Exploring Turkish biodiversity: A rich source of chemical diversity for drug leads discovery

2011 ◽  
Vol 83 (9) ◽  
pp. 1699-1707 ◽  
Author(s):  
Bilge Şener ◽  
İlkay Orhan
Keyword(s):  
Inhibitory Activity ◽  
Biological Activities ◽  
Chemical Diversity ◽  
Biological Investigation ◽  
Synthetic Drugs ◽  
Drug Molecules ◽  
Cholinesterase Inhibitory Activity ◽  
Plant Families ◽  
Drug Leads

Bioresources offer tremendous potential by having excellent chemical diversity for drug discovery programs and by serving as templates for synthetic drugs. There are well-known examples of clinically important drugs derived from natural sources. The development of pharmaceutical, nutraceutical, agricultural, and industrial products from bioresources can be used to promote incentives for conservation by providing an economic return to innovative use. Of those sources, medicinal plants have a virtually untapped reserve of original drug molecules, which await determination and chemical and biological investigation. Marine organisms have also gained increasing attention from researchers worldwide due to their chemically diverse secondary metabolites with desirable biological activities. There is still a great need for novel compounds with unique mechanisms of action to treat diseases such as cancer, Alzheimer’s, arthritis, and diabetes. Besides, multiresistance development by the parasites to the present drugs also constitutes another problem for the treatment of parasitic diseases as well as tuberculosis. In this article, 209 plant species belonging to 11 plant families were investigated for cholinesterase inhibitory activity by in vitro Ellman method at 10 μg/ml and 1 mg/ml doses. Among them, Salvia, Rosmarinus, and Fumaria species were found to have the most significant cholinesterase inhibitory activity.

scholarly journals Chemical Profiling and Cholinesterase Inhibitory Activity of Five Phaedranassa Herb. (Amaryllidaceae) Species from Ecuador

Molecules ◽  
2020 ◽  
Vol 25 (9) ◽  
pp. 2092 ◽  
Author(s):  
Raúl Moreno ◽  
Luciana R. Tallini ◽  
Cristina Salazar ◽  
Edison H. Osorio ◽  
Evelin Montero ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Potential Role ◽  
Biological Activities ◽  
New Drugs ◽  
Inhibitory Effects ◽  
Chemical Profiling ◽  
Cholinesterase Inhibitory Activity ◽  
Insight Into

It is estimated that 50 million people in the world live with dementia, 60–70% of whom suffer from Alzheimer’s disease (AD). Different factors are involved in the development of AD, including a reduction in the cholinergic neurotransmission level. The Amaryllidaceae plant family contains an exclusive, large, and still understudied alkaloid group characterized by a singular skeleton arrangement and a broad spectrum of biological activities. The chemistry and biodiversity of Ecuadorian representatives of the Phaedranassa genus (Amaryllidaceae) have not been widely studied. In this work, five Ecuadorian Phaedranassa species were examined in vitro for their activity towards the enzymes acetyl- (AChE) and butyrylcholinesterase (BuChE), and the alkaloid profile of bulb extracts was analyzed by GC-MS. The species Phaedranassa cuencana and Phaedranassa dubia showed the most AChE and BuChE inhibitory activity, respectively. To obtain insight into the potential role of the identified alkaloids in these inhibitory effects, docking experiments were carried out, and cantabricine showed in silico inhibitory activity against both cholinesterase structures. Our results show that Amaryllidaceae species from Ecuador are a potential source of new drugs for the palliative treatment of AD.

scholarly journals Chemical Diversity and Bioactivities of Monoterpene Indole Alkaloids (MIAs) from Six Apocynaceae Genera

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 488
Author(s):  
Afrah E. Mohammed ◽  
Zainab H. Abdul-Hameed ◽  
Modhi O. Alotaibi ◽  
Nahed O. Bawakid ◽  
Tariq R. Sobahi ◽  
...  
Keyword(s):  
Biological Activities ◽  
Indole Alkaloids ◽  
Natural Compounds ◽  
Molecular Target ◽  
Chemical Diversity ◽  
Drug Lead ◽  
The Family ◽  
Monoterpene Indole Alkaloids ◽  
Drug Leads ◽  
Anti Hiv

