Drugs from Natural Products Flashcards

1
Q

In the 16th century, which books became popular? What information did they contain?

A

In the 16th century, texts known as herbals became very popular. These books listed common herbal remedies and the ailments they were indicated for.

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2
Q

What was the first synthetically produced medicine?

A

The first synthetic production medicine was acetylsalicylate (aspirin) by Bayer in 1899.

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3
Q

Why are natural products chemically/pharmaceutically relevant?

A

Nature can do chemistry that chemists find very hard, at room temperature and in water. Nature has had millions of years to perfect the chemical reactions that produce such products which leads to the production of a wide range of complex molecules.

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4
Q

Give an example of a chemical characteristic that nature can create more efficiently than scientists?

A

Chiral centres.

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5
Q

What is the active moiety in Curare?

A

Tubocurarine.

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6
Q

When did western explorers first come across Curare?

A

The 16th century.

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7
Q

In the early 1800s Charles Waterton and Claud Bernard experimented with Curare, what did they discover?

A

They discovered it blocked nerve transmission leading to respiratory failure.

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8
Q

How did Charles Waterton and Claude Bernard carry out their experiments with Curare?

A

They experimented on animals and themselves, so they personally could describe the effects they felt.

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9
Q

When tubocurarine was isolated from Curare, what was it used for/as?

A

It was used as a muscle relaxant in surgery. This proved very beneficial in abdominal surgery as the abdominal muscles can contract when they are cut into and this can cause the flesh to tear and become damaged.

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10
Q

Name two synthetic analogues of tubocurarine.

A

Panocurium and atracurium.

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11
Q

The structure of which neurotransmitter is mimicked by that of tubocurarine?

A

Acetylcholine.

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12
Q

Describe the action of tubocurarine.

A

Tubocurarine acts by binding to motor end plate receptors blocking the action of nicotinic acetylcholine, blocking nerve transmission and muscle contraction.

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13
Q

Tubocurarine has two acetylcholine mimicking sections which are spaced apart in the molecule; why is this important for its action?

A

This spacing is incredibly important as it helps define the drugs therapeutic index; preventing toxicity and allowing the drug to be used at optimum doses.

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14
Q

From what plant is hyoscine derived?

A

Henbane.

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15
Q

From what plant is atropine derived?

A

The deadly nightshade.

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16
Q

Describe the actions of hyoscine and atropine.

A

These compounds block the muscarinic acetylcholine receptor selectively.

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17
Q

How were deadly nightshade berries used cosmetically in renaissance Italy?

A

In Italy, during the Renaissance, deadly nightshade berries were squeezed into the eyes of women to dilate their pupils and make them more attractive to men. Belladonna translates to ‘beautiful woman’ and this is where the name comes from.

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18
Q

In ancient Greece and Rome, how was henbane used?

A

In ancient Greece and Rome, henbane was used to induce trance-like states associated with prophecy.

19
Q

In what year was atropine first isolated?

A

1831.

20
Q

What was the first medical use of atropine?

A

In ophthalmology, to look into a patient’s eye.

21
Q

Give a synthetic analogue of atropine?

A

Ipratropium.

22
Q

What is ipratropium used for?

A

The treatment of asthma by inhalation.

23
Q

Esere is extracted from what plant?

A

The castor bean.

24
Q

What was esere used for by African tribes?

A

Trial by ordeal.

25
Q

What did Robert Christison find out about esere, after testing it on himself?

A

That it blocked the heart muscle rather than the respiratory system.

26
Q

What did Thomas Fraser note when he put esere into an eye?

A

That is caused by pupillary contraction and copious tear production, the opposite of atropine.

27
Q

What did Thomas Fraser’s experiments show about the potential medical uses of esere?

A

That it could be used as a treatment for glaucoma.

28
Q

What is the active moiety in esere?

A

Physostigmine.

29
Q

What did the discovery of the active moiety of esere, physostigmine, also lead to?

A

The discovery of acetylcholine as a neurotransmitter and acetylcholinesterase.

30
Q

What enzyme does physostigmine block?

A

Acetylcholinesterase.

31
Q

What conditions are still treated by physostigmine?

A

This compound is still used to treat myasthenia gravis, glaucoma, and Alzheimer’s (through the stabilization of neurons).

32
Q

What are the active compounds in the Amanita muscarina mushroom?

A

Ibotenic acid and muscimol.

33
Q

What receptor does ibotenic acid work on?

A

NMDA.

34
Q

What receptor does muscimol work on?

A

GABA.

35
Q

The Amanita phalloides mushroom also goes by another name, what is it?

A

The death cap mushroom.

36
Q

What are the active compounds in the Amanita phalloides mushroom?

A

Amanitins.

37
Q

What pharmacological effect do amanitins have?

A

These compounds block RNA polymerase II and have a slow onset.

38
Q

What is St. Anthony’s Fire?

A

Consummation of bread made from contaminated rye causes loss of blood flow to the extremities, a condition known as St. Anthony’s fire, which can lead to gangrene.

39
Q

Chemically, what is ergotamine?

A

An ergot alkaloid.

40
Q

The vasoconstrictive effects of ergotamine have been used for what medical uses?

A

Post-partum bleeding and initiation of abortion.

41
Q

Which drug of abuse was inspired by/developed from ergotamine?

A

LSD.

42
Q

What neurotransmitter is mimicked by ergotamine?

A

5-HT.

43
Q

Describe the process of microbial screening.

A

In this process, microorganisms are isolated from the environment and grown in the lab. They are then screened for activity of interest. If this is successful, then the active compounds are purified using the activity as a marker.