strains, has not been thoroughly investigated. Numerous studies have been conducted in recent years to determine whether natural products can aid in improving or treating kidney diseases. In this study, we focused on the renoprotective effects of the brown strain of F. velutipes on cisplatin-induced acute kidney injury (AKI) in mice. Mice were pretreated with water extract from the brown strain of F. velutipes (WFV) from day 1 to day 10, with a single-dose intraperitoneal injection of cisplatin on day 7 to induce AKI. Our results demonstrated that WFV administration resulted in a reduction in weight loss and the amelioration of renal function and renal histological changes in mice with cisplatin-induced AKI. WFV improved antioxidative stress and anti-inflammatory capacity by increasing antioxidant enzymes and decreasing inflammatory factors. The expression of related proteins was determined via Western blot analysis, which showed that WFV could improve the expression of apoptosis and autophagy. We used the PI3K inhibitor Wortmannin and found that WFV achieved a protective effect by modulating the PI3K/AKT pathway and the expression of autophagy. Overall, WFV as a natural substance could be used as a new therapeutic agent for AKI. Full article
(This article belongs to the Special Issue Bioactive Compounds in Cancer, Inflammation and Related Diseases)
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14 pages, 1938 KiB  
Article
Synthesis and Anticancer Evaluation of 4-Anilinoquinolinylchalcone Derivatives
by Cheng-Yao Yang, Min-Yu Lee, Yeh-Long Chen, Jun-Ping Shiau, Yung-Hsiang Tsai, Chia-Ning Yang, Hsueh-Wei Chang and Chih-Hua Tseng
Int. J. Mol. Sci. 2023, 24(7), 6034; https://doi.org/10.3390/ijms24076034 - 23 Mar 2023
Cited by 2 | Viewed by 1334
Abstract
A series of 4-anilinoquinolinylchalcone derivatives were synthesized and evaluated for antiproliferative activities against the growth of human cancer cell lines (Huh-7 and MDA-MB-231) and normal lung cells (MRC-5). The results exhibited low cytotoxicity against human lung cells (MRC-5). Among them, (E)-3-{4-{[4-(benzyloxy)phenyl]amino}quinolin-2-yl}-1-(4-methoxyphenyl) [...] Read more.
A series of 4-anilinoquinolinylchalcone derivatives were synthesized and evaluated for antiproliferative activities against the growth of human cancer cell lines (Huh-7 and MDA-MB-231) and normal lung cells (MRC-5). The results exhibited low cytotoxicity against human lung cells (MRC-5). Among them, (E)-3-{4-{[4-(benzyloxy)phenyl]amino}quinolin-2-yl}-1-(4-methoxyphenyl) prop-2-en-1-one (4a) was found to have the highest cytotoxicity in breast cancer cells and low cytotoxicity in normal cells. Compound 4a causes ATP depletion and apoptosis of breast cancer MDA-MB-231 cells and triggers reactive oxygen species (ROS)-dependent caspase 3/7 activation. In conclusion, it is worth studying 4-anilinoquinolinylchalcone derivatives further as new potential anticancer agents for the treatment of human cancers. Full article
(This article belongs to the Special Issue Bioactive Compounds in Cancer, Inflammation and Related Diseases)
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15 pages, 5445 KiB  
Article
Guanidine Derivatives Containing the Chalcone Skeleton Are Potent Antiproliferative Compounds against Human Leukemia Cells
by Francisco Estévez-Sarmiento, Ester Saavedra, Ignacio Brouard, Jesús Peyrac, Judith Hernández-Garcés, Celina García, José Quintana and Francisco Estévez
Int. J. Mol. Sci. 2022, 23(24), 15518; https://doi.org/10.3390/ijms232415518 - 08 Dec 2022
Cited by 2 | Viewed by 1293
Abstract
In this study, we investigated the effects of eleven synthetic guanidines containing the 1,3-diphenylpropenone core on the viabilities of six human cancer cells. The most cytotoxic compound against human cancer cells of this series contains a N-tosyl group and a N-methylpiperazine [...] Read more.
