The Synthesis, Structural Modification and Mode of Anticancer Action of Evodiamine: a review

2021 ◽  
Vol 17 ◽  
Author(s):  
Meixia Fan ◽  
Lei Yao
Keyword(s):  
Structural Modification ◽  
Biological Activities ◽  
Indole Alkaloid ◽  
China National Knowledge Infrastructure ◽  
Structural Modifications ◽  
Knowledge Infrastructure ◽  
Evodia Rutaecarpa ◽  
Wide Range ◽  
Anticancer Mechanism

Background: Finding novel antitumor reagents from naturally occurring alkaloids is a widely accepted strategy. Evodiamine, a tryptamine indole alkaloid isolated from Evodia rutaecarpa, has a wide range of biological activities, such as antitumor, anti-inflammation, and anti-bacteria. Hence, research works on the structural modification of evodiamine will facilitate the discovery of new antitumor drugs. Objective: The recent advances in the synthesis of evodiamine, and studies on the drug design, biological activities, and structure-activity-relationships of its derivatives, published in patents and primary literatures, are reviewed in this paper. Methods: The literatures, including patents and follow-up research papers from 2015 to 2020, related to evodiamine is searched in the Scifinder, PubMed, Espacenet, China National Knowledge Infrastructure (CNKI), and Wanfang databases. The key words are evodiamine, synthesis, modification, anticancer, mechanism. Results: The synthesis of evodiamine are summarized. Then, structural modifications of evodiamine are described, and the possible modes of actions are discussed. Conclusion: Evodiamine has a 6/5/6/6/6 ring system, and the structural modifications are focused on ring A, D, E, C5, N-13, and N-14. Some compounds show promising anticancer potentials and warrant further study.

scholarly journals A Bibliometric Analysis and Visualization of Fractional Order Research in China over Two Decades (2001–2020)

2021 ◽  
Vol 2021 ◽  
pp. 1-16
Author(s):  
Yunfei Yang ◽  
Ke Lv ◽  
Jian Xue ◽  
Xi Huang
Keyword(s):  
Bibliometric Analysis ◽  
Fractional Order ◽  
China National Knowledge Infrastructure ◽  
Research Status ◽  
Knowledge Infrastructure ◽  
Data Source ◽  
Area Of Concern ◽  
Research Frontiers ◽  
Research Hotspots

Fractional order research has interdisciplinary characteristics and has been widely used in the field of natural sciences. Therefore, fractional order research has become an important area of concern for scholars. This paper used 2854 literatures collected from China National Knowledge Infrastructure (CNKI) database from 2001 to 2020 as the data source and used bibliometrics and two visualization methods to conduct bibliometric analysis and visualization research on China’s fractional order research. To begin with, this paper analyzed the time series distribution of publications, the distribution of research institutions, the author cooccurrence network, the distribution of important journals, and the distribution of important literature, which explained the research status of the fractional order. Furthermore, this paper used VOSviewer software to analyze the clustering and density distribution of the fractional order research keywords, which revealed the hotspots of the fractional order research. Finally, with the help of CiteSpace software, the burst keywords were analyzed to further explore the frontiers of fractional order research. This paper systematically reveals the research status, research hotspots, and research frontiers of China’s fractional order research, which can provide certain theoretical and practical references for related follow-up researchers.

scholarly journals Geospatial Distribution of Toxoplasmosis Prevalence among Livestock, Pets and Humans in China, 1984-2020

2021 ◽  
Author(s):  
Yajing Su ◽  
Xia Qiao ◽  
Wei Jia ◽  
Pengtao Wang ◽  
Yuting Kang ◽  
...  
Keyword(s):  
Human Infection ◽  
Toxoplasmic Encephalitis ◽  
China National Knowledge Infrastructure ◽  
Raw Meat ◽  
Sheep And Goats ◽  
Knowledge Infrastructure ◽  
Infection Pressure ◽  
Wide Range ◽  
Visualization Techniques ◽  
And Control

