scholarly journals Plectranthus ecklonii Benth: A Comprehensive Review Into its Phytochemistry and Exerted Biological Activities

2021 ◽  
Vol 12 ◽  
Author(s):  
Ana Ribeirinha Antão ◽  
Gabrielle Bangay ◽  
Eva María Domínguez-Martín ◽  
Ana María Díaz-Lanza ◽  
Patrícia Ríjo
Keyword(s):  
Biological Activities ◽  
Eligibility Criteria ◽  
Database Retrieval ◽  
Pharmaceutical Ingredients ◽  
Chemical Structures ◽  
Potential Applications ◽  
Anti Inflammatory ◽  
Antibacterial And Antifungal ◽  
Pharmaceutical Uses

Ethnopharmacological Relevance:Plectranthus genus (Lamiaceae family) contain several species with acknowledged ethnopharmacological uses, such as, for gastrointestinal and respiratory-related problems, due to their anti-inflammatory, antibacterial and antifungal properties. The bioactivity of isolated medicinal compounds from this genus justifies the increased interest in recent times for species of Plectranthus, placing them in the spotlight for natural product drug development.Aim of the study: To the best of our knowledge, this is the first review on the biological activities of Plectranthus ecklonii Benth. As such, the aim of this review was three-fold: 1) to summarize the chemical compounds isolated from P. ecklonii; 2) to collate the biological activities and mechanisms of action of these compounds from in vitro studies; and 3) to evaluate the documented uses and potential applications of this species, in order to postulate on the direction of pharmaceutical uses of this species.Materials and methods: An extensive database retrieval was performed using the electronic databases Web of Science, PubMed, Google Scholar and ScienceDirect. The search criteria consisted of the keywords “Plectranthus ecklonii”, “Plectranthus ecklonii + review”, “Plectranthus ecklonii + diterpenes” or “Plectranthus ecklonii + abietanes”, “ecklonii + parviflorone D”, searched individually and as combinations. Eligibility criteria were set out and titles in English, Portuguese and Spanish were reviewed, with all references included dating from 1970 to 2021. A total of 169 papers were selected and included. Chemical structures were drawn using ChemDraw 20.0, CID numbers were searched in PubChem and the PRISMA diagram was created using PowerPoint 2012.Results: To date, a total of 28 compounds have been isolated from P. ecklonii, including diterpenes, triterpenes, flavonoids, and hydroxycinnamic acids. Most focused on the antimicrobial action of its constituents, although compounds have demonstrated other bioactivities, namely antioxidant, anti-inflammatory and antitumor. The most recent studies emphasize the diterpenoids, particularly parviflorone D, with the help of nanotechnology.Conclusions: The widespread ethnobotanical and traditional uses of P. ecklonii can be scientifically justified by a range of biological activities, demonstrated by isolated secondary metabolites. These bioactivities showcase the potential of this species in the development of economically important active pharmaceutical ingredients, particularly in anticancer therapy.

scholarly journals In vitro and in vivo biological activities of azulene derivatives with potential applications in medicine

2021 ◽  
Author(s):  
Paweł Bakun ◽  
Beata Czarczynska-Goslinska ◽  
Tomasz Goslinski ◽  
Sebastian Lijewski
Keyword(s):  
Biological Activities ◽  
Biological Properties ◽  
Biologically Active ◽  
Peptic Ulcers ◽  
Artemisia Absinthium ◽  
Potential Applications ◽  
Anti Inflammatory ◽  
Unique Chemical

AbstractAzulene is an aromatic hydrocarbon that possesses a unique chemical structure and interesting biological properties. Azulene derivatives, including guaiazulene or chamazulene, occur in nature as components of many plants and mushrooms, such as Matricaria chamomilla, Artemisia absinthium, Achillea millefolium, and Lactarius indigo. Due to physicochemical properties, azulene and its derivatives have found many potential applications in technology, especially in optoelectronic devices. In medicine, the ingredients of these plants have been widely used for hundreds of years in antiallergic, antibacterial, and anti-inflammatory therapies. Herein, the applications of azulene, its derivatives and their conjugates with biologically active compounds are presented. The potential use of these compounds concerns various areas of medicine, including anti-inflammatory with peptic ulcers, antineoplastic with leukemia, antidiabetes, antiretroviral with HIV-1, antimicrobial, including antimicrobial photodynamic therapy, and antifungal.