By the end of the twentieth century, the interest in natural compounds as probable sources of drugs has declined and was replaced by other strategies such as molecular target-based drug discovery. However, in the recent times, natural compounds regained their position as extremely important source drug leads. Indole-containing compounds are under clinical use which includes vinblastine and vincristine (anticancer), atevirdine (anti-HIV), yohimbine (erectile dysfunction), reserpine (antihypertension), ajmalicine (vascular disorders), ajmaline (anti-arrhythmic), vincamine (vasodilator), etc. Monoterpene Indole Alkaloids (MIAs) deserve the curiosity and attention of researchers due to their chemical diversity and biological activities. These compounds were considered as an impending source of drug-lead. In this review 444 compounds, were identified from six genera belonging to the family Apocynaceae, will be discussed. These genera (Alstonia, Rauvolfia, Kopsia, Ervatamia, and Tabernaemontana, and Rhazya) consist of 400 members and represent 20% of Apocynaceae species. Only 30 (7.5%) species were investigated, whereas the rest are promising to be investigated. Eleven bioactivities, including antibacterial, antifungal, anti-inflammatory and immunosuppressant activities, were reported. Whereas cytotoxic effect represents 47% of the reported activities. Convincingly, the genera selected in this review are a wealthy source for future anticancer drug lead.

Salvia leriifolia Benth (Lamiaceae) extract demonstrates in vitro antioxidant properties and cholinesterase inhibitory activity

2010 ◽  
Vol 30 (12) ◽  
pp. 823-830 ◽  
Author(s):  
Monica R. Loizzo ◽  
Rosa Tundis ◽  
Filomena Conforti ◽  
Federica Menichini ◽  
Marco Bonesi ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Antioxidant Properties ◽  
Cholinesterase Inhibitory Activity

scholarly journals Engineering of Marine-derived Antimicrobial Peptides (mAMPs) into Improved Anti-infective Drug Leads: A Mini-review

2021 ◽  
Vol 1192 (1) ◽  
pp. 012013
Author(s):  
L Sukmarini
Keyword(s):  
Antimicrobial Peptides ◽  
Chemical Diversity ◽  
Cytotoxic Activities ◽  
Small Molecular Weight ◽  
Resistance Development ◽  
Drug Candidates ◽  
Bacteria And Fungi ◽  
Drug Leads ◽  
Net Positive Charge

Abstract Marine-derived antimicrobial compounds possess chemical diversity varying from peptides, fatty acids to terpenes, alkaloids, and polyketides. These compounds, especially of peptide origin called antimicrobial peptides (AMPs), are present in the majority of marine organisms, including microbes (bacteria and fungi), invertebrates (molluscs, echinoderms, and sponges), vertebrates (fish and mammals), and plants (marine algae). They are defined by small molecular weight (less than 10 kDa), a net positive charge, and amphipathic structures. Moreover, due to their profound in vitro antimicrobial and cytotoxic activities and a low risk for resistance development, naturally occurring marine-derived AMPs (mAMPs) have been used as drug design templates for a large variety of semi-synthetic or synthetic AMPs, some of which have reached clinical trials. This mini-review aims to discuss AMPs from marine sources, mainly emphasizing the engineering of these peptides with improved pharmacological properties to develop drug candidates. Some selected recent examples of these engineered mAMPs as anti-infective drug leads are herein highlighted.

scholarly journals New Chemovariety of Lippia alba From Colombia: Compositional Analysis of the Volatile Secondary Metabolites and Some in vitro Biological Activities of the Essential Oil From Plant Leaves

2019 ◽  
Vol 14 (7) ◽  
pp. 1934578X1986290
Author(s):  
Amner Muñoz-Acevedo ◽  
María C. González ◽  
Juan D. Rodríguez ◽  
Yurina Sh. De Moya
Keyword(s):  
Secondary Metabolites ◽  
Essential Oil ◽  
Solid Phase ◽  
Biological Activities ◽  
Biological Properties ◽  
Northern Region ◽  
Chemical Diversity ◽  
Gas Chromatography Mass Spectrometry ◽  
Lippia Alba

Lippia alba is a plant widely studied due to both chemical diversity and bioactivities related to its ethnobotanical uses. In this work, the composition of the volatile secondary metabolites (volatile fractions/essential oil, EO) of the flower/leaves of L. alba (from northern region of Colombia) was determined by solid phase micro-extraction/distillation-solvent extraction/microwave-hydrodistillation/gas chromatography-mass spectrometry (MWHD/GC-MS), along with some in vitro biological properties (cytotoxicity and acetylcholinesterase enzyme [AChe] inhibition) from leaf EO. Outstanding results were found: (i) cis-piperitone oxide (~13%-46%), germacrene D (~11%-30%), and limonene (~10%-22%) characterized the volatile secondary metabolites from different parts of the plant; (ii) leaf EO showed a moderate hemolytic activity (HC50: 580 ± 1 µg/mL), a significant cytotoxicity on lymphocytes (LC50: 127 ± 3 µg/mL), a high cytotoxicity on HEp2 cell line (LC50: 38 ± 2 µg/mL), and a moderate inhibitory effect on AChE (IC50: 28 ± 2 µg/mL). Based on these results, a new chemovar of L. alba is reported (represented by cis-piperitone oxide) along with its promising cytotoxic and AChE inhibiting properties.

