scholarly journals Pinocembrin: A Novel Natural Compound with Versatile Pharmacological and Biological Activities

2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
Azhar Rasul ◽  
Faya Martin Millimouno ◽  
Wafa Ali Eltayb ◽  
Muhammad Ali ◽  
Jiang Li ◽  
...  
Keyword(s):  
Time Window ◽  
Biological Activities ◽  
New Drugs ◽  
Pharmacological Effects ◽  
Anticancer Activities ◽  
Anti Inflammatory ◽  
Cerebral Ischemic ◽  
Sites Of Action ◽  
Almost All ◽  
Apoptotic Effects

Pinocembrin (5,7-dihydroxyflavanone) is one of the primary flavonoids isolated from the variety of plants, mainly fromPinusheartwood,Eucalyptus, Populus, Euphorbia, andSparattosperma leucanthum, in the diverse flora and purified by various chromatographic techniques. Pinocembrin is a major flavonoid molecule incorporated as multifunctional in the pharmaceutical industry. Its vast range of pharmacological activities has been well researched including antimicrobial, anti-inflammatory, antioxidant, and anticancer activities. In addition, pinocembrin can be used as neuroprotective against cerebral ischemic injury with a wide therapeutic time window, which may be attributed to its antiexcitotoxic effects. Pinocembrin exhibits pharmacological effects on almost all systems, and our aim is to review the pharmacological and therapeutic applications of pinocembrin with specific emphasis on mechanisms of actions. The design of new drugs based on the pharmacological effects of pinocembrin could be beneficial. This review suggests that pinocembrin is a potentially promising pharmacological candidate, but additional studies and clinical trials are required to determine its specific intracellular sites of action and derivative targets in order to fully understand the mechanism of its anti-inflammatory, anticancer, and apoptotic effects to further validate its medical applications.

scholarly journals Terpenoids and Their Biological Activities from Cinnamomum: A Review

2020 ◽  
Vol 2020 ◽  
pp. 1-14
Author(s):  
Meiting Wu ◽  
Lin Ni ◽  
Haixiao Lu ◽  
Huiyou Xu ◽  
Shuangquan Zou ◽  
...  
Keyword(s):  
Biological Activities ◽  
Biological Effects ◽  
Pharmacological Effects ◽  
Bioactive Components ◽  
Anticancer Activities ◽  
Chemical Structures ◽  
The Family ◽  
Beneficial Uses ◽  
The Future ◽  
Depth Study

Cinnamomum is a genus of the family Lauraceae, which has been recognized worldwide as an important genus due to its beneficial uses. A great deal of research on its phytochemistry and pharmacological effects has been conducted. It is noteworthy that terpenoids are the characteristic of Cinnamomum due to the peculiar structures and significant biological effects. For a more in-depth study and the better use of Cinnamomum plants in the future, the chemical structures and biological effects of terpenoids obtained from Cinnamomum were summarized in the present study. To date, a total of 181 terpenoids with various skeletons have been isolated from Cinnamomum. These compounds have been demonstrated to play an important role in immunomodulatory, anti-inflammatory, antimicrobial, antioxidant, and anticancer activities. However, studies on the bioactive components from Cinnamomum plants have only focused on a dozen species. Hence, further studies on the potential pharmacological effects need to be conducted in the future.

scholarly journals Intestinal Anti-Inflammatory Activity of Terpenes in Experimental Models (2010–2020): A Review

Molecules ◽  
2020 ◽  
Vol 25 (22) ◽  
pp. 5430
Author(s):  
Maria Elaine Araruna ◽  
Catarina Serafim ◽  
Edvaldo Alves Júnior ◽  
Clelia Hiruma-Lima ◽  
Margareth Diniz ◽  
...  
Keyword(s):  
Gastrointestinal Tract ◽  
Biological Activities ◽  
Structural Diversity ◽  
Experimental Models ◽  
New Drugs ◽  
Inflammatory Activity ◽  
Bowel Diseases ◽  
Inflammatory Bowel ◽  
Anti Inflammatory

Inflammatory bowel diseases (IBDs) refer to a group of disorders characterized by inflammation in the mucosa of the gastrointestinal tract, which mainly comprises Crohn’s disease (CD) and ulcerative colitis (UC). IBDs are characterized by inflammation of the intestinal mucosa, are highly debilitating, and are without a definitive cure. Their pathogenesis has not yet been fully elucidated; however, it is assumed that genetic, immunological, and environmental factors are involved. People affected by IBDs have relapses, and therapeutic regimens are not always able to keep symptoms in remission over the long term. Natural products emerge as an alternative for the development of new drugs; bioactive compounds are promising in the treatment of several disorders, among them those that affect the gastrointestinal tract, due to their wide structural diversity and biological activities. This review compiles 12 terpenes with intestinal anti-inflammatory activity evaluated in animal models and in vitro studies. The therapeutic approach to IBDs using terpenes acts basically to prevent oxidative stress, combat dysbiosis, restore intestinal permeability, and improve the inflammation process in different signaling pathways.

