Podcast
Questions and Answers
Productivity in agriculture has been enhanced due to advances in ______ control.
Productivity in agriculture has been enhanced due to advances in ______ control.
pest
The rise in resistance to current control agents has prompted the search for new ______.
The rise in resistance to current control agents has prompted the search for new ______.
pesticides
Between 1984 to 1990, resistance to synthetic chemical pesticides increased by ______%.
Between 1984 to 1990, resistance to synthetic chemical pesticides increased by ______%.
13
A significant amount of research has focused on isolating insecticidal leads from marine ______.
A significant amount of research has focused on isolating insecticidal leads from marine ______.
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This research has led to the isolation of over ______ active constituents.
This research has led to the isolation of over ______ active constituents.
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Synthetic chemical pesticides are also referred to as ______ (SCPs).
Synthetic chemical pesticides are also referred to as ______ (SCPs).
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The search for new pesticides has been necessary due to the significant rise in ______ to current control agents.
The search for new pesticides has been necessary due to the significant rise in ______ to current control agents.
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Insects and mites have shown resistance to chemical pesticides, prompting an increase in ______ research.
Insects and mites have shown resistance to chemical pesticides, prompting an increase in ______ research.
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The AIDS pandemic in the 1980s forced organizations to explore natural products as sources of potential drug candidates for the treatment of ______.
The AIDS pandemic in the 1980s forced organizations to explore natural products as sources of potential drug candidates for the treatment of ______.
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Over 60,000 extracts of plants and marine organisms were tested against lymphoblastic cells infected with ______.
Over 60,000 extracts of plants and marine organisms were tested against lymphoblastic cells infected with ______.
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The most important compounds found through these tests are known as ______.
The most important compounds found through these tests are known as ______.
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Calanolide A and B were isolated from the ______ species.
Calanolide A and B were isolated from the ______ species.
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Prostratin was isolated from ______ nutans.
Prostratin was isolated from ______ nutans.
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Arteether, introduced in 2000, is derived from ______.
Arteether, introduced in 2000, is derived from ______.
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Artemisia annua was first used in traditional Chinese medicine as a remedy for ______ and fevers.
Artemisia annua was first used in traditional Chinese medicine as a remedy for ______ and fevers.
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Bryologs, including ______, are derived from bryostatin 1.
Bryologs, including ______, are derived from bryostatin 1.
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Other derivatives of artemisinin are in various stages of ______ development as antimalarial drugs in Europe.
Other derivatives of artemisinin are in various stages of ______ development as antimalarial drugs in Europe.
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Bryostatin 1 (54) is an antineoplastic compound isolated from ______.
Bryostatin 1 (54) is an antineoplastic compound isolated from ______.
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Bryostatin 1 (54) has been involved in more than ______ clinical trials.
Bryostatin 1 (54) has been involved in more than ______ clinical trials.
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From 2007 to now, there have been four Phase ______ trials of bryostatin 1.
From 2007 to now, there have been four Phase ______ trials of bryostatin 1.
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Halichondrin B (55) has been isolated from several types of ______.
Halichondrin B (55) has been isolated from several types of ______.
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Halichondrin E-7389 (56) is currently in Phase ______ trials for breast carcinoma.
Halichondrin E-7389 (56) is currently in Phase ______ trials for breast carcinoma.
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Halichondrin B (55) was successfully ______ along with its analogues.
Halichondrin B (55) was successfully ______ along with its analogues.
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Bryostatin 1 (54) has shown responses ranging from complete to ______ remission.
Bryostatin 1 (54) has shown responses ranging from complete to ______ remission.
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The process of isolating, purifying, and determining the structure of a suspected novel ______ can be time-consuming.
The process of isolating, purifying, and determining the structure of a suspected novel ______ can be time-consuming.
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Classical techniques such as Ultraviolet absorption Spectroscopy (UV) and Infra-red spectroscopy (IR) assist in the determination of ______ compounds.