Abstract Background: Toxoplasma gondii (T. gondii) is an important foodborne zoonotic parasite with respect to abortion, intracranial calcifications, congenital hydrocephalus, retinochoroiditis, and toxoplasmic encephalitis in severely immunosuppressed individuals. Undercooked/raw meat containing cyst-stage bradyzoites and contaminated pets are presumed to constitute a major source of human infection. Although many seroprevalence studies have been performed in humans and different animal species in China, data on the geospatial distribution of toxoplasmosis prevalence are extremely scarce. The aim of the present study was to investigate the prevalence and geospatial distribution of toxoplasmosis among livestock, pets and humans in China using geographic information system (GIS) for the prevention and control of toxoplasmosis.Methods: This article is based on the data from PubMed, China National Knowledge Infrastructure (CNKI) and Baidu Scholar databases from 1984 up to 2020 regarding prevalence data of toxoplasmosis among livestock (sheep and goats, swines, cattle and yaks), pets (cats, dogs) and humans in China. Geospatial distribution of the prevalence of toxoplasmosis in these hosts was performed using the GIS visualization techniques.Results: Analysis revealed wide geospatial variation of toxoplasmosis in China. The estimated pooled seroprevalence of T. gondii was ranged from 3.98% to 43.02% among sheep and goats in China, 0.75% to 30.34% in cattle and yaks, 10.45% to 66.47% in swines, 2.50% to 60.00% in cats, 0.56% to 27.65% in dogs, and 0.72% to 23.41% in humans. The higher seroprevalences of T. gondii were observed in districts Chongqing, Zhejiang and Beijing in sheep and goats. The infection rates of T. gondii in cattle and yaks were higher in districts Guizhou, Zhejiang and Chongqing. Moreover, the swines from districts Chongqing and Guizhou were also most severely infected with T. gondii. In cats, districts Shanxi, Hebei and Yunnan had higher seroprevalences of T. gondii and, the infections among dogs were higher in districts Yunnan and Hebei as well. Furthermore, higher infection pressure of T. gondii exists in districts Taiwan and Tibet in humans.Conclusion: The present study indicated that the infection with T. gondii was widely spread in China, with a wide range of variation. The investigation of T. gondii infection in livestock, pets and humans can be useful for assessing T. gondii environmental contamination and the risk for public health. Certain measures can be taken to prevent the prevalence of T. gondii infection in China, such as strengthening the management of livestock farms, keeping the barn clean, preventing feline excreta from polluting environment, using filtered water or water boiling, wearing gloves when handling raw meat and improving the practice of good hand hygiene.

Benzoylthioureas: Design, Synthesis and Antimycobacterial Evaluation

2020 ◽  
Vol 16 (1) ◽  
pp. 93-103
Author(s):  
Tiago O. Brito ◽  
Lethícia O. Abreu ◽  
Karen M. Gomes ◽  
Maria C.S. Lourenço ◽  
Patricia M.L. Pereira ◽  
...  
Keyword(s):  
Benzene Ring ◽  
Biological Activities ◽  
Antitubercular Activity ◽  
Antimycobacterial Activity ◽  
New Drugs ◽  
Design Synthesis ◽  
Thiourea Derivatives ◽  
Structural Modifications ◽  
General Series ◽  
Wide Range

Background: New drugs and strategies to treat tuberculosis (TB) are urgently needed. In this context, thiourea derivatives have a wide range of biological activities, including anti-TB. This fact can be illustrated with the structure of isoxyl, an old anti-TB drug, which has a thiourea as a pharmacophore group. Objective: The aim of this study is to describe the synthesis and the antimycobacterial activity of fifty-nine benzoylthioureas derivatives. Methods: Benzoylthiourea derivatives have been synthesized and evaluated for their activity against Mycobacterium tuberculosis using the MABA assay. After that, a structure-activity relationship study of this series of compounds has been performed. Results and Discussion: Nineteen compounds exhibited antimycobacterial activity between 423.1 and 9.6 μM. In general, we observed that the presence of bromine, chlorine and t-Bu group at the para-position in benzene ring plays an important role in the antitubercular activity of Series A. These substituents were fixed at this position in benzene ring and other groups such as Cl, Br, NO2 and OMe were introduced in the benzoyl ring, leading to the derivatives of Series B. In general, Series B was less cytotoxic than Series A, which indicates that the presence of a substituent at benzoyl ring contributes to an improvement in both antimycobacterial activity and toxicity profiles. Conclusion: Compound 4c could be considered a good prototype to be submitted to further structural modifications in the search for new anti-TB drugs, since it is 1.8 times more active than the first line anti-TB drug ethambutol and 0.65 times less active than isoxyl.