Cyclooxygenase Enzyme and Lipid Peroxidation Inhibitory Terpenoids and Steroidal compounds as Major Constituents in Cleome viscosa Leaves

Planta Medica ◽  
2021 ◽  
Author(s):  
Amila Abishake Dissanayake ◽  
Kambou Georges ◽  
Muraleedharan G. Nair
Keyword(s):  
Lipid Peroxidation ◽  
Antioxidant Activity ◽  
Biological Activities ◽  
Chemical Structures ◽  
Ic50 Values ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 1 ◽  
Cleome Viscosa

Bioassay guided study of Cleome viscosa Linn. (Cleomaceae) leaves led to the isolation of a new cembrenoid diterpene (1) and three known compounds (2-4) from the hexane extract. The chemical structures of these compounds were elucidated by spectroscopic methods such as NMR (1D and 2D), HRMS and IR and identified and afforded compound 1, malabaric acid (2), stigmast-4-en-3-one (3) and stigmast-4-ene-3,6-dione (4). This is the first report of compounds 1 and 2 from C. viscosa Linn. Isolates were evaluated for anti-inflammatory activity using in vitro cyclooxygenase enzyme (COX-1 and -2) inhibitory assays. The novel cembrenoid diterpene (1) exhibited IC50 values of 8.4 μM for COX-1 enzyme and 45.2 μM for COX-2 enzyme, respectively. Similarly, malabaric acid (2) exhibited IC50 values of 11.5 μM for COX-1 enzyme and 46.9 μM for COX-2 enzyme, respectively. Their inhibitory activities were in par with non-steroidal anti-inflammatory drugs aspirin, ibuprofen and naproxen. Sterols 3 and 4 gave IC50 values of 62.6 and 67.9 μM, respectively for COX-1 enzyme while indicating weak COX-2 enzyme inhibition. Lipid peroxidation inhibitory (LPO) and MTT assays were used to determine antioxidant activity of these compounds. Compounds 1-4 showed LPO inhibition with IC50 values between 82 and 100 µM and moderate antioxidant activity in the MTT assay. Biological activities reported for these compounds are for the first time and it support anecdotal medicinal claims of C. viscosa Linn. leaves.

Comparative Analysis of In-Vitro Biological Activities of Methyl Eugenol Rich Cymbopogon khasianus Hack., Leaf Essential Oil with Pure Methyl Eugenol Compound

2020 ◽  
Vol 21 (10) ◽  
pp. 927-938 ◽  
Author(s):  
Roktim Gogoi ◽  
Rikraj Loying ◽  
Neelav Sarma ◽  
Twahira Begum ◽  
Sudin K. Pandey ◽  
...  
Keyword(s):  
Chemical Composition ◽  
Essential Oil ◽  
Biological Activities ◽  
Methyl Eugenol ◽  
Dpph Assay ◽  
Pure Compound ◽  
Allium Cepa Assay ◽  
Anti Inflammatory ◽  
Lemongrass Essential Oil

