scholarly journals Bioactive Compounds of Softwood Bark as Potential Agents against Human Diseases Include the SARS-CoV-2 Virus

2021 ◽  
Vol 12 (5) ◽  
pp. 5860-5869
Keyword(s):  
Biological Activities ◽  
Therapeutic Agents ◽  
Pharmaceutical Products ◽  
Cytotoxic Activities ◽  
Naturally Occurring ◽  
New Development ◽  
Main Class ◽  
Natural Drugs ◽  
Human Viruses

In recent years, significant progress has been achieved in developing natural drugs derived from medicinal plants. Multiple in-vitro screening studies reported that some naturally occurring compounds could possess inhibitory activity against various human viruses. The presented work describes significant biological activities of the main class of secondary metabolites such as phenolic compounds and terpenes located in industrially important tree species Norway spruce (Picea Abies) and Scots pine (Pinus Sylvestris). Phytochemicals show promising in vitro antiviral and cytotoxic activities, making them an attractive starting material for new development in various pharmaceutical products. They have the potential to effectively protect human health against cardiovascular diseases, diabetes mellitus, and as therapeutic agents against the SARS-CoV-2 virus.

scholarly journals Antimicrobial Peptides and Cancer: Potential Use of Antimicrobial-Like Peptides in Chemotherapy

2019 ◽  
pp. 233-242
Author(s):  
Mizejewski GJ
Keyword(s):  
Antimicrobial Peptides ◽  
Human Cancer ◽  
Biological Activities ◽  
Therapeutic Agents ◽  
Human Protein ◽  
Potential Candidate ◽  
Host Defense Peptides ◽  
Naturally Occurring

Antimicrobial peptides (AMPs) constitute host defense peptides found among insects, fish, amphibians, and mammals including man. The targets of AMPs are gram-negative and gram-positive bacteria, fungi, enveloped viruses, and transformed/cancerous cells. The AMPs are broad spectrum antibiotics which display the propensity to serve as therapeutic agents not only in infectious disease, but also in human cancer. AMPs demonstrate unique properties which include cell membrane penetration, destabilization of biological membranes, ability to form and/or interact with membrane channels, and the capability to modulate host immune responses. The three types of AMPs consists a) naturally-occurring; b) artificially synthesized; and c) cleaved peptide fragments from blood and extracellular matrix proteins. The present treatise presents one such example of an AMP-like peptide derived from a naturally-occurring human protein as a potential candidate for future cancer therapy. The biological activities of human AMP-like peptides as cancer therapeutic agents are reviewed and reported in multiple in vitro and in vivo cancer assays. The possibility of using such human protein-derived peptides as primary and adjunct cancer therapeutic agents is addressed.

Flavones as a Privileged Scaffold in Drug Discovery: Current Developments

2019 ◽  
Vol 16 (7) ◽  
pp. 968-1001
Author(s):  
Pone K. Boniface ◽  
Ferreira I. Elizabeth
Keyword(s):  
Biological Activities ◽  
Therapeutic Agents ◽  
Pharmacological Properties ◽  
Chemical Transformations ◽  
National Library ◽  
Scientific Publications ◽  
Multifactorial Diseases ◽  
Naturally Occurring ◽  
Privileged Scaffold

Background: Flavones are one of the main subclasses of flavonoids with diverse pharmacological properties. They have been reported to possess antimalarial, antimicrobial, anti-tuberculosis, anti-allergic, antioxidant, anti-inflammatory activities, among others. Objective: The present review summarizes the recent information on the pharmacological properties of naturally occurring and synthetic flavones. Method: Scientific publications referring to natural and synthetic flavones in relation to their biological activities were hand-searched in databases such as SciFinder, PubMed (National Library of Medicine), Science Direct, Wiley, ACS, SciELO, Springer, among others. Results: As per the literature, seventy-five natural flavones were predicted as active compounds with reference to their IC50 (<20 µg/mL) in in vitro studies. Also, synthetic flavones were found active against several diseases. Conclusion: As per the literature, flavones are important sources for the potential treatment of multifactorial diseases. However, efforts toward the development of flavone-based therapeutic agents are still needed. The appearance of new catalysts and chemical transformations is expected to provide avenues for the synthesis of unexplored flavones, leading to the discovery of flavones with new properties and biological activities.

scholarly journals Hemisynthesis and Biological Evaluation of Cinnamylated, Benzylated, and Prenylated Dihydrochalcones from a Common Bio-Sourced Precursor

Antibiotics ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 620
Author(s):  
Anne Ardaillou ◽  
Jérôme Alsarraf ◽  
Jean Legault ◽  
François Simard ◽  
André Pichette
Keyword(s):  
Biological Activities ◽  
Biological Evaluation ◽  
Pharmacological Properties ◽  
Cytotoxic Potential ◽  
Naturally Occurring

