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Cepharanthine: Pharmacological Properties and Medical Applications

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A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (30 July 2023) | Viewed by 8705

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Special Issue Editors

Dr. Huahao Fan

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Guest Editor

College of life science and technology, Beijing University of Chemical Technology, Beijing, China
Interests: coronavirus; enterovirus; drug screening; immune escape; phage

Prof. Dr. Yigang Tong

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Guest Editor

College of life science and technology, Beijing University of Chemical Technology, Beijing, China
Interests: bio-safety; microbiology; genomics; bioinformatics; high-throughput sequencing; super-resistant bacteria; bacteriophagology

Dr. Guifang Dou

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Guest Editor

Department of Pharmaceutical Sciences, Beijing Institute of Radiation Medicine, Beijing, China
Interests: pharmaceutical analysis; natural product; pharmacology; clinical pharmacokinetics; drug discovery; biopharmaceutics pharmacokinetics

Dr. Chi Song

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Guest Editor

Institute of Herbgenomics, Chengdu University of Traditional Chinese Medicine, Chengdu, China
Interests: medicinal plants; high-throughput sequencing technology; bioinformatics

Special Issue Information

Dear Colleagues,

Cepharanthine is a dibenzyl isoquinoline alkaloid extracted from the rhizomes of Stephania. It was discovered in 1934, and has been used as a drug since the 1950s to treat a variety of chronic diseases, such as leukopenia, alopecia areata, bronchial asthma and snakebite. It has anti-tumor, anti-inflammatory, anti-oxidation, anti-viral, anti-parasitic, anti-bacterial, bone absorption inhibition, and immune regulation activities. At present, the extensive medicinal values of cepharanthine have been widely investigated, but the clinical application of cepharanthine is limited due to its low solubility and low bioavailability. Therefore, further research on its pharmacological properties and medical application can improve the existing deficiencies and promote the application of cepharanthine in medicine and the development of related industries.

This Special Issue will publish studies related to cepharanthine, including the synthesis, metabolism, drug activity, related signaling pathways, pharmacokinetics, toxicology, clinical application and other studies related to cepharanthine, and encourages submissions from all fields of pharmacology, life science and clinical medicine. Topics of special interest include, but are not limited to, anti-tumor, anti-inflammatory, immunomodulatory, epidemiological studies of cepharanthine, and studies related to its pharmacological properties and medical applications in inhibiting bone absorption, treating alopecia, treating snakebite, and regulating signaling pathways.

Dr. Huahao Fan
Prof. Dr. Yigang Tong
Dr. Guifang Dou
Dr. Chi Song
Guest Editors

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. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). 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

cepharanthine
pharmacological properties
medical applications
clinical medicine
natural products

Published Papers (4 papers)

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Research

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12 pages, 2346 KiB

Open AccessArticle

Cepharanthine Dry Powder Inhaler for the Treatment of Acute Lung Injury

by Di Liang, Wanmei Wang, Guangrui Chen, Jian Li, Guifang Dou, Hui Gan, Peng Han, Lina Du and Ruolan Gu

Molecules 2023, 28(11), 4441; https://doi.org/10.3390/molecules28114441 - 30 May 2023

Cited by 2 | Viewed by 1670

Abstract

Severe acute respiratory syndrome Coronavirus 2 (SARS-CoV-2) induces a severe cytokine storm that may cause acute lung injury/acute respiratory distress syndrome (ALI/ARDS) with high clinical morbidity and mortality in infected individuals. Cepharanthine (CEP) is a bisbenzylisoquinoline alkaloid isolated and extracted from Stephania cepharantha Hayata. It exhibits various pharmacological effects, including antioxidant, anti-inflammatory, immunomodulatory, anti-tumor, and antiviral activities. The low oral bioavailability of CEP can be attributed to its poor water solubility. In this study, we utilized the freeze-drying method to prepare dry powder inhalers (DPI) for the treatment of acute lung injury (ALI) in rats via pulmonary administration. According to the powder properties study, the aerodynamic median diameter (D_a) of the DPIs was 3.2 μm, and the in vitro lung deposition rate was 30.26; thus, meeting the Chinese Pharmacopoeia standard for pulmonary inhalation administration. We established an ALI rat model by intratracheal injection of hydrochloric acid (1.2 mL/kg, pH = 1.25). At 1 h after the model’s establishment, CEP dry powder inhalers (CEP DPIs) (30 mg/kg) were sprayed into the lungs of rats with ALI via the trachea. Compared with the model group, the treatment group exhibited a reduced pulmonary edema and hemorrhage, and significantly reduced content of inflammatory factors (TNF-α, IL-6 and total protein) in their lungs (p < 0.01), indicating that the main mechanism of CEP underlying the treatment of ALI is anti-inflammation. Overall, the dry powder inhaler can deliver the drug directly to the site of the disease, increasing the intrapulmonary utilization of CEP and improving its efficacy, making it a promising inhalable formulation for the treatment of ALI. Full article

(This article belongs to the Special Issue Cepharanthine: Pharmacological Properties and Medical Applications)

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14 pages, 2711 KiB

Open AccessArticle

Cepharanthine Alleviates DSS-Induced Ulcerative Colitis via Regulating Aconitate Decarboxylase 1 Expression and Macrophage Infiltration

by Min-Na Zhang, Rui Xie, Hong-Gang Wang, Xin Wen, Jing-Yi Wang, Le He, Meng-Hui Zhang and Xiao-Zhong Yang

Molecules 2023, 28(3), 1060; https://doi.org/10.3390/molecules28031060 - 20 Jan 2023