Background: The essential oil of methyl eugenol rich Cymbopogon khasianus Hack. was evaluated and its bioactivities were compared with pure methyl eugenol. So far, methyl eugenol rich essential oil of lemongrass was not studied for any biological activities; hence, the present study was conducted. Objective: This study examined the chemical composition of essential oil of methyl eugenol rich Cymbopogon khasianus Hack., and evaluated its antioxidant, anti-inflammatory, antimicrobial, and herbicidal properties and genotoxicity, which were compared with pure compound, methyl eugenol. Material and Methods: Methyl eugenol rich variety of Cymbopogon khasianus Hack., with registration no. INGR18037 (c.v. Jor Lab L-9) was collected from experimental farm CSIR-NEIST, Jorhat, Assam (26.7378°N, 94.1570°E). The essential oil wasobtained by hydro-distillation using a Clevenger apparatus. The chemical composition of the essential oil was evaluated using GC/MS analysis and its antioxidant (DPPH assay, reducing power assay), anti-inflammatory (Egg albumin denaturation assay), and antimicrobial (Disc diffusion assay, MIC) properties, seed germination effect and genotoxicity (Allium cepa assay) were studied and compared with pure Methyl Eugenol compound (ME). Results: Major components detected in the Essential Oil (EO) through Gas chromatography/mass spectroscopy analysis were methyl eugenol (73.17%) and β-myrcene (8.58%). A total of 35components were detected with a total identified area percentage of 98.34%. DPPH assay revealed considerable antioxidant activity of methyl eugenol rich lemongrass essential oil (IC50= 2.263 μg/mL), which is lower than standard ascorbic acid (IC50 2.58 μg/mL), and higher than standard Methyl Eugenol (ME) (IC50 2.253 μg/mL). Methyl eugenol rich lemongrass EO showed IC50 38.00 μg/mL, ME 36.44 μg/mL, and sodium diclofenac 22.76 μg/mL, in in-vitro anti-inflammatory test. Moderate antimicrobial activity towards the 8 tested microbes was shown by methyl eugenol rich lemongrass essential oil whose effectiveness against the microbes was less as compared to pure ME standard. Seed germination assay further revealed the herbicidal properties of methyl eugenol rich essential oil. Moreover, Allium cepa assay revealed moderate genotoxicity of the essential oil. Conclusion: This paper compared the antioxidant, anti-inflammatory, antimicrobial, genotoxicity and herbicidal activities of methyl eugenol rich lemongrass with pure methyl eugenol. This methyl eugenol rich lemongrass variety can be used as an alternative of methyl eugenol pure compound. Hence, the essential oil of this variety has the potential of developing cost-effective, easily available antioxidative/ antimicrobial drugs but its use should be under the safety range of methyl eugenol and needs further clinical trials.

Design, Synthesis, Characterization and in silico molecular docking studies and in vivo anti-inflammatory Activity of Pyrazoline clubbed Thiazolinone Derivatives

2020 ◽  
Vol 17 ◽  
Author(s):  
Deepak Kumar Singh ◽  
Mayank Kulshreshtha ◽  
Yogesh Kumar ◽  
Pooja A Chawla ◽  
Akash Ved ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Biological Activities ◽  
Inflammatory Activity ◽  
Standard Drug ◽  
Docking Score ◽  
Chemical Structures ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 1

Background: The pyrazolines give the reactions of aliphatic derivatives, resembling unsaturated compounds in their behavior towards permanganate and nascent hydrogen. This nucleus has been associated with various biological activities including inflammatory. Thiazolinone is a heterocyclic compound that contains both sulfur and nitrogen atom with a carbonyl group in their structure.Thiazolinone and their derivatives have attracted continuing interest because of their various biological activities, such as anti-inflammatory, antimicrobial, anti-proliferative, antiviral, anticonvulsant etc. The aim of the research was to club pyrazoline nucleus with thiazolinone in order to have significantanti-inflammatory activity. The synthesized compounds were chemically characterized for the establishment of their chemical structures and to evaluate as anti-inflammatory agent. Method: In the present work, eight derivatives of substituted pyrazoline (PT1-PT8) were synthesized by a three step reaction.The compounds were subjected to spectral analysis by Infrared, Mass and Nuclear magnetic resonance spectroscopy and elemental analysis data. All the synthesized were evaluated for their in vivo anti-inflammatory activity. The synthesized derivatives were evaluated for their affinity towards target COX-1 and COX-2, using indomethacin as the reference compound molecular docking visualization through AutoDock Vina. Results: Compounds PT-1, PT-3, PT-4 and PT-8 exhibited significant anti-inflammatory activity at 3rd hour being 50.7%, 54.3%, 52.3% and 57% respectively closer to that of the standard drug indomethacin (61.9%).From selected anti-inflammatory targets, the synthesized derivatives exhibited better interaction with COX-1 and COX-2 receptor, where indomethacin showed docking score of -6.5 kJ/mol, compound PT-1 exhibited highest docking score of -9.1 kJ/mol for COX-1 and compound PT-8 having docking score of 9.4 kJ/mol for COX-2. Conclusion: It was concluded that synthesized derivatives have more interaction with COX-2 receptors in comparison to the COX-1 receptors because the docking score with COX-2 receptors were very good. It is concluded that the synthesized derivatives (PT-1 to PT-8) are potent COX-2 inhibitors.