Classical techniques such as Ultraviolet absorption Spectroscopy (UV) and Infra-red spectroscopy (IR) assist in the determination of ______ compounds.
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Single-crystal ______ analysis is utilized when the absolute configuration cannot be determined.
Single-crystal ______ analysis is utilized when the absolute configuration cannot be determined.
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Hyphenated systems like HPLC-FTIR help in the ______ process of natural product extracts.
Hyphenated systems like HPLC-FTIR help in the ______ process of natural product extracts.
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FIA-NMR involves the injection of a sample as a ______ into a fluid stream.
FIA-NMR involves the injection of a sample as a ______ into a fluid stream.
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The mobile phase in FIA-NMR acts as a ______ to carry the sample to the NMR detector.
The mobile phase in FIA-NMR acts as a ______ to carry the sample to the NMR detector.
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HPLC-NMR-MS is an advanced hyphenated ______ technique used in dereplication.
HPLC-NMR-MS is an advanced hyphenated ______ technique used in dereplication.
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The main advantage of HPLC-NMR-MS is the unequivocal matching of the MS data to the ______ spectrum.
The main advantage of HPLC-NMR-MS is the unequivocal matching of the MS data to the ______ spectrum.
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The application of HPLC-NMR to crude extracts was found to be a powerful ______ tool.
The application of HPLC-NMR to crude extracts was found to be a powerful ______ tool.
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Extraction, isolation, purification, and structure elucidation are classical methodologies for studying novel bioactive ______ products.
Extraction, isolation, purification, and structure elucidation are classical methodologies for studying novel bioactive ______ products.
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Microcoil HPLC-NMR and capillary NMR have advanced due to the advent of higher field ______ and cryo-probes.
Microcoil HPLC-NMR and capillary NMR have advanced due to the advent of higher field ______ and cryo-probes.
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The choice of extraction solvent can cause many problems including the formation of ______.
The choice of extraction solvent can cause many problems including the formation of ______.
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Capillary NMR allows the use of non-deuterated solvents in the off-line HPLC ______.
Capillary NMR allows the use of non-deuterated solvents in the off-line HPLC ______.
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Homogenization and lyophilization with organic solvents can affect the nature and relative amounts of extracted ______ metabolites.
Homogenization and lyophilization with organic solvents can affect the nature and relative amounts of extracted ______ metabolites.
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The extraction is normally the first step for both marine and terrestrial ______.
The extraction is normally the first step for both marine and terrestrial ______.
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Isolated compounds are redissolved in deuterated solvents and subjected to ______-NMR spectroscopy.
Isolated compounds are redissolved in deuterated solvents and subjected to ______-NMR spectroscopy.
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The information acquired from both 1D and 2D NMR spectra may be sufficient to identify compound ______.
The information acquired from both 1D and 2D NMR spectra may be sufficient to identify compound ______.
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The use of HPLC-NMR in natural products identification is well ______ in the literature.
The use of HPLC-NMR in natural products identification is well ______ in the literature.
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Metabolomics aims to characterize all gene and cell products including mRNA, proteins, glycan structures and ______.
Metabolomics aims to characterize all gene and cell products including mRNA, proteins, glycan structures and ______.
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A single analytical technique capable of profiling all low molecular weight ______ of a given organism does not exist.
A single analytical technique capable of profiling all low molecular weight ______ of a given organism does not exist.
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Mass spectrometry hyphenated with gas chromatography, liquid chromatography, or capillary electrophoresis and nuclear magnetic resonance (NMR) are the leading analytical ______.
Mass spectrometry hyphenated with gas chromatography, liquid chromatography, or capillary electrophoresis and nuclear magnetic resonance (NMR) are the leading analytical ______.
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Both primary and secondary metabolites in tissues and biofluids are extracted utilizing ______ crude extraction procedures.
Both primary and secondary metabolites in tissues and biofluids are extracted utilizing ______ crude extraction procedures.
