Natural products as sources of new fungicides (V): Design and synthesis of acetophenone derivatives against phytopathogenic fungi in vitro and in vivo

2018 ◽  
Vol 28 (17) ◽  
pp. 2861-2864 ◽  
Author(s):  
Wen-Jia Dan ◽  
Thi-Mai-Luong Tuong ◽  
Da-Cheng Wang ◽  
Ding Li ◽  
An-Ling Zhang ◽  
...  
Keyword(s):  
Natural Products ◽  
Phytopathogenic Fungi ◽  
Design And Synthesis ◽  
Acetophenone Derivatives

scholarly journals Natural compounds: A sustainable alternative for controlling phytopathogens

2018 ◽  
Author(s):  
María Fernanda Jiménez-Reyes ◽  
Héctor Carrasco ◽  
Andrés Olea ◽  
Evelyn Silva-Moreno
Keyword(s):  
Natural Products ◽  
Secondary Metabolites ◽  
Antifungal Agents ◽  
Phytopathogenic Fungi ◽  
Direct Application ◽  
Economic Losses ◽  
Infectious Agents ◽  
Active Compounds

Fungi are the primary infectious agents in plants causing significant economic losses in agroindustry. Traditionally, these pathogens have been treated with different synthetic fungicides such as hydroxianilides, anilinopyrimidines, and azoles, to name a few. However, the indiscriminate use of these chemicals has increased fungi resistance in plants. Natural products have been researched as a control, and an alternative to these synthetic fungicides since they are not harmful to health and contribute to the environment caring. This review describes plants extracts, essential oils, and active compounds or secondary metabolites as antifungal agents both, in vitro and in vivo. Active compounds have been recently described as the best candidates for the control of phytopathogenic fungi. When metabolized by plants, these compounds concentrations rely on the environmental conditions and pathogens incidence. However, one issue regarding the direct application of these preformed compounds in plants touch upon their low persistence in the environment, and their even lower bioavailability than synthetic fungicides. Hence the challenge is to develop useful formulations based on natural products to increase the compounds solubility facilitating thus their application in the field while maintaining their properties.

scholarly journals Natural compounds: A sustainable alternative for controlling phytopathogens

2018 ◽  
Author(s):  
María Fernanda Jiménez-Reyes ◽  
Héctor Carrasco ◽  
Andrés Olea ◽  
Evelyn Silva-Moreno
Keyword(s):  
Natural Products ◽  
Secondary Metabolites ◽  
Antifungal Agents ◽  
Phytopathogenic Fungi ◽  
Direct Application ◽  
Economic Losses ◽  
Infectious Agents ◽  
Active Compounds

Fungi are the primary infectious agents in plants causing significant economic losses in agroindustry. Traditionally, these pathogens have been treated with different synthetic fungicides such as hydroxianilides, anilinopyrimidines, and azoles, to name a few. However, the indiscriminate use of these chemicals has increased fungi resistance in plants. Natural products have been researched as a control, and an alternative to these synthetic fungicides since they are not harmful to health and contribute to the environment caring. This review describes plants extracts, essential oils, and active compounds or secondary metabolites as antifungal agents both, in vitro and in vivo. Active compounds have been recently described as the best candidates for the control of phytopathogenic fungi. When metabolized by plants, these compounds concentrations rely on the environmental conditions and pathogens incidence. However, one issue regarding the direct application of these preformed compounds in plants touch upon their low persistence in the environment, and their even lower bioavailability than synthetic fungicides. Hence the challenge is to develop useful formulations based on natural products to increase the compounds solubility facilitating thus their application in the field while maintaining their properties.