scholarly journals A review on Indole and Benzothiazole derivatives its importance

2019 ◽  
Vol 9 (1-s) ◽  
pp. 505-509 ◽  
Author(s):  
Shaheen Sulthana ◽  
P. Pandian
Keyword(s):  
Heterocyclic Compounds ◽  
Structural Modification ◽  
Biological Activities ◽  
New Product ◽  
Review Article ◽  
Literature Survey ◽  
Pharmacological Activities ◽  
Benzothiazole Derivatives ◽  
Wide Range ◽  
Anti Inflammatory

In recent years heterocyclic compounds analogues and derivatives have attracted wide attention due to their useful biological and pharmacological properties. Indole, Benzothiazole and its analogs are versatile substrates, which can be used for the synthesis of numerous heterocyclic compounds. Indole, Benzothiazole and its derivatives are used in organic synthesis and they are used in evaluating new product that possesses different biological activities. Hence, their extensive structural modification has result in different analogues of Indole and Benzothiazole derivatives depicting wide range of biological and pharmacological activities such as antiviral, anticonvulsant, anti-inflammatory, analgesic, antimicrobial and anticancer. This review article literature survey summarizes the synthesis and pharmacological activities of Indole, Benzothiazole and its derivatives. Keywords: Indole, Benzothiazole, antiviral, anticonvulsant, anti-inflammatory, analgesic, antimicrobial and anticancer

Andrographolide: Synthetic Methods and Biological Activities

2020 ◽  
Vol 20 (16) ◽  
pp. 1633-1652
Author(s):  
Meng Hao ◽  
Min Lv ◽  
Hui Xu
Keyword(s):  
Antimalarial Activity ◽  
Biological Activities ◽  
Biological Properties ◽  
Hepatoprotective Activity ◽  
Synthetic Methods ◽  
Antidiabetic Activity ◽  
Structural Modifications ◽  
Structure Activity ◽  
Wide Range ◽  
Labdane Diterpenoid

Andrographolide, a labdane diterpenoid, is extracted and isolated from the plants of Andrographis paniculata. Andrographolide and its derivatives exhibited a wide range of biological properties, including anticancer activity, antibacterial activity, hepatoprotective activity, antiinflammatory activity, antiviral activity, antimalarial activity, antidiabetic activity, insecticidal activity, etc. As a continuation, this review aims at giving an overview of the recent advances (from 2015 to 2018) of andrographolide and its derivatives with regard to bioactivities, mechanisms of action, structural modifications, and structure-activity relationships.

Novel anthraquinone compounds as anticancer agents and their potential mechanism

2020 ◽  
Author(s):  
Wei Tian ◽  
Chunmiao Wang ◽  
Danrong Li ◽  
Huaxin Hou
Keyword(s):  
Dna Damage ◽  
Anticancer Activity ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Review Article ◽  
Potential Mechanism ◽  
Structural Modifications ◽  
Design And Synthesis ◽  
Cycle Arrest ◽  
Anticancer Mechanism

Anthraquinones exhibit a unique anticancer activity. Since their discovery, medicinal chemists have made several structural modifications, resulting in the design and synthesis of a large number of novel anthraquinone compounds with different biological activities. In general, anthraquinone compounds have been considered to have anticancer activity mainly through DNA damage, cycle arrest and apoptosis. However, recent studies have shown that novel anthraquinone compounds may also inhibit cancer through paraptosis, autophagy, radiosensitising, overcoming chemoresistance and other methods. This Review article provides an overview of novel anthraquinone compounds that have been developed as anticancer agents in recent years and focuses on their anticancer mechanism.

