Antioxidant, anti-inflammatory, antibacterial, and analgesic activities and mechanisms of quinolines, indoles and related derivatives

2021 ◽  
Vol 21 ◽  
Author(s):  
Shan-Shan Zhang ◽  
Qiu-Wan Tan ◽  
Li-Ping Guan
Keyword(s):  
Biological Activities ◽  
Rational Drug Design ◽  
Research Progress ◽  
Lead Compounds ◽  
The Past ◽  
Indole Compounds ◽  
Rational Drug ◽  
Anti Inflammatory ◽  
Analgesic Activities ◽  
Traditional Natural

: Quinoline, isoquinoline and indoles are common heterocyclic compounds. They have many biological activities, such as antioxidant, anti-inflammatory, antibacterial, antitumor, anti-virus, anti-rheumatism, immunity regulation, expectorant, and analgesic. Over the past few centuries, traditional natural products have made great contributions to the discovery and development of new therapeutic agents. Many important drugs have been found from these three classes of compounds. In this mini-review, we mainly cover the research progress on antioxidant, anti-inflammatory, antibacterial, analgesic activities of quinoline, isoquinoline, and indole compounds over the past 20 years (2000-2019). We aim to explore new characteristic groups or structures in the search for active lead compounds and provide a basis for rational drug design.

scholarly journals Diterpenoid Lactones with Anti-Inflammatory Effects from the Aerial Parts of Andrographis paniculata

Molecules ◽  
2019 ◽  
Vol 24 (15) ◽  
pp. 2726 ◽  
Author(s):  
Lin Gan ◽  
Yuanru Zheng ◽  
Lijuan Deng ◽  
Pinghua Sun ◽  
Jiaxi Ye ◽  
...  
Keyword(s):  
Biological Activities ◽  
Quantitative Structure Activity Relationship ◽  
Rational Drug Design ◽  
Andrographis Paniculata ◽  
Aerial Parts ◽  
Rational Drug ◽  
Tnf Α ◽  
Qsar Models ◽  
Anti Inflammatory ◽  
New Compounds

Andrographis paniculata (AP) has been widely used in China for centuries to treat various diseases, and especially to treat inflammation. Diterpenoid lactones are the main anti-inflammatory components of AP. However, systematic chemical composition and biological activities, as well as key pharmacophores, of these diterpenoid lactones from AP have not yet been clearly understood. In this study, 17 diterpenoid lactones, including 2 new compounds, were identified by spectroscopic methods, and most of them attenuated the generation of TNF-α and IL-6 in LPS-induced RAW 274.7 cells examined by ELISA. Pharmacophores of diterpenoid lactones responsible for the anti-inflammatory activities were revealed based on the quantitative structure-activity relationship (QSAR) models. Moreover, new compounds (AP-1 and AP-4) exerted anti-inflammatory activity in LPS microinjection-induced zebrafish, which might be correlated with the inhibition of the translocation of NF-κB p65 from cytoplasm to nucleus. Our study provides guidelines for future structure modification and rational drug design of diterpenoid lactones with anti-inflammatory properties in medical chemistry.

scholarly journals A Review of Terpenes from Marine-Derived Fungi: 2015–2019

Marine Drugs ◽  
2020 ◽  
Vol 18 (6) ◽  
pp. 321 ◽  
Author(s):  
Minghua Jiang ◽  
Zhenger Wu ◽  
Heng Guo ◽  
Lan Liu ◽  
Senhua Chen
Keyword(s):  
Enzyme Inhibitor ◽  
Biological Activities ◽  
Chemical Diversity ◽  
Active Metabolites ◽  
Marine Animals ◽  
Research Papers ◽  
Lead Compounds ◽  
Chemical Structures ◽  
The Past ◽  
Pharmacologically Active