Synthesis, Antimicrobial Evaluation and Docking Study of Novel Thiosemicarbazone clubbed with 1,2,3-Triazoles

2020 ◽  
Vol 16 ◽  
Author(s):  
Adinath D. Badar ◽  
Shubham M. Sulakhe ◽  
Mahesh B. Muluk ◽  
Naziya N. M. A. Rehman ◽  
Prashant P. Dixit ◽  
...  
Keyword(s):  
Binding Affinity ◽  
Biological Activities ◽  
Dna Gyrase ◽  
Docking Study ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Molecular Docking Study ◽  
Triazole Derivatives ◽  
Antibacterial And Antifungal

Background: Thiosemicarbazone, 1,2,3-triazole and their derivatives received great pharmaceutical importance due to their prominent biological activities. In the present study, the molecular hybrid thiosemicarbazone-1,2,3-triazoles derivatives were synthesized and screened for their antimicrobial activities. Methods: A series of thiosemicarbazone clubbed with 1,2,3-triazole derivatives were synthesized via click chemistry approach in good yields. The structures of synthesized compounds were assigned by their spectral data. The in vitro antimicrobial activity was performed by the agar well diffusion method. A molecular docking study was performed to identify the possible mode of action of synthesized derivatives. Results: The compounds 5d, 5h, 5i and 5k have exhibited excellent antimicrobial activities against both antibacterial and antifungal pathogens. The active thiosemicarbazone-1,2,3-triazole derivatives have shown excellent binding affinity towards DNA gyrase. Conclusion: The molecular hybrid thiosemicarbazone-1,2,3-triazole derivatives were synthesized. The newly synthesized compounds were evaluated for their antimicrobial activities. Few of the thiosemicarbazone-1,2,3-triazoles derivatives have exhibited good antimicrobial activities. They have been shown excellent binding affinity towards DNA gyrase.

scholarly journals Sesquiterpene Lactones: Promising Natural Compounds to Fight Inflammation

Pharmaceutics ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 991
Author(s):  
Melanie S. Matos ◽  
José D. Anastácio ◽  
Cláudia Nunes dos Santos
Keyword(s):  
Biological Activities ◽  
Sesquiterpene Lactones ◽  
Physiological State ◽  
Plant Secondary Metabolites ◽  
Inflammatory Pathways ◽  
Inflammatory State ◽  
Anti Inflammatory ◽  
Inflammatory Molecules

Inflammation is a crucial and complex process that reestablishes the physiological state after a noxious stimulus. In pathological conditions the inflammatory state may persist, leading to chronic inflammation and causing tissue damage. Sesquiterpene lactones (SLs) are composed of a large and diverse group of highly bioactive plant secondary metabolites, characterized by a 15-carbon backbone structure. In recent years, the interest in SLs has risen due to their vast array of biological activities beneficial for human health. The anti-inflammatory potential of these compounds results from their ability to target and inhibit various key pro-inflammatory molecules enrolled in diverse inflammatory pathways, and prevent or reduce the inflammatory damage on tissues. Research on the anti-inflammatory mechanisms of SLs has thrived over the last years, and numerous compounds from diverse plants have been studied, using in silico, in vitro, and in vivo assays. Besides their anti-inflammatory potential, their cytotoxicity, structure–activity relationships, and pharmacokinetics have been investigated. This review aims to gather the most relevant results and insights concerning the anti-inflammatory potential of SL-rich extracts and pure SLs, focusing on their effects in different inflammatory pathways and on different molecular players.

