Pages 16-20 - Cancer Treatments Flashcards

(94 cards)

1
Q

What were the sources of anti- cancer drugs?

A

Naturally occurring secondary products from plants

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2
Q

How many anti- cancer drugs do we have today ?

A

77

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3
Q

Provide a breakdown of 77 anti - cancer drugs

A

12- proteins
30- secondary products or their semi synthetic derivatives from higher plants
18- synthetics to mimic 2nd producys
17- total synthetics

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4
Q

How were many anti- cancer drugs developed?

A

Random screening of plant material
Modification (semi synthesis) of 2nd products

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5
Q

Drugs used in cancer chemotherapy are …..

A

Cytotoxic

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6
Q

What is cytotoxic ?

A

Main component cancer chemotherapy - kill specific cell
Kill cancerous cells
prevention from dividing and poliferating

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7
Q

Cytotoxin is used in ?

A

Chemotherapy
Therapeutically after semi synthetic synthesis to make them safer and effective

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8
Q

However what can cause limit use of cytotoxin?

A

Adverse side affects

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9
Q

List the anti- cancer drugs derived from plants

A

Rosy periwinkle
Pacific yew
Mayapple / american mandrake
Tree of joy
Petty spurge
Dysoxylum
Plum yew
Maytennus

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10
Q

Define Rosy Periwinkle

A

Small annual plant growing to a 1m
Native to madagascar
Common horticulture plant
Has become serious invasive weed in some cultures

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11
Q

What were some old uses of Rosy periwinkle?

A

Anti diabetic in Madagascar and Carribean (periwinkle tea cheap subs to insulin)
Smith Africa , Phillipes, southern europe - orally to lower blood sugar
South africa - diabetes and rheumatism
Brazilians - hemorrhage and scurvy

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12
Q

Tests on Rosy Periwinkle

A

NCI tested for anti- cancer properties - none
Noble and charles for diabetic properties - none found

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13
Q

If none of the tests were successful, how did rosy periwinkle become and imp anti - cancer drug?

A

Noble and charles tested for anti- diabetes- no success
Found out
- extract caused dec in WBC
- reduced bone marrow activity
- the affect on WBC led to investigation against treating leukaemia cancer

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14
Q

Leukemia cancer

A

Fatal blood disorder - abnormal increase in cancerous WBC

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15
Q

What are the two anti- cancer components found in rosy periwinkle?

A

Vinca Alkaloid - vinblastine and vincristine

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16
Q

Semi synthetic of vinca alkaloid

A

Vinorelbin

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17
Q

Which cancers did vinblastine treat

A

Hodgkin disease
Choriocarcinoma
Neoplasms

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18
Q

Hodgkin diseases

A

Cancer on lymphatic system

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19
Q

Choriocarcinoma

A

Cancer on placenta

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20
Q

Neoplasm

A

Abnormal tissue growths - tumors

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21
Q

Whats cancer did vincristine treat

A

Acute childhood leukemia

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22
Q

What cancers vinorelbine treated

A

Breast cancer
Non- small cell lung cancer

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23
Q

How do vinca alkaloids work?

A

Interfere with the spindle fibre formation during mitosis
Most effective when taken in comb with other drugs

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24
Q

PACIFIC YEW

A

Small , slow growing carniferous tree
Native to coast and intermountain regions of W.N America
Uncommon tree occurring as isolated indv in forest understory
Height of 15m
Diameter of 60cm

