Rational approaches to lead discovery based on traditional medicine MCQs With Answer

Rational approaches to lead discovery based on traditional medicine integrate ethnopharmacology, pharmacognosy and modern drug‑discovery tools to identify, validate and optimize bioactive natural products. B.Pharm students should understand bioassay‑guided fractionation, dereplication, phytochemical screening, metabolomics, molecular docking, SAR and ADMET profiling to translate folk claims into credible drug leads. Emphasis on standardization, voucher specimens, quality control, ethical bioprospecting and regulatory pathways ensures reproducible, safe candidates. Combining computational methods, high‑throughput approaches and network pharmacology with traditional knowledge accelerates hit‑to‑lead progression while minimizing rediscovery and attrition. This evidence‑based framework equips future pharmacists for interdisciplinary R&D in natural product drug discovery. Now let’s test your knowledge with 30 MCQs on this topic.

Q1. What is the primary goal of ethnopharmacology in rational lead discovery from traditional medicine?

• To commercialize traditional remedies without scientific validation
• To document traditional uses and provide leads for scientific investigation
• To replace modern drugs with herbal preparations
• To synthesize analogues of synthetic drugs

Correct Answer: To document traditional uses and provide leads for scientific investigation

Q2. Reverse pharmacology in the context of traditional medicines means:

• Starting with high‑throughput screening of pure compounds and then testing in humans
• Beginning with clinical or traditional use observations and moving back to laboratory validation
• Using animal models only for lead identification
• Designing synthetic libraries based on folk recipes

Correct Answer: Beginning with clinical or traditional use observations and moving back to laboratory validation

Q3. Bioassay‑guided fractionation is best described as:

• Isolating compounds solely by polarity regardless of activity
• Tracking biological activity through successive fractionation to isolate active constituents
• Using genomic assays to identify active species
• Analyzing botanical identity by DNA barcoding

Correct Answer: Tracking biological activity through successive fractionation to isolate active constituents

Q4. Dereplication in natural product research aims to:

• Ensure all isolates are novel without using databases
• Rapidly identify known compounds early to avoid re‑isolating them
• Enhance extraction yields of minor constituents
• Replace bioassays with chemical tests

Correct Answer: Rapidly identify known compounds early to avoid re‑isolating them

Q5. Why is a voucher specimen important when studying medicinal plants?

• It provides chemical standardization of extracts
• It serves as authenticated physical reference for species identity
• It is required only for patent applications
• It replaces the need for DNA authentication

Correct Answer: It serves as authenticated physical reference for species identity

Q6. Which marker is most useful for extract standardization?

• A non‑bioactive impurity
• A reproducible active or characteristic compound quantified in the extract
• An unrelated synthetic molecule added post‑extraction
• Only the total dry weight of the extract

Correct Answer: A reproducible active or characteristic compound quantified in the extract

Q7. Metabolomics contributes to lead discovery by:

• Sequencing DNA of medicinal plants
• Profiling the full complement of small molecules to identify biomarkers and chemical fingerprints
• Replacing all bioassays with MS data
• Measuring only primary metabolites like sugars

Correct Answer: Profiling the full complement of small molecules to identify biomarkers and chemical fingerprints

Q8. Molecular docking in the context of traditional‑medicine leads is used to:

• Predict compound‑target interactions computationally and prioritize candidates
• Measure in vivo efficacy directly
• Standardize plant extracts based on color
• Quantify total phenolic content

Correct Answer: Predict compound‑target interactions computationally and prioritize candidates

Q9. Network pharmacology is particularly advantageous for herbal mixtures because it:

• Assumes a single active principle is always responsible for efficacy
• Models multi‑target, multi‑component interactions to explain synergistic effects
• Only applies to synthetic drug combinations
• Focuses exclusively on pharmacokinetics

Correct Answer: Models multi‑target, multi‑component interactions to explain synergistic effects

Q10. A common challenge when adapting high‑throughput screening (HTS) to natural product libraries is:

• Natural products always show no bioactivity
• Crude extracts cause assay interference and supply/complexity issues
• HTS is ineffective for any complex mixtures
• HTS requires no optimization for extracts

Correct Answer: Crude extracts cause assay interference and supply/complexity issues

Q11. Structure‑activity relationship (SAR) studies help lead optimization by:

• Altering molecular features to improve potency, selectivity and ADMET
• Only increasing molecular weight to enhance efficacy
• Eliminating all polar groups regardless of activity
• Replacing natural extract studies entirely

Correct Answer: Altering molecular features to improve potency, selectivity and ADMET

Q12. Why is ADMET profiling critical for natural product leads?

• It confirms botanical identity
• It assesses absorption, distribution, metabolism, excretion and toxicity to predict in vivo behavior
• It replaces the need for efficacy studies
• It is only relevant for synthetic small molecules

Correct Answer: It assesses absorption, distribution, metabolism, excretion and toxicity to predict in vivo behavior

Q13. Which analytical approach is most useful for early dereplication of known natural products?

• LC‑MS coupled with database matching
• Thin‑layer chromatography without standards
• Visual inspection of extract color
• Only NMR without prior MS data

Correct Answer: LC‑MS coupled with database matching

Q14. An effective strategy to improve oral bioavailability of a poorly absorbed phytochemical is:

• Administering the pure compound with a high‑fat diet only
• Formulating it as nanoparticles or using prodrugs to enhance absorption
• Reducing dose frequency without formulation changes
• Avoiding any formulation changes and relying on traditional use

Correct Answer: Formulating it as nanoparticles or using prodrugs to enhance absorption

Q15. Ethical bioprospecting requires which of the following practices?

