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For Bryan................Patent on variouis whole cell 5AR-inhibitors (Topicals)
Ive cut and pasted from the patent (a very long patent indeed, geesh):
http://www.patentstorm.us/patents/6696484-description.html
1. Green Tea Catechins
TABLE 1
Inhibition of 5 α-reductase isozymes by green tea catechinsa
5 α-Reductase
Cell-Free assay IC50 (µM) Whole-cell assay IC50
(µM)
Catechin Type 1 Type 2 Type 1 Type 2
EC >100 (14) >100 (4) >100 (0) >100 (1)
EGC >100 (15) >100 (3) >100 (15) >100 (1)
ECG 11 (100) 69 (83) >100 (0) >100 (0)
EGCG 15 (99) 74 (74) >100 (6) >100 (0)
a IC50 : concentration (µM) of compound producing 50%
inhibition of 5 α-reductase activity. Values in parentheses are
percent inhibition of 5 α-reductase activity in the presence of 100
µM concentration of the indicated compound.
Here is another:
3. Flavonoids
A variety of naturally occurring flavonoids with structures related to the tea catechins were also tested (FIG. 1, Table 3).
TABLE 3
Inhibition of 5 α-reductase isozymes by various natural
flavonoidsa
5 α-Reductase
Cell-Free assay IC50 (µM) Whole-cell assay IC50
(µM)
Polyphenol Type 1 Type 2 Type 1 Type 2
Myricetin 23 (96) >100 (31) >100 (11) >100 (11)
Quercitin 23 (96) >100 (14) >100 (15) >100 (29)
Baicalein 29 (79) 99 (51) >100 (24) >100 (4)
Fisetin 57 (97) >100 (4) >100 (42) >100 (27)
Biochanin A >100 (50) 17 (74) 64 (64) 5 (93)
Daidzein >100 (3) 29 (69) 10 (13) 7 (89)
Kaempferol >100 (22) 12 (62) 79 (60) 20 (85)
Flavone >100 (20) >100 (-52) NDb ND
Genistein >100 (16) 23 (76) >100 (22) 20 (89)
Morin >100 (6) >100 (33) ND ND
Alpha- >100 (6) >100 (-13) ND ND
napthoflavone
Taxifolin >100 (5) >100 (5) ND ND
Beta- >100 (3) >100 (4) ND ND
napthoflavone
Chrysin >100 (2) >100 (1) ND ND
Rutin >100 (4) >100 (0) ND ND
Another:
TABLE 4
Inhibition of 5 α-reductase by compounds containing catecholsa
5 α-Reductase
Whole-cell
Cell-free assay IC50 (µM) assay IC50 (µM)
Catechol Type 1 Type 2 Type 1 Type 2
Anthrarobon 4 (99) 50 (97) 6 (91) >100 (31)
Bromopyrogallol 7 (98) 84 (58) NDb ND
red
Gossypol 7 (99) 21 (99) 7 (100) 6 (99)
Pyrogallol red 15 (97) >100 (27) ND ND
Nordihydro- 19 (99) 50 (80) 19 (99) 22 (99)
guaiaretic acid
Caffeic acid 26 (97) >100 (36) 8 (99) 7 (98)
phenethyl ester
Octyl gallate 27 (99) 58 (90) 7 (99) 18 (94)
Purpurogallin 30 (81) >100 (31) ND ND
Hydroxydopamine 42 (69) >100 (41) ND ND
Dodecyl gallate 43 (88) >100 (36) 3 (99) 7 (98)
Pyrocatechol violet 48 (85) 100 (47) ND ND
Pyrogallol 70 (60) >100 (28) >100 (7) >100 (15)
Hematoxylin 83 (59) >100 (38) ND ND
HZIV-82 >100 (43) >100 (0) 3 (79) >100 (15)
Cnc >100 (42) >100 (-75) ND ND
HZIV 90 >100 (23) >100 (13) >100 (34) >100 (14)
Caffeic acid >100 (13) >100 (8) ND ND
HZIV 275 >100 (10) >100 (6) ND ND
Esculetin >100 (7) >100 (13) ND ND
Ellagic acid >100 (7) >100 (9) ND ND
Catechol >100 (5) >100 (0) >100 (9) >100 (3)
Methyl gallate >100 (5) >100 (3) >100 (0) >100 (0)
Propyl gallate >100 (0) >100 (0) >100 (5) >100 (0)
Fraxetin >100 (2) >100 (8) ND ND
Curcumoids:
TABLE 5
Inhibition of 5 α-reductase isozymes by curcumin and related
compoundsa
5 α-Reductase
Whole-cell
Cell-Free assay IC50 (µM) assay IC50 (µM)