scholarly journals Effects of prostaglandin lipid mediators on agonist-induced lung endothelial permeability and inflammation

2017 ◽  
Vol 313 (4) ◽  
pp. L710-L721 ◽  
Author(s):  
Yunbo Ke ◽  
Olga V. Oskolkova ◽  
Nicolene Sarich ◽  
Yufeng Tian ◽  
Albert Sitikov ◽  
...  
Keyword(s):  
Protective Effect ◽  
Vascular Endothelial Cells ◽  
Biological Activities ◽  
Cell Monolayer ◽  
Endothelial Permeability ◽  
In Vivo Model ◽  
Barrier Dysfunction ◽  
Anti Inflammatory

Prostaglandins (PG), the products of cyclooxygenase-mediated conversion of arachidonic acid, become upregulated in many situations including allergic response, inflammation, and injury, and exhibit a variety of biological activities. Previous studies described barrier-enhancing and anti-inflammatory effects of PGE2 and PGI2 on vascular endothelial cells (EC). Yet, the effects of other PG members on EC barrier and inflammatory activation have not been systematically analyzed. This study compared effects of PGE2, PGI2, PGF2α, PGA2, PGJ2, and PGD2 on human pulmonary EC. EC permeability was assessed by measurements of transendothelial electrical resistance and cell monolayer permeability for FITC-labeled tracer. Anti-inflammatory effects of PGs were evaluated by analysis of expression of adhesion molecule ICAM1 and secretion of soluble ICAM1 and cytokines by EC. PGE2, PGI2, and PGA2 exhibited the most potent barrier-enhancing effects and most efficient attenuation of thrombin-induced EC permeability and contractile response, whereas PGI2 effectively suppressed thrombin-induced permeability but was less efficient in the attenuation of prolonged EC hyperpermeability caused by interleukin-6 or bacterial wall lipopolysaccharide, LPS. PGD2 showed a modest protective effect on the EC inflammatory response, whereas PGF2α and PGJ2 were without effect on agonist-induced EC barrier dysfunction. In vivo, PGE2, PGI2, and PGA2 attenuated LPS-induced lung inflammation, whereas PGF2α and PGJ2 were without effect. Interestingly, PGD2 exhibited a protective effect in the in vivo model of LPS-induced lung injury. This study provides a comprehensive analysis of barrier-protective and anti-inflammatory effects of different prostaglandins on lung EC in vitro and in vivo and identifies PGE2, PGI2, and PGA2 as prostaglandins with the most potent protective properties.

scholarly journals SYNTHESIS AND ANTITUMOR ACTIVITY OF NEW MULTIFUNCTIONAL COUMARINS

2020 ◽  
Vol 17 (36) ◽  
pp. 871-883
Author(s):  
Moath Kahtan BASHIR ◽  
Yasser Fakri MUSTAFA ◽  
Mahmood Khudhayer OGLAH
Keyword(s):  
Schiff Base ◽  
Antitumor Activity ◽  
Human Cancer ◽  
Biological Activities ◽  
Cell Viability Assay ◽  
Chemical Structures ◽  
Viability Assay ◽  
Schiff Base Formation ◽  
Mcf 7

Cancer constitutes one of the most severe public health menaces worldwide. It is imperative to synthesize new compounds and explore their antitumor activity to find a potential resolution to this health problem. Synthesis of new scaffolds and evaluating their antitumor activity is a relevant approach for combating cancer development. Coumarins can exhibit diverse biological activities, and one of these is the antitumor activity. This study aimed to synthesize new coumarins by grafting their precursors to the aromatic amines via Schiff base formation and evaluating their introductory antitumor activity. New multifunctional coumarins (MC1-MC9) were prepared by integrating a functionalized coumarin with different toluidine derivatives via a Schiff-base linkage. Spectral characterization inspired by FTIR, 1H- and 13C- NMR spectroscopies has established the chemical structures of the synthesized products. The antitumor activity was explored in vitro versus four dominant human cancer lines, including HeLa, SKG, MCF-7, and AMN3. The outcomes acquired from the cell viability assay inspected by applying MTT dye have revealed that the synthesized multifunctional coumarins, particularly MC3, have a hopeful activity. It can be concluded that a similar trend of activity against the test cell lines was observed for the synthesized coumarins, with the best action being versus MCF-7 and the least one versus AMN3. This study not only affords a new scaffold of a significant antitumor activity but also provides some insights into its structureactivity relationship.