Marine-derived fungi are a significant source of pharmacologically active metabolites with interesting structural properties, especially terpenoids with biological and chemical diversity. In the past five years, there has been a tremendous increase in the rate of new terpenoids from marine-derived fungi being discovered. In this updated review, we examine the chemical structures and bioactive properties of new terpenes from marine-derived fungi, and the biodiversity of these fungi from 2015 to 2019. A total of 140 research papers describing 471 new terpenoids of six groups (monoterpenes, sesquiterpenes, diterpenes, sesterterpenes, triterpenes, and meroterpenes) from 133 marine fungal strains belonging to 34 genera were included. Among them, sesquiterpenes, meroterpenes, and diterpenes comprise the largest proportions of terpenes, and the fungi genera of Penicillium, Aspergillus, and Trichoderma are the dominant producers of terpenoids. The majority of the marine-derived fungi are isolated from live marine matter: marine animals and aquatic plants (including mangrove plants and algae). Moreover, many terpenoids display various bioactivities, including cytotoxicity, antibacterial activity, lethal toxicity, anti-inflammatory activity, enzyme inhibitor activity, etc. In our opinion, the chemical diversity and biological activities of these novel terpenoids will provide medical and chemical researchers with a plenty variety of promising lead compounds for the development of marine drugs.

scholarly journals Anti-Inflammatory and Antinociceptive Activity of Pollen Extract Collected by Stingless Bee Melipona fasciculata

2019 ◽  
Vol 20 (18) ◽  
pp. 4512 ◽  
Author(s):  
Alberto Jorge Oliveira Lopes ◽  
Cleydlenne Costa Vasconcelos ◽  
Francisco Assis Nascimento Pereira ◽  
Rosa Helena Moraes Silva ◽  
Pedro Felipe dos Santos Queiroz ◽  
...  
Keyword(s):  
Native Species ◽  
Biological Activities ◽  
Stingless Bee ◽  
In Vitro Assays ◽  
Pollen Extract ◽  
Biological Potential ◽  
Anti Inflammatory ◽  
Analgesic Activities

The stingless bee, Melipona fasciculata Smith (Apidae, Meliponini), is a native species from Brazil. Their products have high biotechnological potential, however there are no studies about the biological activities of pollen collected by M. fasciculata. In this context, the present study investigated the chemical composition, anti-oxidant, anti-inflammatory, and analgesic activities of hydroethanolic pollen extracts collected by M. fasciculata in three cities in Maranhão State, Brazil. We verified the antioxidant activity of the extracts and inhibitory activity against the cyclooxygenase enzyme using in vitro assays and in allowed to select the extract with higher efficiency to be used on in vivo assays. In these trials, the selected extract showed high anti-inflammatory activity as well as nociceptive effects at central and peripheral level, suggesting that this extract acts on inhibition of histamine release and decreased synthesis of prostaglandins and the in-silico study suggested that polyphenols and acids fatty acids in the extract may be associated with these activities. The results of the present study report the high biological potential of pollen extract and we conclude that the pollen collected by M. fasciculata can be considered as the object of research for new pharmacological alternatives.

Rational Drug Design

2014 ◽  
Vol 4 (1) ◽  
pp. 59-85 ◽  
Author(s):  
Khaled H. Barakat ◽  
Michael Houghton ◽  
D. Lorne Tyrrel ◽  
Jack A. Tuszynski
Keyword(s):  
Drug Design ◽  
Rational Drug Design ◽  
Dimensional Structure ◽  
Computational Tools ◽  
Structure Based Drug Design ◽  
Practical Applications ◽  
3 Dimensional ◽  
Drug Candidates ◽  
The Past ◽  
Rational Drug

For the past three decades rationale drug design (RDD) has been developing as an innovative, rapid and successful way to discover new drug candidates. Many strategies have been followed and several targets with diverse structures and different biological roles have been investigated. Despite the variety of computational tools available, one can broadly divide them into two major classes that can be adopted either separately or in combination. The first class involves structure-based drug design, when the target's 3-dimensional structure is available or it can be computationally generated using homology modeling. On the other hand, when only a set of active molecules is available, and the structure of the target is unknown, ligand-based drug design tools are usually used. This review describes some recent advances in rational drug design, summarizes a number of their practical applications, and discusses both the advantages and shortcomings of the various techniques used.