scholarly journals BIOLOGICAL ACTIVITIES OF NOVEL IN VITRO RAISED STEVIA PLANT

2017 ◽  
Vol 10 (8) ◽  
pp. 240 ◽  
Author(s):  
Neeta Raj Sharma ◽  
Vineet Meshram ◽  
Mahiti Gupta
Keyword(s):  
Pancreatic Lipase ◽  
Staphylococcus Epidermidis ◽  
Inhibitory Activity ◽  
Inhibitory Concentration ◽  
Methanolic Extract ◽  
Biological Activities ◽  
Gram Negative Bacteria ◽  
Herbal Formulation ◽  
Further Development

  Objective: This communication explores a lead fraction from methanolic extract of novel Stevia species raised under in vitro conditions for its various biological activities.Methods: The dried Stevia leaves were crushed in methanol to get the polar extract. This methanol extract was tested for pancreatic lipase and alpha-amylase inhibitory activity using quantitative plate assays. Antibacterial property of the extract was also evaluated against Staphylococcus epidermidis, Escherichia coli, Bacillus subtilis, Staphylococcus aureus, and Pseudomonas aeruginosa. Further, the antioxidant potential was evaluated using 1,1-diphenyl-2-picrylhydrazyl.Results: The methanolic extract inhibited pancreatic lipase with IC50 of 5.74 μg/ml in a similar manner to a well-known anti-obesity drug in the market orlistat. The methanolic extract also showed a better pancreatic α-amylase inhibitory activity (IC50=88 μg/ml) than acarbose. Further, the lead fraction exhibited 88.48% antioxidant activity. It also exhibited broad spectrum antimicrobial activity against the spectrum of Gram-positive and Gram-negative bacteria tested under laboratory conditions with a minimal inhibitory concentration ranging from 1.95 to 31.25 μg/ml.Conclusion: Thus, this study signifies the vast potential of the lead fraction from a novel Stevia species for further development into a herbal formulation for prevention of various infectious and non-infectious diseases.

scholarly journals Fullerenol: A new nanopharmaceutic?

2008 ◽  
Vol 16 (3-4) ◽  
pp. 42-45 ◽  
Author(s):  
Aleksandar Djordjevic ◽  
Gordana Bogdanovic
Keyword(s):  
Biological Activities ◽  
Cancer Cell Growth ◽  
Biological Investigation ◽  
In Vivo Models ◽  
Breast Cancer Cell Growth ◽  
Biodistribution Studies ◽  
Biological Studies ◽  
C60 Derivatives

Chemical modification of fullerenes to hydrosoluble cluster molecules made fullerenes interesting for biological investigation. Among them, polycarbonated and polyhydroxylated fullerene C60 derivatives showed the most interesting biological activities. In this paper, we present the most important recent results of in vitro and in vivo biological studies with fullerenol C60(OH)24. Fullerenol C60(OH)24 was strong antioxidant: it reacted with superoxide anion radical, hydroxy radical and nitrous oxide radical in chemical and biological systems. Fullerenol C60(OH)24 did not inhibit human breast cancer cell growth at concentrations from 0.8 to 3.45 ?M, but strongly modulated cytotoxic effects of doxorubicin and cis-platinum after 24 and 48 hours of treatment. Radioprotective effects of fullerenol C60(OH)24 were shown in different in vitro and in vivo models. Fullerenol C60(OH)24 (100 mg/kg) protected rat heart from doxorubicin toxicity. Biodistribution studies of fulelrenol were also investigated. Accumulating data from the literature and from our studies suggest that fullerenol, as a nanoparticle might be a new promising pharmaceutical in the near future.

scholarly journals Biological activities of the lignicolous fungus Meripilus giganteus (Pers.: Pers.) Karst.