Several families of naturally occurring C-alkylated dihydrochalcones display a broad range of biological activities, including antimicrobial and cytotoxic properties, depending on their alkylation sidechain. The catalytic Friedel–Crafts alkylation of the readily available aglycon moiety of neohesperidin dihydrochalcone was performed using cinnamyl, benzyl, and isoprenyl alcohols. This procedure provided a straightforward access to a series of derivatives that were structurally related to natural balsacones, uvaretin, and erioschalcones, respectively. The antibacterial and cytotoxic potential of these novel analogs was evaluated in vitro and highlighted some relations between the structure and the pharmacological properties of alkylated dihydrochalcones.

In Vitro Screening for Cytotoxic, Anti-bacterial, Anti-HIV1-RT Activities and Chemical Constituents of Croton fluviatilis, Croton acutifolius, and Croton thorelii

2021 ◽  
Vol 11 ◽  
Author(s):  
Charina Worarat ◽  
Wilart Pompimon ◽  
Phansuang Udomputtimekakul ◽  
Sukee Sukdee ◽  
Punchavee Sombutsiri ◽  
...  
Keyword(s):  
Ethyl Acetate ◽  
Ethyl Acetate Extract ◽  
Biological Activities ◽  
Chemical Constituents ◽  
Bacterial Activity ◽  
Cytotoxic Activities ◽  
Separation And Purification ◽  
Crude Extracts ◽  
Cytotoxicity Activities

Background: Although the chemical constituents and biological activities of a large number of plants in the Croton genus have been studied, there are still recently discovered plants to be investigated. Objective: 1. To investigate the anti-bacterial, anti-HIV1-RT, and cytotoxicity activities of crude extracts from these plants. 2. To investigate the chemical constituents of Croton fluviatilis, Croton acutifolius, and Croton thorelii. Method: The anti-bacterial, anti-HIV1-RT, and cytotoxicity of the three plants were evaluated by standard techniques. Extraction, separation, and purification of extracts from the three plants were undertaken. Results: The ethyl acetate extract of C. fluviatilis showed low anti-bacterial activity against E. aerogenes, E. coli 0157: H7, and P. mirabilis, together with the ethyl acetate extract of C. acutifolius displayed low anti-bacterial activity against E. aerogenes, while all the crude extracts of C. thorelii were inactive. The ethyl acetate extracts of C. thorelii, and C. fluviatilis showed strong inhibited HIV1-RT, whereas the ethyl acetate extract of C. acutifolius, and the hexane extract of C. fluviatilis displayed moderate inhibited HIV1-RT. Cytotoxic properties of three Croton plants were specific to KKU-M213, MDA-MB-231, A-549, and MMNK-1. Especially, the ethyl acetate extract of C. acutifolius exhibited strong cytotoxic activities against MDA-MB-231, A-549, and MMNK-1. Furthermore, the ethyl acetate extract of C. thorelii showed high cytotoxic activities against KKU-M213, and MDA-MB-231. Compounds 1, and 4 were found in C. fluviatilis. Compounds 2 and 4 were also found in C. acutifolius. Moreover, compound 3 was only found in C. thorelii. Conclusion: The present study revealed that the three Croton species are good sources of flavonoid compounds and further investigation of the chemical constituents from these plants may prove to be fruitful to discover more active compounds to be tested as potential medicines.

scholarly journals Leishmanicidal and Cytotoxic Activities of Extracts and Naturally-Occurring Compounds from two Lauraceae Species

2011 ◽  
Vol 6 (2) ◽  
pp. 1934578X1100600
Author(s):  
Jeysson Sánchez-Suárez ◽  
Ericsson Coy-Barrera ◽  
Luis Enrique Cuca ◽  
Gabriela Delgado
Keyword(s):  
Leishmania Species ◽  
In Vitro Cytotoxicity ◽  
Cytotoxic Activities ◽  
Naturally Occurring ◽  
Ethanolic Extracts ◽  
Leishmania Panamensis ◽  
J774 Cells ◽  
Different Levels ◽  
Leishmania Parasites

The in vitro leishmanicidal effects of ethanolic extracts and fifteen naturally-occurring compounds (five lignans, eight neolignans, a diterpene and a dihydrochalcone), obtained from Pleurothyrium cinereum and Ocotea macrophylla, were evaluated on promastigotes of Leishmania panamensis and L. braziliensis. In addition, in order to determine the selective action on Leishmania species as a safety principle, in vitro cytotoxicity on J774 cells was also evaluated for test compounds and extracts. One extract and seven compounds showed activity against Leishmania parasites at different levels. Dihydroflavokawin B (8) was found to be the most potent antileishmanial compound on both parasites, whilst (+)-otobaphenol (14), was found to be the most selective compound on L. panamensis.