Synthesis and Biological Evaluation of Polyfluoroalkylated Antipyrines and their Isomeric O-Methylpyrazoles

2019 ◽  
Vol 15 (5) ◽  
pp. 521-536 ◽  
Author(s):  
Natalya Agafonova ◽  
Evgeny Shchegolkov ◽  
Yanina Burgart ◽  
Victor Saloutin ◽  
Alexandra Trefilova ◽  
...  
Keyword(s):  
Biological Activities ◽  
Biological Evaluation ◽  
Antipyretic Activity ◽  
Starting Point ◽  
Anti Inflammatory ◽  
Analgesic Activities ◽  
Synthesis And Biological Evaluation ◽  
Cox 1

Background: Formally belonging to the non-steroidal anti-inflammatory drug class pyrazolones have long been used in medical practices. Objective: Our goal is to synthesize N-methylated 1-aryl-3-polyfluoroalkylpyrazolones as fluorinated analogs of antipyrine, their isomeric O-methylated derivatives resembling celecoxib structure and evaluate biological activities of obtained compounds. Methods: In vitro (permeability) and in vivo (anti-inflammatory and analgesic activities, acute toxicity, hyperalgesia, antipyretic activity, “open field” test) experiments. To suggest the mechanism of biological activity, molecular docking of the synthesized compounds was carried out into the tyrosine site of COX-1/2. Conclusion: The trifluoromethyl antipyrine represents a valuable starting point in design of the lead series for discovery new antipyretic analgesics with anti-inflammatory properties.

Research Progress on Natural Compounds Exerting an Antidepressant Effect through Anti-inflammatory

2021 ◽  
Vol 28 ◽  
Author(s):  
Caixia Yuan ◽  
Yucen Yao ◽  
Tao Liu ◽  
Ying Jin ◽  
Chunrong Yang ◽  
...  
Keyword(s):  
Emotional Disorders ◽  
Natural Compounds ◽  
Research Progress ◽  
Receptor Protein ◽  
Antidepressant Effect ◽  
Cytokine Signaling ◽  
Monoamine Neurotransmitters ◽  
The Past ◽  
Treatment Of Depression ◽  
Anti Inflammatory

: Depression is a common mental illness that belongs to the category of emotional disorders that causes serious damage to the health and life of patients, while inflammation is considered to be one of the important factors that causes depression. In this case, it might be important to explore the possible therapeutic approach by using natural compounds exerting an anti-inflammatory and antidepressant effect, which it filed has not been systematically reviewed recently. Hence, this review aims to systematically sort the literature related to the mechanism of exerting an antidepressant effect through anti-inflammatory actions, and to summarize the related natural products in the past 20 years, in terms of a number of inflammatory related pathways (i.e., the protein kinase B (Akt) pathway, monoamine neurotransmitters (5-hydroxytryptamine and norepinephrine) (5-HT and NE), the nod-like receptor protein-3 (NLRP3) inflammasome, proinflammatory cytokines, neurotrophins, or cytokine-signaling pathways), which might provide a useful reference for the potential treatment of depression.

Synthesis, Characterization and Preliminary Pharmacological Evaluation of Triazolothiadiazoles Derived from some NSAIDs and Thiocarbohydrazide

2018 ◽  
pp. 73-92
Keyword(s):  
Biological Activities ◽  
Enzyme Synthesis ◽  
Control Group ◽  
Paw Edema ◽  
H Nmr ◽  
Pharmacological Test ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Analgesic Activities