• Ignoring local knowledge and patenting discoveries unilaterally
• Benefit sharing, informed consent and respecting indigenous rights
• Using plant resources without documentation
• Exporting specimens without permits

Correct Answer: Benefit sharing, informed consent and respecting indigenous rights

Q16. A major patentability challenge for leads from traditional medicine is:

• Proving novelty when similar uses are documented in traditional knowledge
• High chance of immediate patent grant without evidence
• Patents are not applicable to chemical entities
• Patenting guarantees market approval

Correct Answer: Proving novelty when similar uses are documented in traditional knowledge

Q17. Which method is commonly used to quantify synergy between two herbal constituents?

• Random sampling without statistical analysis
• Isobologram or combination index analysis
• Only organoleptic testing
• Serial dilution without reference controls

Correct Answer: Isobologram or combination index analysis

Q18. Important quality control tests for herbal raw materials include:

• Only organoleptic properties and taste
• Heavy metals, pesticide residues, microbial limits and phytochemical fingerprints
• Exclusively DNA sequencing for all batches
• No testing is needed if traditional use exists

Correct Answer: Heavy metals, pesticide residues, microbial limits and phytochemical fingerprints

Q19. The difference between authentication and standardization of herbal materials is:

• Authentication verifies species identity; standardization ensures consistent chemical composition
• They are identical terms with no practical difference
• Authentication standardizes extract potency
• Standardization replaces the need for authentication

Correct Answer: Authentication verifies species identity; standardization ensures consistent chemical composition

Q20. Which phytochemical class is most frequently associated with antioxidant activity in medicinal plants?

• Saturated hydrocarbons
• Phenolics and flavonoids
• Inorganic salts
• Polysaccharides only

Correct Answer: Phenolics and flavonoids

Q21. Activity‑guided isolation typically requires which of the following to be effective?

• Bioassays that are relevant, sensitive and reproducible for the target activity
• Random chemical separation without monitoring activity
• Only spectroscopic dereplication without bioassays
• Exclusively computational predictions

Correct Answer: Bioassays that are relevant, sensitive and reproducible for the target activity

Q22. A major analytical advance that reduces rediscovery of known compounds is:

• Anonymous crude extract testing
• Integration of LC‑MS/MS, NMR databases and cheminformatics for dereplication
• Relying solely on botanical morphology
• Ignoring spectral databases

Correct Answer: Integration of LC‑MS/MS, NMR databases and cheminformatics for dereplication

Q23. Chemometrics assists in traditional‑medicine lead discovery by:

• Applying multivariate statistics to analyze complex chemical fingerprints and correlate with bioactivity
• Replacing biological assays entirely
• Only measuring single marker compounds
• Eliminating need for sample preparation

Correct Answer: Applying multivariate statistics to analyze complex chemical fingerprints and correlate with bioactivity

Q24. An important factor when translating in vitro activity of a phytochemical to in vivo efficacy is:

• Assuming identical potency in vivo without testing
• Metabolic stability, bioavailability and pharmacokinetics
• Only the color of the extract
• Using in vitro data as final proof of therapeutic effect

Correct Answer: Metabolic stability, bioavailability and pharmacokinetics

Q25. Which preclinical toxicology studies are typically required before first‑in‑human trials for a new herbal lead?

• No studies are required if the herb is traditionally used
• Acute, subchronic toxicity and genotoxicity assessments
• Only chronic toxicity for five years
• Only organoleptic testing

Correct Answer: Acute, subchronic toxicity and genotoxicity assessments

Q26. The gold‑standard clinical design to validate an efficacy claim from traditional medicine is:

• An uncontrolled observational report
• A randomized, placebo‑controlled, double‑blind clinical trial
• A single case study without controls
• Only in vitro evidence submitted to regulators

Correct Answer: A randomized, placebo‑controlled, double‑blind clinical trial

Q27. Which statement best describes the role of standard operating procedures (SOPs) in lead discovery from herbs?

• SOPs are optional and not useful for reproducibility
• SOPs ensure consistent collection, extraction and assay procedures to make results reproducible
• SOPs only document marketing claims
• SOPs guarantee clinical success

Correct Answer: SOPs ensure consistent collection, extraction and assay procedures to make results reproducible

Q28. In the context of herbal formulations, ‘quality by design’ means:

• Designing products without considering variability
• Systematically understanding factors affecting quality to design robust manufacturing processes
• Relying exclusively on traditional recipes without testing
• Using ad hoc adjustments during production only

Correct Answer: Systematically understanding factors affecting quality to design robust manufacturing processes

Q29. Which approach helps prioritize candidates from complex extracts for isolation?

• Biochemometrics combining bioactivity data with chemical profiling
• Isolating the most abundant compound regardless of activity
• Random compound selection
• Only relying on traditional popularity

Correct Answer: Biochemometrics combining bioactivity data with chemical profiling

Q30. Regulatory expectations for herbal-derived leads typically require evidence of:

• Only traditional use with no scientific data
• Quality, safety and appropriate evidence of efficacy proportional to the intended claim
• Immediate market approval without data
• Only botanical illustrations

Correct Answer: Quality, safety and appropriate evidence of efficacy proportional to the intended claim

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