scholarly journals The Effect of Hydroxybenzoate Lithium Complexes in Inducing Apoptosis in HT-1080 Human Fibrosarcoma Cells

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Jassem G. Mahdi ◽  
Eamon J. Mahdi ◽  
Amal Al-Hazzaa ◽  
Chris J. Pepper
Keyword(s):  
Biological Activities ◽  
Cytotoxic Activities ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Beneficial Effects ◽  
Fibrosarcoma Cells ◽  
Lithium Complexes ◽  
Human Fibrosarcoma Cells ◽  
Apoptotic Effects

There has been a growing interest in the beneficial effects of simple phenolic acids and their ability to exhibit various biological activities. The aim of this study was to assess in vitro biological activities of 2-, 3-, and 4-hydroxybenzoate lithium (HBLi) complexes on HT-1080 human fibrosarcoma cells by methods of using a metabolic activity assay, immunochemical and morphological techniques. Results showed that HBLi complexes exert their cytotoxic activities in a concentration- and chemical structure-dependent manner in the following order: 4-HBLi > 3-HBLi > 2-HBLi. Flow cytometry displayed evidence of apoptosis induced by 3-HBLi (21.8%) and 4-HBLi (33.2%). These results were verified by SEM, which revealed the formation of apoptotic bodies. In addition, these 3-HBLi and 4-HBLi caused an increase in HT-1080 cell cycle arrest in G0/G1 phase when compared to the controls (25% and 30.6%, resp.) when cells were treated with 6 mM for 24 hours. Immunochemical studies related to the molecular mechanism of apoptosis indicated that HBLi complexes downregulated the expression of Bcl-2 and upregulated Bax, p53, and caspases-3 in a concentration-dependent manner. HBLi complexes lowered Bcl-2/Bax ratios and induced the expression of p53 and caspase-3. These results suggest that HBLi complexes may exert their apoptotic effects through mitochondrial-mediated, caspase-dependent, apoptotic mechanisms.

scholarly journals Actinidia macrospermaC. F. Liang (a Wild Kiwi): Preliminary Study of Its Antioxidant and Cytotoxic Activities

2012 ◽  
Vol 2012 ◽  
pp. 1-7
Author(s):  
Yin Lu ◽  
Xiangtao Du ◽  
Lidan Lai ◽  
Hao Jin
Keyword(s):  
Antioxidant Activity ◽  
Cytotoxic Activity ◽  
Biological Activities ◽  
Positive Control ◽  
Total Phenolic ◽  
Cytotoxic Activities ◽  
Dependent Manner ◽  
Etoac Extract ◽  
Total Antioxidant

The antioxidant potential ofActinidia macrospermaC. F. Liang (Actinidiaceae) was investigated in vitro for total phenolic content, along with total antioxidant activity (TAA), 1,1-diphenyl 2-picryl hydrazyl (DPPH), and lipid peroxidation (LP). The results indicated that different polarity extracts ofA. macrospermaexhibit different biological activities, which depends mainly on the presence of phenolic compounds. The antioxidant activity was in the following decreasing order: MeOH extract > EtOAc extract > aqueous extract > CHCl3extract > Hexane extract. Moreover, the cytotoxic activity of this plant by MTT dye assay using SMMC-7721 has been determined also. The hexane, EtOAc, and CHCl3extracts showed cytotoxicity in a dose-dependent manner. Methanol and aqueous extracts, however, showed weak activities in this test. And a very significant cytotoxic activity, not significantly different from the positive control of quercetin, was observed in CHCl3extract.

scholarly journals Marine Terpenic Endoperoxides

Marine Drugs ◽  
2021 ◽  
Vol 19 (12) ◽  
pp. 661
Author(s):  
Irene Torres-García ◽  
Josefa L. López-Martínez ◽  
Manuel Muñoz-Dorado ◽  
Ignacio Rodríguez-García ◽  
Miriam Álvarez-Corral
Keyword(s):  
Total Synthesis ◽  
Marine Invertebrates ◽  
Biological Activities ◽  
Structural Features ◽  
Naturally Occurring ◽  
Organic Extracts ◽  
Pharmaceutical Uses ◽  
Potential Use ◽  
Dioxane Ring