Cited by 4 | Viewed by 2321

Abstract

Cepharanthine (CEP), a bisbenzylisoquinoline alkaloid from tubers of Stephania, protects against some inflammatory diseases. Aconitate decarboxylase 1 (ACOD1) is also known as immune-responsive gene 1 (IRG1), which plays an important immunometabolism role in inflammatory diseases by mediating the production of itaconic acid. ACOD1 exhibits abnormal expression in ulcerative colitis (UC). However, whether CEP can combat UC by affecting ACOD1 expression remains unanswered. This study was designed to explore the protective effects and mechanisms of CEP in treating colitis through in vitro and in vivo experiments. In vitro assays indicated that CEP inhibited LPS-induced secretion of pro-inflammatory cytokines and ACOD1 expression in RAW264.7 macrophages. Additionally, in the mouse model of DSS-induced colitis, CEP decreased macrophage infiltration and ACOD1 expression in colon tissue. After treatment with antibiotics (Abx), the expression of ACOD1 changed with the composition of gut microbiota. Correlation analysis also revealed that Family-XIII-AD3011-group and Rumini-clostridium-6 were positively correlated with ACOD1 expression level. Additionally, data of the integrative Human Microbiome Project (iHMP) showed that ACOD1 was highly expressed in the colon tissue of UC patients and this expression was positively correlated with the severity of intestinal inflammation. Collectively, CEP can counter UC by modulating gut microbiota and inhibiting the expression of ACOD1. CEP may serve as a potential pharmaceutical candidate in the treatment of UC. Full article

(This article belongs to the Special Issue Cepharanthine: Pharmacological Properties and Medical Applications)

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15 pages, 5240 KiB

Open AccessArticle

Cepharanthine Ameliorates Pulmonary Fibrosis by Inhibiting the NF-κB/NLRP3 Pathway, Fibroblast-to-Myofibroblast Transition and Inflammation

by Guangrui Chen, Jian Li, Huimeng Liu, Huiyu Zhou, Mingqiu Liu, Di Liang, Zhiyun Meng, Hui Gan, Zhuona Wu, Xiaoxia Zhu, Peng Han, Taoyun Liu, Ruolan Gu, Shuchen Liu and Guifang Dou

Molecules 2023, 28(2), 753; https://doi.org/10.3390/molecules28020753 - 11 Jan 2023

Cited by 3 | Viewed by 2138

Abstract

Pulmonary fibrosis (PF) is one of the sequelae of Corona Virus Disease 2019 (COVID-19), and currently, lung transplantation is the only viable treatment option. Hence, other effective treatments are urgently required. We investigated the therapeutic effects of an approved botanical drug, cepharanthine (CEP), in a cell culture model of transforming growth factor-β1 (TGF-β1) and bleomycin (BLM)-induced pulmonary fibrosis rat models both in vitro and in vivo. In this study, CEP and pirfenidone (PFD) suppressed BLM-induced lung tissue inflammation, proliferation of blue collagen fibers, and damage to lung structures in vivo. Furthermore, we also found increased collagen deposition marked by α-smooth muscle actin (α-SMA) and Collagen Type I Alpha 1 (COL1A1), which was significantly alleviated by the addition of PFD and CEP. Moreover, we elucidated the underlying mechanism of CEP against PF in vitro. Various assays confirmed that CEP reduced the viability and migration and promoted apoptosis of myofibroblasts. The expression levels of myofibroblast markers, including COL1A1, vimentin, α-SMA, and Matrix Metallopeptidase 2 (MMP2), were also suppressed by CEP. Simultaneously, CEP significantly suppressed the elevated Phospho-NF-κB p65 (p-p65)/NF-κB p65 (p65) ratio, NOD-like receptor thermal protein domain associated protein 3 (NLRP3) levels, and elevated inhibitor of NF-κB Alpha (IκBα) degradation and reversed the progression of PF. Hence, our study demonstrated that CEP prevented myofibroblast activation and treated BLM-induced pulmonary fibrosis in a dose-dependent manner by regulating nuclear factor kappa-B (NF-κB)/ NLRP3 signaling, thereby suggesting that CEP has potential clinical application in pulmonary fibrosis in the future. Full article

(This article belongs to the Special Issue Cepharanthine: Pharmacological Properties and Medical Applications)

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Review

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34 pages, 2119 KiB

Open AccessReview

Pharmacological Activity of Cepharanthine

by Ke Liu, Bixia Hong, Shuqi Wang, Fuxing Lou, Yecheng You, Ruolan Hu, Amna Shafqat, Huahao Fan and Yigang Tong

Molecules 2023, 28(13), 5019; https://doi.org/10.3390/molecules28135019 - 27 Jun 2023

Cited by 3 | Viewed by 1874

Abstract

Cepharanthine, a natural bisbenzylisoquinoline (BBIQ) alkaloid isolated from the plant Stephania Cephalantha Hayata, is the only bisbenzylisoquinoline alkaloid approved for human use and has been used in the clinic for more than 70 years. Cepharanthine has a variety of medicinal properties, including signaling pathway inhibitory activities, immunomodulatory activities, and antiviral activities. Recently, cepharanthine has been confirmed to greatly inhibit SARS-CoV-2 infection. Therefore, we aimed to describe the pharmacological properties and mechanisms of cepharanthine, mainly including antitumor, anti-inflammatory, anti-pathogen activities, inhibition of bone resorption, treatment of alopecia, treatment of snake bite, and other activities. At the same time, we analyzed and summarized the potential antiviral mechanism of cepharanthine and concluded that one of the most important anti-viral mechanisms of cepharanthine may be the stability of plasma membrane fluidity. Additionally, we explained its safety and bioavailability, which provides evidence for cepharanthine as a potential drug for the treatment of a variety of diseases. Finally, we further discuss the potential new clinical applications of cepharanthine and provide direction for its future development. Full article

(This article belongs to the Special Issue Cepharanthine: Pharmacological Properties and Medical Applications)

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