Maydis Stigma Elicits Analgesia and Blocks Edema in Mice and Inhibits Inflammation in Macrophages

2017 ◽  
Vol 45 (07) ◽  
pp. 1477-1496 ◽  
Author(s):  
Yun Hee Jeong ◽  
You-Chang Oh ◽  
Won-Kyung Cho ◽  
Hye Jin Yang ◽  
Jin Yeul Ma
Keyword(s):  
Acetic Acid ◽  
Target Genes ◽  
Biological Activities ◽  
Scientific Evidence ◽  
Ethanolic Extract ◽  
Anticancer Activities ◽  
Ear Edema ◽  
Anti Inflammatory

Maydis Stigma (MS) is an herb traditionally used in many parts of the world. Previous studies have reported that MS plays a role in several biological activities, including antidiabetic and anticancer activities. However, the effects of a MS ethanolic extract (MSE) on the anti-inflammatory cellular mechanism remain unclear. Here, we investigated the anti-inflammatory properties of MSE and its molecular mechanism both in vitro and in vivo. The effects of MSE on the production of inflammatory mediators, cytokines, and related proteins and the identification of target genes were determined using LPS-stimulated macrophages. We also determined the analgesic and anti-inflammatory effects of MSE by examining acetic acid-induced writhing responses and xylene-induced ear edema in mice. Our results indicated that MSE markedly decreased iNOS and COX-2 levels without causing cytotoxicity and suppressed the secretion of NO in LPS-stimulated macrophages. MSE also inhibited the production of proinflammatory cytokines, such as TNF-[Formula: see text], IL-6, and IL-1[Formula: see text], and induced the expression of HO-1. Moreover, MSE treatment significantly reduced the LPS-stimulated activation of MAPK, NF-[Formula: see text]B, and AP-1. Furthermore, MSE exerted an analgesic effect on the acetic acid-induced abdominal writhing response test and an anti-inflammatory effect on xylene-induced ear edema in ICR mice. Finally, we investigated the components of MSE using UPLC-ESI-MS and found that it contains the maysin as a marker component. Overall, these observations demonstrate that MSE has anti-inflammatory and antinociceptive effects both in vitro and in vivo, which may provide new scientific evidence for its use as a potential therapeutic agent for the treatment of inflammation.

scholarly journals Biological Properties of Some Volatile Phenylpropanoids

2016 ◽  
Vol 11 (10) ◽  
pp. 1934578X1601101 ◽  
Author(s):  
Radmila Ilijeva ◽  
Gerhard Buchbauer
Keyword(s):  
Clinical Trials ◽  
Essential Oils ◽  
Mechanism Of Action ◽  
Biological Activities ◽  
Biological Properties ◽  
Anticancer Activities ◽  
Pharmacological Activities ◽  
Prevention And Treatment ◽  
Pharmaceutical Industries ◽  
Almost All

Plants and their extracts are the new field of interest for many scientists and also of some pharmaceutical industries. In order to provide more information for their usage in the prevention and treatment of diseases many clinical trials and researches are being carried out. In this review the biological activities and the mechanism of action of volatile phenylpropanoids (PPs) found in essential oils (EOs) are presented. The aim of this overview is to show that volatile PPs found in EOs can exert many of the biological activities which are generally attributed to EOs. Almost all of the PPs possess antimicrobial, anti-inflammatory and anticancer activities. These are related to the different substitution of the phenylpropane molecule. For each isolated group not only one, but more pharmacological activities can be credited.