Natural Anti-inflammatory compounds as Drug candidates in Alzheimer’s disease

2020 ◽  
Vol 27 ◽  
Author(s):  
Reyaz Hassan Mir ◽  
Abdul Jalil Shah ◽  
Roohi Mohi-ud-din ◽  
Faheem Hyder Potoo ◽  
Mohd. Akbar Dar ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Natural Products ◽  
Protective Action ◽  
New Drugs ◽  
Huperzine A ◽  
Brain Disorder ◽  
Anti Inflammatory

: Alzheimer's disease (AD) is a chronic neurodegenerative brain disorder characterized by memory impairment, dementia, oxidative stress in elderly people. Currently, only a few drugs are available in the market with various adverse effects. So to develop new drugs with protective action against the disease, research is turning to the identification of plant products as a remedy. Natural compounds with anti-inflammatory activity could be good candidates for developing effective therapeutic strategies. Phytochemicals including Curcumin, Resveratrol, Quercetin, Huperzine-A, Rosmarinic acid, genistein, obovatol, and Oxyresvertarol were reported molecules for the treatment of AD. Several alkaloids such as galantamine, oridonin, glaucocalyxin B, tetrandrine, berberine, anatabine have been shown anti-inflammatory effects in AD models in vitro as well as in-vivo. In conclusion, natural products from plants represent interesting candidates for the treatment of AD. This review highlights the potential of specific compounds from natural products along with their synthetic derivatives to counteract AD in the CNS.

Potential for Treatment of Neurodegenerative Diseases with Natural Products or Synthetic Compounds that Stabilize Microtubules

2020 ◽  
Vol 26 (35) ◽  
pp. 4362-4372
Author(s):  
John H. Miller ◽  
Viswanath Das
Keyword(s):  
Natural Products ◽  
Neurodegenerative Diseases ◽  
In Vivo Models ◽  
Synthetic Compounds ◽  
Stabilizing Agents ◽  
Animal Models Of Disease ◽  
Model Studies ◽  
Models Of Disease

No effective therapeutics to treat neurodegenerative diseases exist, despite significant attempts to find drugs that can reduce or rescue the debilitating symptoms of tauopathies such as Alzheimer’s disease, Parkinson’s disease, frontotemporal dementia, amyotrophic lateral sclerosis, or Pick’s disease. A number of in vitro and in vivo models exist for studying neurodegenerative diseases, including cell models employing induced-pluripotent stem cells, cerebral organoids, and animal models of disease. Recent research has focused on microtubulestabilizing agents, either natural products or synthetic compounds that can prevent the axonal destruction caused by tau protein pathologies. Although promising results have come from animal model studies using brainpenetrant natural product microtubule-stabilizing agents, such as paclitaxel analogs that can access the brain, epothilones B and D, and other synthetic compounds such as davunetide or the triazolopyrimidines, early clinical trials in humans have been disappointing. This review aims to summarize the research that has been carried out in this area and discuss the potential for the future development of an effective microtubule stabilizing drug to treat neurodegenerative disease.

Novel Phytochemical Constituents and their Potential to Manage Diabetes

2020 ◽  
Vol 26 ◽  
Author(s):  
Shaik Ibrahim Khalivulla ◽  
Arifullah Mohammed ◽  
Kokkanti Mallikarjuna
Keyword(s):  
Natural Products ◽  
Large Population ◽  
World Health ◽  
In Vivo Studies ◽  
Antidiabetic Activity ◽  
Therapeutic Drug ◽  
Pharmacological Activities ◽  
Chemical Structures