Hemoglobin F (HbF) inducers; History, Structure and Efficacies

2021 ◽  
Vol 21 ◽  
Author(s):  
Zahra Hashemi ◽  
Mohammad Ali Ebrahimzadeh
Keyword(s):  
Clinical Trials ◽  
Natural Products ◽  
Biological Activities ◽  
Globin Gene ◽  
Beta Thalassemia ◽  
Gene Promoters ◽  
Hemoglobin F ◽  
Chemical Structures

Abstract: Inherited beta-thalassemia is a major disease caused by irregular production of hemoglobin through reducing beta-globin chains. It has been observed that increasing fetal hemoglobin (HbF) production improves symptoms in the patients. Therefore, an increase in the level of HbF has been an operative approach for treating patients with beta-thalassemia. This review represents compounds with biological activities and pharmacological properties that can promote the HBF level and therefore used in the β-thalassemia patients' therapy. Various natural products with different mechanisms of action can be helpful in this medication cure. Clinical trials were efficient in improving the signs of patients. Association of in vivo, and in vitro studies of HbF induction and γ-globin mRNA growth displays that in vitro experiments could be an indicator of the in vivo response. The current study shows that; (a) HbF inducers can be grouped in several classes based on their chemical structures and mechanism of actions; b) According to several clinical trials, well-known drugs such as hydroxyurea and decitabine are useful HbF inducers; (c) The cellular biosensor K562 carrying genes under the control of the human γ-globin and β-globin gene promoters were applied during the researches; d) New natural products and lead compounds were found based on various studies as HbF inducers.

scholarly journals Antioxidant and Anti-Inflammatory Activities of Safflower (Carthamus tinctorius L.) Honey Extract

Foods ◽  
2020 ◽  
Vol 9 (8) ◽  
pp. 1039
Author(s):  
Li-Ping Sun ◽  
Feng-Feng Shi ◽  
Wen-Wen Zhang ◽  
Zhi-Hao Zhang ◽  
Kai Wang
Keyword(s):  
Chemical Composition ◽  
Biological Activities ◽  
Carthamus Tinctorius ◽  
Raw 264.7 Cells ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Unique Type ◽  
Antioxidant Genes ◽  
Anti Inflammatory

Safflower honey is a unique type of monofloral honey collected from the nectar of Carthamus tinctorius L. in the Apis mellifera colonies of northwestern China. Scant information is available regarding its chemical composition and biological activities. Here, for the first time, we investigated this honey’s chemical composition and evaluated its in vitro antioxidant and anti-inflammatory activities. Basic physicochemical parameters of the safflower honey samples in comparison to established quality standards suggested that safflower honeys presented a good level of quality. The in vitro antioxidant tests showed that extract from Carthamus tinctorius L. honey (ECH) effectively scavenged DPPH and ABTS+ free radicals. In lipopolysaccharides (LPS) activated murine macrophages inflammatory model, ECH treatment to the cells inhibited the release of nitric oxide and down-regulated the expressions of inflammatory-relating genes (iNOS, IL-1β, TNF-α and MCP-1). The expressions of the antioxidant genes TXNRD, HO-1, and NQO-1, were significantly boosted in a concentration-dependent manner. ECH decreased the phosphorylation of IκBα and inhibited the nuclear entry of the NF-κB-p65 protein, in LPS-stimulated Raw 264.7 cells, accompany with the increased expressions of Nrf-2 and HO-1, suggesting that ECH achieved the anti-inflammatory effects by inhibiting NF-κB signal transduction and boosting the antioxidant system via activating Nrf-2/HO-1 signaling. These results, taken together, indicated that safflower honey has great potential into developing as a high-quality agriproduct.

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