The synthesis of new NSAIDs with improved efficacy and selectivity towards COX2, which encouraged by the various biological activities of 1,2,4-triazoles and 1,3,4-thiadiazoles. In this experiment, the production of 1,2,4-triazolothiadiazoles derivatives from Ibuprofen, Naproxen and Indomethacin. We have enhanced anti-inflammatory and analgesic activities by conventional method and microwave-assisted technique, and then compare the time consuming by reaction and yield percent of the product in both way, besides evaluation of anti-inflammatory action of the target compounds by pharmacological test with predictable selectivity towards COX-2 enzyme. Synthesis of the target compounds (P1a-3b, N1a-3b and I1a-3b) has been successfully accomplished by checking purity, characterization, also identification of the synthetic compounds which detected by estimation of physical properties, FT-IR and ¹H-NMR spectroscopy. In vivo potent anti-inflammatory activity of the ending compounds is evaluating in rats utilizing egg-white prompted edema model of inflammation. The experienced compounds (P1a-3b, N1a-3b and I1a-3b) and the reference drugs (Ibuprofen, Naproxen and Indomethacin) produced significant reduction in paw edema in compare to the effect of control group. Wholly tested compounds produced considerable decrease of paw edema in contrast to control group. However, compounds (P3b, N3b and I1b) have considerable more paw edema declining than Ibuprofen, Naproxen and Indomethacin. Intermediate and target compounds are synthesis by microwave method have better result by time and yield in compare with conventional way. The synthesized compounds (Pa1-3b and N1a-3b) may exhibit expected selectivity towards COX-2 enzyme properly due to their large size than its parent Ibuprofen, Naproxen.

scholarly journals Synthesis and analgesic activities of some new 5-chloro-2(3H)-benzoxazolone derivatives

2017 ◽  
Vol 1 (3) ◽  
pp. 235-240 ◽  
Author(s):  
Yusuf Mulazim ◽  
Cevdet Berber ◽  
Hakkı Erdogan ◽  
Melike Hacer Ozkan ◽  
Banu Kesanli
Keyword(s):  
Biological Activities ◽  
Inflammatory Activity ◽  
Microwave Assisted Synthesis ◽  
Tail Flick ◽  
Synthesis Methods ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Tail Flick Test ◽  
Anti Inflammatory ◽  
Analgesic Activities

Abstract Affordable and practical synthesis methods in drug development have always been very attractive. Herein, microwave assisted synthesis was utilized to prepare piperazine substituted 5-chloro-2(3H)-benzoxazolone derivatives in 5 minutes. Structural characterization of these 5-chloro-2(3H)-benzoxazolone derivatives was achieved by IR, NMR, ESI-MS and elemental analysis. Since these types of compounds have been shown to have anti-inflammatory and analgesic activities there biological activities were also examined. Indomethacin (INDO) and acetylsalicylic acid (ASA) were used as reference. Carrageenan-induced hind paw edema in mice test was used to study anti-inflammatory activity. Compound 1 (100 mg / kg dose) showed the longest anti-inflammatory activity among the title compounds synthesized. For the analgesic activities, both hot-plate and tail-flick tests were employed. Compound 3 was found to have the highest activity in the hot-plate test whereas in the tail-flick test, compounds 1 and 2 showed higher anti-nociceptive activity.

Recent advancements on Benzimidazole: A versatile scaffold in medicinal chemistry

2021 ◽  
Vol 21 ◽  
Author(s):  
Zohor Mohammad Mahdi Alzhrani ◽  
Mohammad Mahboob Alam ◽  
Syed Nazreen
Keyword(s):  
Clinical Trials ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Review Article ◽  
Present Review ◽  
Benzimidazole Derivatives ◽  
The Past ◽  
Anti Inflammatory

: Benzimidazole is nitrogen containing fused heterocycle which has been extensively explored in medicinal chemistry. Benzimidizole nucleus has been found to possess various biological activities such as anticancer, antimicrobial, anti-inflammatory, antiviral, antitubercular and antidiabetic. A number of benzimidazoles such as bendamustine, pantoprazole have been approved for the treatment of various illnesses whereas galeterone and GSK461364 are in clinical trials. The present review article gives an overview about the different biological activities exhibited by the benzimidazole derivatives as well as different methods used for the synthesis of benzimidazole derivatives for the past ten years.

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