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Systems biology encompasses tools in the post-genomics revolution such as transcriptomics, proteomics, glycomics and ______.
Systems biology encompasses tools in the post-genomics revolution such as transcriptomics, proteomics, glycomics and ______.
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Combining analytical chemistry, biochemistry and sophisticated informatics allows for the analysis of thousands of small ______ in any biological system.
Combining analytical chemistry, biochemistry and sophisticated informatics allows for the analysis of thousands of small ______ in any biological system.
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Study Notes
Historical Overview of Natural Products in Drug Discovery
- Natural products have historically been used for treating illnesses
- Early records of natural product use are found in cuneiform tablets, Ebers Papyrus, and Chinese Materia Medica
- Traditional use of natural products often involved trial and error, with palatability tests and/or observations on negative effects
- Examples include Salvia for childbirth, Alhagi maurorum's sap (manna), and various fungal and plant extracts for specific ailments
- Classical natural product chemistry has led to many drug candidates
- Modern hyphenated spectroscopic techniques aid in natural product discovery
- Metabolomic profiling and dereplication approaches provide comprehensive study of natural extracts
Primary and Secondary Metabolites
- Primary metabolism involves building blocks like proteins, fats, nucleic acids, and carbohydrates, essential for all living things
- Secondary metabolites are not essential for survival and have a unique profile for an organism; they are often a defense mechanism or adaptation to the environment
- Secondary metabolites, also called natural products, are formed from primary metabolic intermediates like acetyl-CoA, shikimic acid, mevalonic acid, and 1-deoxyxylulose-5-phosphate
- Natural products exhibit diverse biological activities
Historically Important Natural Products
- Acetylsalicylic acid (aspirin) was derived from salicin.
- Morphine, isolated from opium poppy.
- Quinine (used for malaria).
- Pilocarpine for glaucoma.
- Penicillin from Penicillium notatum.
- Vancomycin.
- Erythromycin.
- Important natural products for diseases (e.g., cancer, infections, autoimmune disorders).
Natural Products from Fungi
- Piptoporus betulinus fungus used for antiseptic and corn pads.
- Agaricus campestris (field mushroom) for throat ailments.
- Lichens for dyes and cosmetics.
- Penicillin (a significant antibiotic).
Natural Products from Plants
- Plants have been used medicinally for thousands of years
- Extracts of plants have been crucial for developing medicines (e.g., aspirin, morphine, taxol, etc.).
Natural Products from Marine Algae
- Algae are a rich source of structurally diverse natural products (e.g., terpenoids).
- Examples include polycavernoside-A (seafood poisoning), diterpenes (antitumor activity)
- Polycavernoside-A (38) isolated from the red alga (seafood poisoning).
- 4-acetoxydictylolactone (39), dictyolides A (40), B (41), and nordictyolide (42) display antitumor activities sourced from an alga.
Natural Products from Marine Sponges
- Sponges contain unique chemical compounds, like sponge-derived C-nucleosides (e.g., spongouridine (51) and spongothymidine (52)) that are biologically active.
Natural Products from Other Marine Sources
- Bryo-stains for biological activities.
- Halichondrin B and E-7389 for use as anticancer drugs
- Artemisia annua is the source of Artemisin and Arteether
Natural Product Chemistry versus Combinatorial Chemistry
- Combinatorial chemistry creates many compounds efficiently; natural products are structurally complex and their synthesis is challenging
- Current strategies combine methods from natural products, combinatorial chemistry, and new biotechnologies to optimize drug discovery.
Dereplication Strategies
- Dereplication identifies known compounds to eliminate unnecessary testing.
- Uses various methods (e.g., spectroscopic techniques, databases, bioassays) to expedite discovery of novel compounds and identify known ones.
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Description
This quiz explores the innovations in pest control within agriculture, particularly focusing on the rise of pesticide resistance and the investigation of natural products. Participants will learn about the historical context and ongoing research essential for effective pest management. Test your knowledge on the significant findings and developments in the field of pesticide research!