Background: Diabetes is a chronic disease affecting a large population worldwide and stands as one of the major global health challenges to be tackled. According to World Health Organization, about 400 million are having diabetes worldwide and it is the seventh leading cause of deaths in 2016. Plant based natural products had been in use from ancient time as ethnomedicine for the treatment of several diseases including diabetes. As a result of that, there are several reports on plant based natural products displaying antidiabetic activity. In the current review, such antidiabetic potential compounds reported from all plant sources along with their chemical structures are collected, presented and discussed. This kind of reports are essential to pool the available information to one source followed by statistical analysis and screening to check the efficacy of all known compounds in a comparative sense. This kind of analysis can give rise to few numbers of potential compounds from hundreds, whom can further be screened through in vitro and in vivo studies, and human trails leading to the drug development. Methods: Phytochemicals along with their potential antidiabetic property were classified according to their basic chemical skeleton. The chemical structures of all the compounds with antidiabetic activities were elucidated in the present review. In addition to this, the distribution and their other remarkable pharmacological activities of each species is also included. Results: The scrutiny of literature led to identification of 44 plants with antidiabetic compounds (70) and other pharmacological activities. For the sake of information, the distribution of each species in the world is given. Many plant derivatives may exert antidiabetic properties by improving or mimicking the insulin production or action. Different classes of compounds including sulfur compounds (1-4), alkaloids (5-11), phenolic compounds (12-17), tannins (18-23), phenylpropanoids (24-27), xanthanoids (28-31), amino acid (32), stilbenoid (33), benzofuran (34), coumarin (35), flavonoids (36-49) and terpenoids (50-70) were found to be active potential compounds for antidiabetic activity. Of the 70 listed compounds, majorly 17 compounds are from triterpenoids, 13 flavonoids and 7 are from alkaloids. Among all the 44 plant species, maximum number (7) of compounds are reported from Lagerstroemia speciosa followed by Momordica charantia (6) and S. oblonga with 5 compounds. Conclusion: This is the first paper to summarize the established chemical structures of phytochemicals that have been successfully screened for antidiabetic potential and their mechanisms of inhibition. The reported compounds could be considered as potential lead molecules for the treatment of type-2 diabetes. Further, molecular and clinical trials are required to select and establish the therapeutic drug candidates.

Modulation of Matrix Metalloproteinases by Plant-Derived Products

2020 ◽  
Vol 20 ◽  
Author(s):  
Nur Najmi Mohamad Anuar ◽  
Nurul Iman Natasya Zulkafali ◽  
Azizah Ugusman
Keyword(s):  
Clinical Trials ◽  
Natural Products ◽  
Matrix Metalloproteinases ◽  
Animal Studies ◽  
Current Knowledge ◽  
In Vitro Models ◽  
In Vivo Studies ◽  
Extracellular Matrix Components

: Matrix metalloproteinases (MMPs) are a group of zinc-dependent metallo-endopeptidase that are responsible towards the degradation, repair and remodelling of extracellular matrix components. MMPs play an important role in maintaining a normal physiological function and preventing diseases such as cancer and cardiovascular diseases. Natural products derived from plants have been used as traditional medicine for centuries. Its active compounds, such as catechin, resveratrol and quercetin, are suggested to play an important role as MMPs inhibitors, thereby opening new insights into their applications in many fields, such as pharmaceutical, cosmetic and food industries. This review summarises the current knowledge on plant-derived natural products with MMP-modulating activities. Most of the reviewed plant-derived products exhibit an inhibitory activity on MMPs. Amongst MMPs, MMP-2 and MMP-9 are the most studied. The expression of MMPs is inhibited through respective signalling pathways, such as MAPK, NF-κB and PI3 kinase pathways, which contribute to the reduction in cancer cell behaviours, such as proliferation and migration. Most studies have employed in vitro models, but a limited number of animal studies and clinical trials have been conducted. Even though plant-derived products show promising results in modulating MMPs, more in vivo studies and clinical trials are needed to support their therapeutic applications in the future.

scholarly journals A small molecule HIF-1α stabilizer that accelerates diabetic wound healing

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Guodong Li ◽  
Chung-Nga Ko ◽  
Dan Li ◽  
Chao Yang ◽  
Wanhe Wang ◽  
...  
Keyword(s):  
Wound Healing ◽  
Small Molecule ◽  
Hypoxia Inducible Factor ◽  
Diabetic Patients ◽  
Diabetic Mice ◽  
Impaired Wound Healing ◽  
Von Hippel Lindau ◽  
Design And Synthesis