2009 ◽  
Vol 61 (4) ◽  
pp. 853-861 ◽  
Author(s):  
Maja Karaman ◽  
Sonja Kaisarevic ◽  
Jelena Somborski ◽  
M. Kebert ◽  
M. Matavulj
Keyword(s):  
Biological Activities ◽  
Breast Cancer Cell Lines ◽  
Oh Radicals ◽  
Acetyl Cholinesterase ◽  
Reducing Ability ◽  
Cholinesterase Inhibitory Activity ◽  
Dried Extract ◽  
Bacterial Effect ◽  
Mcf 7

Crude extracts (methanolic-ME andwater-WE) of the fungus Meripilus giganteus (Pers.: Pers.) Karst. were analyzed for their antioxidative, antibacterial, cytotoxic, neurotoxic, and hemolytic activities using tests in vitro. The highest scavenging activity was exhibited by WE on OH? radicals, showing a 50% effective concentration (EC50) at 292.83?2.5 ?g/ml and ferric-reducing ability at 14.24?2.9 mg eq of ascorbic acid per g of dried extract (mg/g).An anti?bacterial effect was detected mostly against Gram-positive strains of bacteria. Toxicity assays exhibited higher effects for ME, reaching EC50=403.43?5.8 ?g/ml against estrogen-dependent breast cancer cell lines (MCF-7); 50% hemolytic activity at a concentration of 30?0.03 ?g/ml against erythrocytes; andEC50=4.5?0.05 mg/ml for acetyl cholinesterase-inhibitory activity. These results suggest possible use of this fungus as a new source of pharmaceuticals.

scholarly journals In Vitro Anticancer Screening and Preliminary Mechanistic Study of A-Ring Substituted Anthraquinone Derivatives

Cells ◽  
2022 ◽  
Vol 11 (1) ◽  
pp. 168
Author(s):  
Ibrahim Morgan ◽  
Ludger A. Wessjohann ◽  
Goran N. Kaluđerović
Keyword(s):  
Cell Lines ◽  
Mechanism Of Action ◽  
Biological Activities ◽  
Mechanistic Study ◽  
Redox Active ◽  
Anthraquinone Derivatives ◽  
M Phase ◽  
Ic50 Values ◽  
Plant Families

Anthraquinone derivatives exhibit various biological activities, e.g., antifungal, antibacterial and in vitro antiviral activities. They are naturally produced in many fungal and plant families such as Rhamnaceae or Fabaceae. Furthermore, they were found to have anticancer activity, exemplified by mitoxantrone and pixantrone, and many are well known redox-active compounds. In this study, various nature inspired synthetic anthraquinone derivatives were tested against colon, prostate, liver and cervical cancer cell lines. Most of the compounds exhibit anticancer effects against all cell lines, therefore the compounds were further studied to determine their IC50-values. Of these compounds, 1,4-bis(benzyloxy)-2,3-bis(hydroxymethyl)anthracene-9,10-dione (4) exhibited the highest cytotoxicity against PC3 cells and was chosen for a deeper look into its mechanism of action. Based on flow cytometry, the compound was proven to induce apoptosis through the activation of caspases and to demolish the ROS/RNS and NO equilibrium in the PC3 cell line. It trapped cells in the G2/M phase. Western blotting was performed for several proteins related to the effects observed. Compound 4 enhanced the production of PARP and caspase-3. Moreover, it activated the conversion of LC3A/B-I to LC3A/B-II showing that also autophagy plays a role in its mechanism of action, and it caused the phosphorylation of p70 s6 kinase.

scholarly journals Synthesis and Biological Evaluation of New Substituted 3-[4-(Phenylsulfonamido)benzoyl]-2H-1-benzopyran-2-one Derivatives asα-Glucosidase Inhibitors

2014 ◽  
Vol 2014 ◽  
pp. 1-6 ◽  
Author(s):  
Yu-ling Wang ◽  
Ting-jian Zhang ◽  
Jing-wei Liang ◽  
Fan-hao Meng ◽  
Shao-jie Wang
Keyword(s):  
Inhibitory Activity ◽  
Methoxy Group ◽  
Biological Activities ◽  
Biological Evaluation ◽  
Glucosidase Inhibitors ◽  
Further Development ◽  
Synthesis And Biological Evaluation

A series of new substituted 3-[4-(phenylsulfonamido)benzoyl]-2H-1-benzopyran-2-one derivatives bearing groups methoxy,tert-butyl, and atoms of halogens at thepara-position of the A-ring were synthesized andin vitrobiological activities were evaluated as nonsugarα-glucosidase inhibitors. Most of the test compounds demonstrated significantα-glucosidase inhibitory activity relative to that of Acarbose (IC50= 29.26 μM). Thepara-substitution with a methoxy group or halogens could notably increase the potency. Compounds17,18, and23, with IC50values of 0.025 μM, 0.014 μM, and 0.018 μM, respectively, may be of significance for the further development of new nonsugarα-glucosidase inhibitors.

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