Compound Type 1 Type 2 Type 1 Type 2
Curcumin 3 (95) 5 (87) 9 (99) 7 (99)
Tetrahydrocurcumin 80 (56) 29 (73) NDb ND
Demethoxy- >100 (23) >100 (42) ND ND
tetrahydrocurcumin
4-hydroxy-3- >100 (10) >100 (-60) ND ND
methoxy-
cinnamaldehyde
Coniferol >100 (10) 100 (49) ND ND
4-(4-hydroxy-3- >100 (3) >100 (4) ND ND
methoxyphenol)-3-
buten-2-one
Ferulic Acid >100 (0) >100 (18) ND ND
Capsaicin >100 (0) >100 (8) ND ND
Eugenol >100 (0) 100 (50) ND ND
TABLE 1
Inhibition of 5 α-reductase isozymes by green tea catechinsa
5 α-Reductase
Cell-Free assay IC50 (µM) Whole-cell assay IC50
(µM)
Catechin Type 1 Type 2 Type 1 Type 2
EC >100 (14) >100 (4) >100 (0) >100 (1)
EGC >100 (15) >100 (3) >100 (15) >100 (1)
ECG 11 (100) 69 (83) >100 (0) >100 (0)
EGCG 15 (99) 74 (74) >100 (6) >100 (0)
TABLE 2
Inhibition of 5 α-reductase by various EGC derivativesa
5 α-Reductase
Whole-cell assay
Cell-free assay IC50 (µM) IC50 (µM)
EGC derivatives Type 1 Type 2 Type 1 Type 2
1. EGCG 12 (99) 73 (76) >100 (11) >100 (5)
2. HZIV 160 29 (99) 76 (96) 7 (99) 8 (98)
3. HZIV 134 20 (99) 67 (94) NDb ND
4. HZIV 92 23 (98) >100 (45) 64 (94) 80 (62)
5. HZIV 120 23 (99) 66 (97) 49 (97) 57 (96)
6. HZIV 142 25 (97) 63 (93) 8 (99) 14 (98)
7. HZIV 68 29 (93) 99 (51) >100 (40) >100 (34)
8. HZIV 75 29 (97) >100 (21) 43 (83) 62 (72)
9. HZIV 166 30 (98) 78 (74) 58 (89) 72 (83)
10. HZIV 63 311 (94) >100 (20) >100 (12) >100 (7)
11. HZIV 169 47 (90) >100 (39) >100 (10) >100 (0)
12. HZIV 74 48 (85) >100 (24) ND ND
13. HZIV 144 49 (88) >100 (38) >100 (12) >100 (7)
14. HZIV 168 49 (98) 73 (92) 28 (93) 41 (94)
15. HZIV 166 59 (95) 71 (84) 58 (89) 72 (83)
16. EGC 62 (61) >100 (30) >100 (15) >100 (1)
17. HZIV 107 98 (52) >100 (39) >100 (23) >100 (2)
18. HZIV 145 >100 (35) >100 (8) >100 (8) >100 (9)
19. HZIV 148 >100 (31) >100 (0) 42 (90) 74 (81)
20. HZIV 109 >100 (17) >100 (0) ND ND
a IC50 : concentration (µM) of compound producing 50%
TABLE 4
Inhibition of 5 α-reductase by compounds containing catecholsa
5 α-Reductase
Whole-cell
Cell-free assay IC50 (µM) assay IC50 (µM)
Catechol Type 1 Type 2 Type 1 Type 2
Anthrarobon 4 (99) 50 (97) 6 (91) >100 (31)
Bromopyrogallol 7 (98) 84 (58) NDb ND
red
Gossypol 7 (99) 21 (99) 7 (100) 6 (99)
Pyrogallol red 15 (97) >100 (27) ND ND
Nordihydro- 19 (99) 50 (80) 19 (99) 22 (99)
guaiaretic acid
Caffeic acid 26 (97) >100 (36) 8 (99) 7 (98)
phenethyl ester
Octyl gallate 27 (99) 58 (90) 7 (99) 18 (94)
Purpurogallin 30 (81) >100 (31) ND ND
Hydroxydopamine 42 (69) >100 (41) ND ND
Dodecyl gallate 43 (88) >100 (36) 3 (99) 7 (98)
Pyrocatechol violet 48 (85) 100 (47) ND ND
Pyrogallol 70 (60) >100 (28) >100 (7) >100 (15)
Hematoxylin 83 (59) >100 (38) ND ND
HZIV-82 >100 (43) >100 (0) 3 (79) >100 (15)
Cnc >100 (42) >100 (-75) ND ND
HZIV 90 >100 (23) >100 (13) >100 (34) >100 (14)
Caffeic acid >100 (13) >100 (8) ND ND
HZIV 275 >100 (10) >100 (6) ND ND
Esculetin >100 (7) >100 (13) ND ND
Ellagic acid >100 (7) >100 (9) ND ND
Catechol >100 (5) >100 (0) >100 (9) >100 (3)
Methyl gallate >100 (5) >100 (3) >100 (0) >100 (0)
Propyl gallate >100 (0) >100 (0) >100 (5) >100 (0)
Fraxetin >100 (2) >100 (8) ND ND
6. Quinones
A variety of quinones were tested for activity against 5α-reductase (Table 6, FIG. 4).