AbstractImpaired wound healing and ulcer complications are a leading cause of death in diabetic patients. In this study, we report the design and synthesis of a cyclometalated iridium(III) metal complex 1a as a stabilizer of hypoxia-inducible factor-1α (HIF-1α). In vitro biophysical and cellular analyses demonstrate that this compound binds to Von Hippel-Lindau (VHL) and inhibits the VHL–HIF-1α interaction. Furthermore, the compound accumulates HIF-1α levels in cellulo and activates HIF-1α mediated gene expression, including VEGF, GLUT1, and EPO. In in vivo mouse models, the compound significantly accelerates wound closure in both normal and diabetic mice, with a greater effect being observed in the diabetic group. We also demonstrate that HIF-1α driven genes related to wound healing (i.e. HSP-90, VEGFR-1, SDF-1, SCF, and Tie-2) are increased in the wound tissue of 1a-treated diabetic mice (including, db/db, HFD/STZ and STZ models). Our study demonstrates a small molecule stabilizer of HIF-1α as a promising therapeutic agent for wound healing, and, more importantly, validates the feasibility of treating diabetic wounds by blocking the VHL and HIF-1α interaction.

scholarly journals In vitro and in vivo Assay for Assessment of the Biological Control Potential of Streptomyces sp. KT

2017 ◽  
Vol 7 (1) ◽  
pp. 10
Author(s):  
Tatsuya Ohike ◽  
Minori Maeda ◽  
Tetsuya Matsukawa ◽  
Masahiro Okanami ◽  
Shin’ichiro Kajiyama ◽  
...  
Keyword(s):  
Biological Control ◽  
Suppressive Effect ◽  
Phytopathogenic Fungi ◽  
Dual Culture ◽  
Biological Control Agents ◽  
Bipolaris Oryzae ◽  
Biological Control Potential ◽  
Dual Culture Assay

Rhizoctonia solani is fungal plant pathogen that infects many different host plants. Recently, biological control agents that are friendly to the environment and ecosystems have attracted much attention as an alternative to the use of chemical fungicide which have been used worldwide to control soil borne pathogens including R. solani. In this study, 53 strains of actinomycetes isolated from environmental soils, and antifungal activities of them were assessed by the dual culture assay. Strain KT showed strong inhibitory activities against 8 phytopathogenic fungi. A great suppressive effect on R. solani growth was observed in the inoculation test of plants using cucumber and chin-geng-sai. In addition, infection of Bipolaris oryzae also could be suppressed in the detached leaf assay using oats. As a result of genetic analysis, it was shown that KT was a species closely related to Streptomyces lavenduligriseus NRRL B-3173T. However, as far as we know, there is no report for biological control agents using S. lavenduligriseus. This study suggests that the strain KT may useful as biological control agents to suppress various crop diseases.

scholarly journals Structure Based Design and Synthesis of Peptide Inhibitor of Human LOX-12: In Vitro and In Vivo Analysis of a Novel Therapeutic Agent for Breast Cancer

PLoS ONE ◽  
2012 ◽  
Vol 7 (2) ◽  
pp. e32521 ◽  
Author(s):  
Abhay kumar Singh ◽  
Ratnakar Singh ◽  
Farhat Naz ◽  
Shyam Singh Chauhan ◽  
Amit Dinda ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Therapeutic Agent ◽  
Peptide Inhibitor ◽  
Design And Synthesis ◽  
In Vivo Analysis ◽  
Novel Therapeutic

scholarly journals Natural products with therapeutic potential in melanoma metastasis

2015 ◽  
Vol 32 (8) ◽  
pp. 1170-1182 ◽  
Author(s):  
A. AlQathama ◽  
J. M. Prieto
Keyword(s):  
Natural Products ◽  
Cancer Treatment ◽  
Therapeutic Potential ◽  
Melanoma Cells ◽  
Mechanisms Of Action ◽  
Melanoma Metastasis ◽  
Pharmacological Effects ◽  
Cytotoxic Compounds

Natural products continue to provide lead cytotoxic compounds for cancer treatment but less attention has been given to antimigratory compounds. We here systematically and critically survey more than 30 natural products with direct in vitro and in vivo pharmacological effects on migration and/or metastasis of melanoma cells and chart the mechanisms of action for this underexploited property.

Sign in / Sign up

Export Citation Format

Share Document