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25
What were some old uses
W.N American indg people - stomach aches Tsimshian of coastal British columbia - anti - cancer
26
When was the cytotoxin in pacific yew first discovered?
Us agriculture department and NCI testing anti- cancer properties in random plant sps across the world, and cytotoxin was discovered during this time . Therefore, ethnobotanical info had no value (mid 20th century)
27
What did the NCI do after ‘ many years ‘ discovering cytotoxin in pacific yew?
Compiled list of anti-cancer drugs , based on info from historical manuscripts - bowers manuscripts
28
Which historical manuscript did the NCI take the anti- cancer cytotoxin drug info from?
Bowers manuscript
29
Bowers manuscripts
4-6th century Sanskrit of Indian medicine mentioning the use of yew as anti- cancer drug in both Ayurvedic and Chinese medicine
30
Which part of pacific yew had the cytotoxin?
Bark extracts had strong cytotoxin effect in their in vitro system
31
What was the principal component in the bark extract
Alkaloid - taxol (renamed - paclitaxel)
32
Paclitaxel was used to treat which cancers ?
Ovarian and breast cancer
33
What was the consequences in use of paclitexel?
Required in very high doses 15- 20kg of paclitaxel - ovarian 200- 300 kg to treat other additional cancers Total pacific yew - 1500 tons Lead to extinction
34
Resolution to the soon extinctions of pacific yew due to large doses ?
Semi synthetic of paclitaxel using BECCATIN III as a precurosr. Obtained from leave sand small branches of European yew Which is comparatively fast growing
35
Define European yew
Comparatively large and fast growing m and common hedegrow sps in europe
36
What is the most common source of commercial paclitaxel
Hedgerow clippings from European yew
37
Mayapple / american mandrake
Long lived understory harbaceous 60m tall Native to eastern decisions forest of north america First species in spring , produces umbrella shaped , deeply lobed leave from rhizome
38
What is the special about mayapple /american mandrake.
First sps in spring Produce umbrella shaped, deeply lobed leaves from rhizomes
39
Which part is used medicinally in mayapple?
Umbrella shaped, deep lobed leaves from rhizome
40
What are the old uses of mayapple? Lost the new uses as well
Cherokee, Delaware, and Iroquois, American colonist - powerful laxative 150 yrs mayapple raisin listed as an effective laxative in the American pharmacopoeia Treatment of veneral warts, Treatment of cancerous tumors and polyps New uses - anti- viral -topical treatment for genital warts - not as an anti- cancer drug due to high toxicity side affects
41
What is the principal component in raisin
Lignan- podophyllotoxin
42
Podophyllotoxic is effective against which type of cancers ?
Kill Some types of cancers cells Damages Tumours
43
Why was podophyllotoxin discontinued
Toxic side affects as an anti - cancer drug
44
How was the toxic side affect resolved
Formation of semi- synthetic of safer ,more effective drugs
45
What were the semi- synthetics of podophyllotoxins?
Teniposides Etoside
46
Teniposide treats which cancers?
Childhood leukemia
47
Etoposides treats
Leukaemia , lymphomas, brain and bladder tumors
48
How does the podophyllotoxin works?
Anti-mitotic drug Bind to tubulin Prevents microtuble formation during cell division
49
How do teniposides and etoposides works?
Inhibition of topoisomerase I, Enzyme that is essential for the maintenance of DNA
50
Tree of Joy
Small, fast growing, deciduous tree native to southern china and Tibet .
51
Tree of joy is also called
Xi - chu
52
Used esp in which medicine?
Chinese medicine
53
Which part of the tree was used in medicine ?
Bark, roots, fruits
54
What was trees of joy used for in chinese medicine?
Treating carcinomas of - stomach - rectum - colon - bladdar
55
What is the principal compound in it ?
Camptithecin
56
How was camptithecin first identifiied?
USDA screening of many plants for cortisone precursor
57
Later on camptothecin was used for treating
Gastrointestinal tumors
58
Why was the tree of joy declined even when it was deemed affective in gastrointestinal tumors?
Severe side effects
59
Resolution to this was S.S.A of comptothecin was?
Semi synthetics of comptothecin
60
Semi synthetics of comptothecin?
Topotecan Irinotecan Other demi sythetics eg lutotecan, exatecan)
61
Topotecan
Ovarian cancer
62
Irinotecan
Colorectal canvers
63
Mode of action of topotecan and irinotecan
Inhibit action of topoisomerase l like (teniposide and etoposide).
64
Other semi synthetics of camptothecin
Chemotherapeutic treatement of leukemia , lymphoma, CNS cancer, breast cancer
65
Camptothecin compounds
Potential drug to AIDS - due to antiviral activity of some camptothecin compounds
66
Petty spurge
Small, annual, euphorb native to Europe and Westrn asia Occurs as a weed in Australia and america
67
How was it used in old times
Treating skin lesions and cancers esp basal cell carcinomas
68
What is the petty spurge principal component ?
Ingenol mebutate
69
What is ingenol mevutate used for now
Non melanoma skin cancers esl basal cell carcinomas Premalognant actinic keratosis
70
Actinin keratosis
Development of thick scaly, crusty, patches of skin following sun exposure in fair skinned patients Pre carcenous , 20 % risk of progressing to aquamous cell carcinoma
71
Mode of action of ingenol mubutate
Applied 2-3 days Induces cell death Promotes healing and restoring normal histological skin Targets sub epidermal vasculature Inflammatory and immunostimulant props
72
Dysolxylum
This genus has 60 large trees belong to meliacea family Mative to indian subcontinent and adj S.E asia and SW. china
73
Used in which medicine
Ayurvedic
74
What was this sp used for in ayurvedic medicine?
Anti -inflammatory agent Diuretic and CNS depressant D. Malabaricum - treats rheumatoid arthritis
75
Whats are the principal component in Dysocoxylum?
Chromane alkaloid - Rohitukine from the bark
76
Rohitukine is isolated from what part of which sps?
Bark of D binectiferum 2-3 % -7%
77
Over 100 semi synthetic formed one if them is anticancer called?
Flavopridol (alvocidib)
78
Falvopridol against which cancers ?
Ovarian , breast and lung cancer
79
Mode of action of flavoprodol
Inhibitor of cyclin decpendent kinases Induces cell death Cell growth inhibitor
80
Falvopridol under development for
Treating leukemia Lymphoma Esphageal lung and liver cancer
81
Falvopridol is used alone or in com
82
Pendent kinases?
Enzymes controlles progression of the cell cycle
83
Falvopridol under investigation for
Rheumatoid arthritis Anti- viral agent Contraceptive disease
84
Falvopridoll granted orphan status is US
For treating acute myeloid leukemia. Orphan status for rare disease
85
PLUM YEW
Small, slow growing caniferous tree native to japan and korea
86
When was plum yew noticed ?
Us and china found anti cancer properties in the bark of cephalotaxus sp
87
Plum yew extract shoed effects against
Leukemi and tumor cells
88
Principal component in plum yew
Alkaloid omacetaxin
89
Semi synthetic of amacetaxin
Imanitib
90
Imanitib is affective against which cancer
Chronic myeloginous leukemia
91
Mode of action of imanitib
Inhibts enzyme that is specific to cancer cell
92
Renewed intrest in omacetoxin after imatinib
Due to resistance to imatinib
93
Oxmacetaxine approved by us for treatement of
Chronic myelogenous leukaemia especially in patients resistant to imatinib
94
Mode of action of omacetaxin
Inhibit elongation steps in protein syn