TABLE 6
Inhibition of 5 α-reductase isozymes by quinonesa
5 α-Reductase
Cell-Free Whole-cell
assay IC50 (µM) assay IC50 (µM)
Quinone Type 1 Type 2 Type 1 Type 2
Purpurin 2 (95) >100 (20) NDb ND
Alizarin 3 (95) >100 (54) 6 (75) >100 (27)
Anthrarobin 4 (99) 50 (97) 6 (91) >100 (31)
Menadione 6 (77) 5 (81) 51 (82) 79 (62)
Coenzyme q 12 (77) 22 (81) ND ND
2,5- 15 (78) 17 (97) ND ND
dichloroindophenol
Alizarin red S 30 (91) >100 (8) >100 (22) >100 (1)
Anthrarufin 40 (67) >100 (13) ND ND
Anthraflavic acid >100 (27) >100 (22) ND ND
Quinizarin >100 (26) >100 (7) ND ND
Lapachol >100 (30) >100 (9) ND ND
t- >100 (19) >100 (4) ND ND
butylhydroxyquinone
Anthraquinone >100 (6) >100 (9) ND ND
TABLE 9
Effects of green tea catechin derivatives and fatty acids, on testosterone-
stimulated growth of the pigmented macules of hamster flank organs.
Pigmented
macule area Inhibition
Treatment (mm2) (%)a P-valueb
T (control) 17.40 ± 1.93 --
T + myristoleic acid (1 mg) 4.63 ± 0.66 73 <0.05
T + EGC-myristoleate (1 mg) 5.00 ± 0.42 71 <0.05
T + γ-linolenic acid (1 mg) 3.15 ± 0.42 82 <0.05
T + EGC-γ-linoleneate acid 5.50 ± 0.56 68 <0.05
(1 mg)
T + EGC (1 mg) 5.50 ± 0.65 68 <0.05
T + EGCG (1 mg) 6.25 ± 0.82 64 <0.05
a Percent decrease in area of macules treated with tea catechins,
fatty acid or catechin derivatives compared to the area of
androgen-treated macules
b Mean area of androgen-treated vs catechin-, fatty acid- or catechin
derivative-treated macules; one-way ANOVA
.
TABLE 10
Effects of alizarin and curcumin on testosterone- or DHT-stimulated
growth of the pigmented macules of hamster flank organs.
Pigmented
macule area Inhibition P-
Experiment Treatment (mm2) (%)a valueb
I T (control) 18.65 ± 0.69 --
T + alizarin (1 mg) 2.40 ± 0.47 87 <0.05
T + curcumin (1 mg) 2.40 ± 0.65 87 <0.05
II DHT (control) 13.67 ± 0.96 --
DHT + alizarin (1 mg) 10.00 ± 0.43 27 <0.05
DHT + curcumin 9.50 ± 0.21 31 <0.05
(1 mg)
a Percent decrease in area of macules treated with alizarin or
curcumin compared to androgen-treated macules
b Mean area of androgen-treated vs. alizarin- or curcumin-treated
macules; one-way ANOVA
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Complete thread:
- Topical green tea................massive reduction in sebum: Study
- benji, 27.03.2008, 02:00 (Topicals)
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- Topical green tea................massive reduction in sebum: Study
- Goingallout, 27.03.2008, 08:52
- Topical green tea................massive reduction in sebum: Study
- benji, 27.03.2008, 13:24
- Topical green tea................massive reduction in sebum: Study
- Bryan, 27.03.2008, 18:30
- Topical green tea................massive reduction in sebum: Study
- ludwig, 27.03.2008, 19:47
- Topical green tea................massive reduction in sebum: Study
- Bryan, 27.03.2008, 21:15
- Topical green tea................massive reduction in sebum: Study
- benji, 27.03.2008, 23:00
- For Bryan................Patent on variouis whole cell 5AR-inhibitors - benji, 27.03.2008, 23:32
- For Bryan..............WHERE CAN WE FIND THESE????
- benji, 27.03.2008, 23:53
- Caffeic acid-----Good Friggin' Grief!!!!!!!!!!!!
- benji, 28.03.2008, 00:16
- Caffeic acid-----Good Friggin' Grief!!!!!!!!!!!! - Jacob, 30.03.2008, 09:46
- Caffeic acid-----Good Friggin' Grief!!!!!!!!!!!!
- benji, 28.03.2008, 00:16
- For Bryan..............WHERE CAN WE FIND THESE????
- benji, 27.03.2008, 23:53
- For Bryan................Patent on variouis whole cell 5AR-inhibitors - benji, 27.03.2008, 23:32
- Topical green tea................massive reduction in sebum: Study
- benji, 27.03.2008, 23:00
- Topical green tea................massive reduction in sebum: Study
- Bryan, 27.03.2008, 21:15
- Topical green tea................massive reduction in sebum: Study
- ludwig, 27.03.2008, 19:47
- Topical green tea................massive reduction in sebum: Study
- Bryan, 27.03.2008, 18:30
- Topical green tea................massive reduction in sebum: Study
- benji, 27.03.2008, 13:24
- Topical green tea................massive reduction in sebum: Study - HanginInThere, 28.03.2008, 15:44
- Topical green tea................massive reduction in sebum: Study - Jtelecom, 30.03.2008, 17:16
- Topical green tea................massive reduction in sebum: Study
- Goingallout, 27.03.2008, 08:52