Goodman and Gilman's The
Pharmacological Basis of Therapeutics
14th Edition
Author(s)Laurence Brunton; Bjorn Knollmann
Print ISBN: 9781264258079
,Question 1
A researcher investigating a traditional medicinal plant identifies several
compounds in its extract. Which next step would most directly help
determine whether a particular compound contributes to the plant’s
therapeutic effect?
A. Determine the compound’s patent status before testing it
B. Isolate the individual compounds and evaluate their biological
,activity
C. Convert all compounds into injectable formulations
D. Perform population-wide clinical trials before identifying active
constituents
Correct Answer:
B. Isolate the individual compounds and evaluate their biological
activity
Rationale:
B is correct because separating constituents allows investigators to
determine which molecule or molecules are responsible for a
measurable biological effect. This process can lead to identification of
an active principle that becomes a starting point for drug discovery.
A is incorrect because intellectual-property considerations are
important later in development but do not establish biological activity.
C is incorrect because formulation development is premature when the
active constituent has not yet been identified.
D is incorrect because clinical development should follow identification
and characterization of promising active compounds rather than
precede them.
Question 2
Why has isolation of active chemical constituents from medicinal plants
been an important strategy in drug discovery?
A. It guarantees that the isolated compound will have a favorable
therapeutic index
B. It converts traditional observations into testable molecular
, hypotheses
C. It eliminates the need for toxicity testing
D. It ensures that the compound will be orally active
Correct Answer:
B. It converts traditional observations into testable molecular
hypotheses
Rationale:
B is correct because identifying a specific constituent allows researchers
to connect an observed biological effect with a defined chemical entity
and subsequently investigate its mechanism, efficacy, and safety.
A is incorrect because isolation does not establish therapeutic safety or
selectivity.
C is incorrect because isolated compounds still require extensive safety
evaluation.
D is incorrect because oral activity depends on properties such as
absorption, stability, and metabolism and cannot be assumed from
natural origin.
Question 3
A medicinal chemistry team modifies the structure of a naturally
occurring compound to improve its duration of action while preserving
its desired biological activity. What is this strategy best described as?
A. Structural optimization of a lead compound
B. Target devalidation
C. Phenotypic blindness
D. Regulatory substitution