Organic extracts of marine invertebrates, mainly sponges, from seas all over the world are well known for their high in vitro anticancer and antibiotic activities which make them promising sources of compounds with potential use as pharmaceutical leads. Most of the structures discovered so far have a peculiar structural feature in common: a 1,2-dioxane ring. This is a highly reactive heterocycle that can be considered as an endoperoxide function. Together with other structural features, this group could be responsible for the strong biological activities of the substances present in the extracts. Numerous research programs have focused on their structural elucidation and total synthesis since the seventies. As a consequence, the number of established chiral centres and the similarity between different naturally occurring substances is increasingly higher. Most of these compounds have a terpenoid nature, mainly diterpene and sesterterpene, with several peculiar structural features, such as the loss of one carbon atom. Although there are many reviews dealing with the occurrence of marine peroxides, their activities, or potential pharmaceutical uses, no one has focused on those having a terpene origin and the endoperoxide function. We present here a comprehensive review of these compounds paying special attention to their structural features and their biological activity.

scholarly journals ANTIMICROBIAL, CYTOTOXIC AND HEMOLYTIC ACTIVITIES OF MARINE ALGAE-ASSOCIATED FUNGAL ISOLATES IN VIETNAM

2019 ◽  
Vol 18 (4) ◽  
pp. 406-412
Author(s):  
Hoang Kim Chi ◽  
Tran Thi Hong Ha ◽  
Le Huu Cuong ◽  
Tran Thi Nhu Hang ◽  
Nguyen Dinh Tuan ◽  
...  
Keyword(s):  
Natural Products ◽  
Human Cancer ◽  
Biological Activities ◽  
Breast Adenocarcinoma ◽  
Cytotoxic Activities ◽  
Marine Microorganisms ◽  
Fungal Strains ◽  
Fungal Isolates ◽  
Fungal Extracts

In the context of sources for natural products discovery are going scarcer, exploiting biotechnologically potential compounds from marine microbial symbionts is considered a relatively new trend. In our study a total of fifteen fungal strains were isolated from marine algal samples belonging to species Kappaphycus cottonii, K. striatus, Gracilaria eucheumatoides and Betaphycus gelatinus collected in Nha Trang in 2017. The in vitro biological activities, including antimicrobial, cytotoxic and hemolytic activities of ethyl acetate extracts of the fungal strains were determined. From fifteen fungal extracts, six displayed antimicrobial activity against at least one test strain. At 20 μg.ml-1, four fungal extracts were found to express cytotoxic activity on two human cancer cell lines hepatocellular carcinoma (Hep-G2) and breast adenocarcinoma (MCF-7), with G. eucheumatoides being the source of the highest number of producer strains. Hemolytic activity was observed in rabbit erythrocytes under almost all fungal extracts’ effect. No apparent relationship was observed between the biological activities of fungal isolates. The biological assessments uncovered several fungal candidates, such as Bge-1.1, Kco-2.1 and Geu-1.1 with relatively potent antimicrobial and cytotoxic activities while expressing less hemolytic effect at concentrations from 20 μg.ml-1 to 200 μg.ml-1. The results evidenced the potential of exploiting natural products from associated marine microorganisms, especially those for the purpose of pharmaceutical applications.

scholarly journals QSAR Analysis of Rocaglamide Derivatives Cytotoxic Activities Using LFER Hansch Model

2010 ◽  
Vol 1 (2) ◽  
pp. 129
Author(s):  
Firdayani Firdayani ◽  
Susi Kusumaningrum ◽  
Doddy Irawan Setyo Utomo ◽  
Agung Eru Wibowo ◽  
Chaidir Chaidir
Keyword(s):  
Cancer Cells ◽  
Quantitative Structure Activity Relationship ◽  
Therapeutic Agents ◽  
Log P ◽  
Cytotoxic Activities ◽  
Qsar Analysis ◽  
Qsar Studies ◽  
Linear Free Energy ◽  
Naturally Occurring ◽  
Structure Activity

Rocaglamide derivatives are the compounds which have featuring cyclopenta[b]tetra-hydrobenzofuran skeleton. Until now it includes more than 50 naturally occurring derivatives. They were chosen to be interesting candidates for possible therapeutic agents primarily in the field of cancer chemotherapy due to their cytotoxic activities data against various cancer cells. A quantitative structure activity relationship (QSAR) studies were done to investigate physicochemical properties of molecule which contribute to their activities. Series of rocaglamide derivatives have been used and analyzed using linear free energy regression Hansch model for their cytotoxic activities against MONO-MAC-6 leukemia cells, RAJI lymphoma cells and MEL-JUSO melanoma cells. Results showed that the best QSAR equations were revealed involving C Log P and CMR parameters with nonlinear regression relationships in cytotoxic activities of rocaglamide derivatives against cancer cells above. Keywords: QSAR, Rocaglamide, LFER Hansch

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