In this study, we investigated the effects of eleven synthetic guanidines containing the 1,3-diphenylpropenone core on the viabilities of six human cancer cells. The most cytotoxic compound against human cancer cells of this series contains a N-tosyl group and a N-methylpiperazine moiety 6f. It was cytotoxic against leukemia cells (U-937, HL-60, MOLT-3, and NALM-6) with significant effects against Bcl-2-overexpressing U-937/Bcl-2 cells as well as the human melanoma SK-MEL-1 cell line. It exhibited low cytotoxicity against quiescent or proliferating human peripheral blood mononuclear cells. The IC50 value for the leukemia U-937 cells was 1.6 ± 0.6 µM, a similar value to that in the antineoplastic agent etoposide. The guanidine containing a N-phenyl substituent 6i was also as cytotoxic as the guanidine containing the N-tosyl substituent and the N-methylpiperazine group 6f against human U-937 leukemia cells and both synthetic guanidines were potent apoptotic inducers. Cell death was mediated by the activation of the initiator caspase-9 and the executioner caspase-3, and associated with the release of cytochrome c. These synthetic guanidines are potent cytotoxic compounds against several human leukemia cells and even the human melanoma cell line SK-MEL-1 and might be useful in the development of new strategies in the fight against cancer. Full article
(This article belongs to the Special Issue Bioactive Compounds in Cancer, Inflammation and Related Diseases)
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Review

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23 pages, 1811 KiB  
Review
Potential Therapeutic Targets of Formononetin, a Type of Methoxylated Isoflavone, and Its Role in Cancer Therapy through the Modulation of Signal Transduction Pathways
by Saleh A. Almatroodi, Ahmad Almatroudi, Amjad Ali Khan and Arshad Husain Rahmani
Int. J. Mol. Sci. 2023, 24(11), 9719; https://doi.org/10.3390/ijms24119719 - 03 Jun 2023
Cited by 2 | Viewed by 1806
Abstract
Cancer is one of the main causes of death in all developed and developing countries. Various factors are involved in cancer development and progression, including inflammation and alterations in cellular processes and signaling transduction pathways. Natural compounds have shown health-promoting effects through their [...] Read more.
Cancer is one of the main causes of death in all developed and developing countries. Various factors are involved in cancer development and progression, including inflammation and alterations in cellular processes and signaling transduction pathways. Natural compounds have shown health-promoting effects through their antioxidant and anti-inflammatory potential, having an important role in the inhibition of cancer growth. In this regard, formononetin, a type of isoflavone, plays a significant role in disease management through the modulation of inflammation, angiogenesis, cell cycle, and apoptosis. Furthermore, its role in cancer management has been proven through the regulation of different signal transduction pathways, such as the signal transducer and activator of transcription 3 (STAT 3), Phosphatidyl inositol 3 kinase/protein kinase B (PI3K/Akt), and mitogen activating protein kinase (MAPK) signaling pathways. The anticancer potential of formononetin has been reported against various cancer types, such as breast, cervical, head and neck, colon, and ovarian cancers. This review focuses on the role of formononetin in different cancer types through the modulation of various cell signaling pathways. Moreover, synergistic effect with anticancer drugs and methods to improve bioavailability are explained. Thus, detailed studies based on clinical trials are required to explore the potential role of formononetin in cancer prevention and treatment. Full article
(This article belongs to the Special Issue Bioactive Compounds in Cancer, Inflammation and Related Diseases)
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34 pages, 2050 KiB  
Review
Effects and Mechanisms of Kaempferol in the Management of Cancers through Modulation of Inflammation and Signal Transduction Pathways
by Ahmad Almatroudi, Khaled S. Allemailem, Wanian M. Alwanian, Basmah F. Alharbi, Faris Alrumaihi, Amjad Ali Khan, Saleh A. Almatroodi and Arshad Husain Rahmani
Int. J. Mol. Sci. 2023, 24(10), 8630; https://doi.org/10.3390/ijms24108630 - 11 May 2023
Cited by 8 | Viewed by 3070
Abstract
Cancer is the principal cause of death and its incidence is increasing continuously worldwide. Various treatment approaches are in practice to treat cancer, but these treatment strategies may be associated with severe side effects and also produce drug resistance. However, natural compounds have [...] Read more.
Cancer is the principal cause of death and its incidence is increasing continuously worldwide. Various treatment approaches are in practice to treat cancer, but these treatment strategies may be associated with severe side effects and also produce drug resistance. However, natural compounds have established their role in cancer management with minimal side effects. In this vista, kaempferol, a natural polyphenol, mainly found in vegetables and fruits, has been revealed to have many health-promoting effects. Besides its health-promoting potential, its anti-cancer potential has also been described in in vivo as well as in in vitro studies. The anti-cancer potential of kaempferol has been proven through modulation of cell signaling pathways in addition to the induction of apoptosis and cell cycle arrest in cancer cells. It leads to the activation of tumor suppressor genes, inhibition of angiogenesis, PI3K/AKT pathways, STAT3, transcription factor AP-1, Nrf2 and other cell signaling molecules. Poor bioavailability of this compound is one of the major limitations for its proper and effective disease management actions. Recently, some novel nanoparticle-based formulations have been used to overcome these limitations. The aim of this review is to provide a clear picture regarding the mechanism of action of kaempferol in different cancers through the modulation of cell signaling molecules. Besides this, strategies to improve the efficacy and synergistic effects of this compound have also been described. However, more studies are needed based on clinical trials to fully explore the therapeutic role of this compound, especially in cancer treatment. Full article
(This article belongs to the Special Issue Bioactive Compounds in Cancer, Inflammation and Related Diseases)
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