scholarly journals Bioactivities and Structure–Activity Relationships of Fusidic Acid Derivatives: A Review

2021 ◽  
Vol 12 ◽  
Author(s):  
Junjun Long ◽  
Wentao Ji ◽  
Doudou Zhang ◽  
Yifei Zhu ◽  
Yi Bi
Keyword(s):  
Fusidic Acid ◽  
Structural Modification ◽  
Biological Activities ◽  
Pharmacological Activities ◽  
Structure Activity ◽  
Wide Range ◽  
Resistance Reversal ◽  
Anti Inflammation

Fusidic acid (FA) is a natural tetracyclic triterpene isolated from fungi, which is clinically used for systemic and local staphylococcal infections, including methicillin-resistant Staphylococcus aureus and coagulase-negative staphylococci infections. FA and its derivatives have been shown to possess a wide range of pharmacological activities, including antibacterial, antimalarial, antituberculosis, anticancer, tumor multidrug resistance reversal, anti-inflammation, antifungal, and antiviral activity in vivo and in vitro. The semisynthesis, structural modification and biological activities of FA derivatives have been extensively studied in recent years. This review summarized the biological activities and structure–activity relationship (SAR) of FA in the last two decades. This summary can prove useful information for drug exploration of FA derivatives.

Pharmacologically potentials of different substituted coumarin derivatives

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Benzene Ring ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
Pharmacological Properties ◽  
Coumarin Derivatives ◽  
Wide Range ◽  
Anti Oxidant ◽  
Anti Inflammatory ◽  
Coumarin Compounds

Coumarin and its derivatives are widely spread in nature. Coumarin goes to agroup as benzopyrones, which consists of a benzene ring connected to a pyronemoiety. Coumarins displayed a broad range of pharmacologically useful profile.Coumarins are considered as a promising group of bioactive compounds thatexhibited a wide range of biological activities like anti-microbial, anti-viral,antiparasitic, anti-helmintic, analgesic, anti-inflammatory, anti-diabetic, anticancer,anti-oxidant, anti-proliferative, anti-convulsant, and antihypertensiveactivities etc. The coumarin compounds have immense interest due to theirdiverse pharmacological properties. In particular, these biological activities makecoumarin compounds more attractive and testing as novel therapeuticcompounds.

Synthesis, Characterization and Antiproliferative Activity Assessment of a Novel 1H-5-mercapto-1,2,4 Triazole Derivative

2017 ◽  
Vol 68 (4) ◽  
pp. 745-747 ◽  
Author(s):  
Marius Mioc ◽  
Sorin Avram ◽  
Vasile Bercean ◽  
Mihaela Balan Porcarasu ◽  
Codruta Soica ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Biological Activities ◽  
Cancer Cell Line ◽  
Vascular Endothelial ◽  
Triazole Derivative ◽  
Activity Assessment ◽  
Wide Range ◽  
Specific Receptors ◽  
Endothelial Growth Factor ◽  
Selection Of

Angiogenesis plays an important function in tumor proliferation, one of the main angiogenic promoters being the vascular endothelial growth factor (VEGF) which activates specific receptors, particularly VEGFR-2. Thus, VEGFR-2 has become an essential therapeutic target in the development of new antitumor drugs. 1,2,4-triazoles show a wide range of biological activities, including antitumor effect, which was documented by numerous reports. In the current study the selection of 5-mercapto-1,2,4-triazole structure (1H-3-styryl-5-benzylidenehydrazino-carbonyl-methylsulfanil-1,2,4-triazole, Tz3a.7) was conducted based on molecular docking that emphasized it as suitable ligand for VEGFR-2 and EGFR1 receptors. Compound Tz3a.7 was synthesized and physicochemically and biologically evaluated thus revealing a moderate antiproliferative activity against breast cancer cell line MDA-MB-231.

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