Recent development of tetrahydro-quinoline/isoquinoline based compounds as anticancer agents

2021 ◽  
Vol 21 ◽  
Author(s):  
Pratik Yadav ◽  
Ashish Kumar ◽  
Ismail Althagafi ◽  
Vishal Nemaysh ◽  
Reeta Rai ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Human Cancer ◽  
Biological Activities ◽  
Cancer Cell Lines ◽  
New Drugs ◽  
Anticancer Activities ◽  
Human Cancer Cell Lines ◽  
Anticancer Properties

: Tetrahydroquinoline and isoquinoline scaffolds are important class heterocyclic compounds, which is implied for the development of new drugs and diagnostic for therapeutic function. Naturally occurring as well as synthetic tetrahydroquinolines/isoquinolines possess many different biological activities and have been testified as remarkable cytotoxic and potency in human cancer cell lines. Tetrahydroquinoline/isoquinolines based compounds displayed a key role in the development of anticancer drugs or lead molecules and acting through various mechanisms such as cell proliferation, apoptosis, DNA fragmentation, inhibition of tubulin polymerization, induced cell cycle arrest, interruption of cell migration, and modulation. The number of tetrahydroquinoline/isoquinoline derivatives has been reported as potent anticancer agents. Due to promising anticancer activities and wide-ranging properties of these molecules, we have compiled the literature for the synthesis and anticancer properties of various tetrahydroquinolines and isoquinolines. We have reported the synthesis of potent tetrahydroquinoline/isoquinoline molecules of the last 10 years with their anticancer properties in various cancer cell lines and stated their half-maximal inhibitory concentration (IC50). In addition, we also considered the discussion of molecular docking and structural activity relationship wherever provided to understand the possible mode of activity a target involved and structural feature responsible for the better activity, so the reader can directly find the detail for designing new anticancer agents.

scholarly journals Natural Chalcones in Chinese Materia Medica: Licorice

2020 ◽  
Vol 2020 ◽  
pp. 1-14
Author(s):  
Danni Wang ◽  
Jing Liang ◽  
Jing Zhang ◽  
Yuefei Wang ◽  
Xin Chai
Keyword(s):  
Clinical Practice ◽  
Theoretical Basis ◽  
Biological Activities ◽  
Pivotal Role ◽  
Pharmacological Effects ◽  
Chinese Materia Medica ◽  
Materia Medica ◽  
Wide Range ◽  
Anti Inflammatory

Licorice is an important Chinese materia medica frequently used in clinical practice, which contains more than 20 triterpenoids and 300 flavonoids. Chalcone, one of the major classes of flavonoid, has a variety of biological activities and is widely distributed in nature. To date, about 42 chalcones have been isolated and identified from licorice. These chalcones play a pivotal role when licorice exerts its pharmacological effects. According to the research reports, these compounds have a wide range of biological activities, containing anticancer, anti-inflammatory, antimicrobial, antioxidative, antiviral, antidiabetic, antidepressive, hepatoprotective activities, and so on. This review aims to summarize structures and biological activities of chalcones from licorice. We hope that this work can provide a theoretical basis for the further studies of chalcones from licorice.

scholarly journals Synthesis and Biological Evaluation of Some Novel Quinoline based Chalcones as Potent Antimalarial, Anti-inflammatory, Antioxidant and Antidiabetic Agents

2020 ◽  
Vol 32 (4) ◽  
pp. 959-964
Author(s):  
Nargisbano A. Peerzade ◽  
Shravan Y. Jadhav ◽  
Raghunath B. Bhosale
Keyword(s):  
Antimalarial Activity ◽  
Biological Activities ◽  
13C Nmr Spectroscopy ◽  
Biological Evaluation ◽  
New Drugs ◽  
Antidiabetic Activity ◽  
High Yield ◽  
Excellent Activity ◽  
Anti Inflammatory

The objective of the present study was to synthesize a series of some novel quinoline based methoxy substituted chalcones and to evaluate their in vitro antimalarial, anti-inflammatory, antioxidant and antidiabetic activitites. The quinoline based chalcones was synthesized by condensation of 2-chloro-3-formyl qunoline with various methoxy substituted acetophenone in presence of NaOH. The Claisen-Schmidt condensation gave high yield of quinoline based chalcones. Synthesis of 2-chloro-3-formyl quinoline was carried out by Vilsmeir-Haack reaction on acetanilide and 4-methoxy acetanilide which on cyclization along with formylation give corresponding 2-chloro-3-formyl quinoline. The synthesized compounds were screened for in vitro antimalarial, anti-inflammatory, antioxiadant and antidiabetic activities. The structures of the synthesized compounds were characterized by infrared, 1H NMR and 13C NMR spectroscopy. Compounds 1f and 1h showed highest antimalarial activity even more than standard chloroquine diphosphate. Compound 1a showed excellent activity whereas 1c and 1d showed potent anti-inflammatory activity as compared to standard diclofenac. On the other hand, compounds 1a and 1g showed excellent antioxidant activity for 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical while compound 1a showed highest inhibition of nitic oxide free radical (NO•) and compound 1h showed highest inhibition for super oxide radical (SOR) as well as highest antidiabetic activity as compared to standard acarbose. All quinolne based chalcones were synthesized in good yields and showed potential biological activities hence they may be helpful for the designing of new drugs.

Flavonoids in the Treatment of Alzheimer’s and Other Neurodegenerative Diseases

2018 ◽  
Vol 25 (27) ◽  
pp. 3228-3246 ◽  
Author(s):  
Cristina Airoldi ◽  
Barbara La Ferla ◽  
Giuseppe D`Orazio ◽  
Carlotta Ciaramelli ◽  
Alessandro Palmioli
Keyword(s):  
Neurodegenerative Diseases ◽  
Biological Activities ◽  
Chemical Properties ◽  
New Drugs ◽  
Terrestrial Plants ◽  
Positive Effects ◽  
Brain Functions ◽  
Age Related ◽  
Physico Chemical ◽  
Almost All

Flavonoids are phytochemicals present in almost all terrestrial plants and, as a consequence, in plant-based foods, and thus consumed by humans through diet. Recent evidences suggest that several flavonoids have positive effects against dementia and Alzheimer’s disease, reversing age-related declines in neurocognitive performances. In this review, we provide a general classification of natural and synthetic flavonoids, a description of their physico-chemical properties, in particular their redox properties and stability, and an extensive overview about their biological activities and structure-activity relationship in the field of neurodegenerative diseases. In addition, a section will be dedicated to the synthetic strategies for the preparation of bioactive derivatives. This information will be essential for the design and development of new drugs that can improve brain functions.

Isatin hybrids and Their Pharmacological Investigations

2020 ◽  
Vol 20 ◽  
Author(s):  
Bhushan D. Varpe ◽  
Amol A. Kulkarni ◽  
Shailaja B. Jadhav ◽  
Anil S. Mali ◽  
Shravan Y. Jadhav
Keyword(s):  
Biological Activities ◽  
New Drugs ◽  
Pharmacological Properties ◽  
Anticancer Activities ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Molecular Hybrids ◽  
Anti Hiv

Abstract:: Hybridization is an important strategy to design molecules that can be effectively used to treat fatal diseases known to mankind. Molecular hybrids and their pharmacological investigations aided to discover several potent isatin (Indole 2, 3 dione) derivatives with anti-HIV, antimalarial, antitubercular, antibacterial, and anticancer activities. Indole‐2,3‐dione and their derivatives have diverse pharmacological properties and have a prominent role in the discovery of new drugs. To understand the various approaches in designing new molecules based on isatin nucleus analysis of various pharmacophore hybrids, spacers/linkers between pharmacophores and isatin for hybridization and their biological activities is important. This review discusses the progress in developing isatin hybrids as biologically effective agents, and their crucial aspects of design and structure-activity relationships.

Host Defence Cryptides from Human Apolipoproteins: Applications in Medicinal Chemistry

2020 ◽  
Vol 20 (14) ◽  
pp. 1324-1337 ◽  
Author(s):  
Rosa Gaglione ◽  
Elio Pizzo ◽  
Eugenio Notomista ◽  
Cesar de la Fuente-Nunez ◽  
Angela Arciello
Keyword(s):  
Bioactive Peptides ◽  
Biological Activities ◽  
Host Defence ◽  
New Drugs ◽  
In Vitro Assays ◽  
Protein Cleavage ◽  
Anticancer Activities ◽  
In Vivo Experiments

Several eukaryotic proteins with defined physiological roles may act as precursors of cryptic bioactive peptides released upon protein cleavage by the host and/or bacterial proteases. Based on this, the term “cryptome” has been used to define the unique portion of the proteome encompassing proteins with the ability to generate bioactive peptides (cryptides) and proteins (crypteins) upon proteolytic cleavage. Hence, the cryptome represents a source of peptides with potential pharmacological interest. Among eukaryotic precursor proteins, human apolipoproteins play an important role, since promising bioactive peptides have been identified and characterized from apolipoproteins E, B, and A-I sequences. Human apolipoproteins derived peptides have been shown to exhibit antibacterial, anti-biofilm, antiviral, anti-inflammatory, anti-atherogenic, antioxidant, or anticancer activities in in vitro assays and, in some cases, also in in vivo experiments on animal models. The most interesting Host Defence Peptides (HDPs) identified thus far in human apolipoproteins are described here with a focus on their biological activities applicable to biomedicine. Altogether, reported evidence clearly indicates that cryptic peptides represent promising templates for the generation of new drugs and therapeutics against infectious diseases.

Sign in / Sign up

Export Citation Format

Share Document