Table 2.
Quantification of anti-HSV activity of Kampo formulas with reference compounds.
| Test Sample | Viability of HSV- Infected Cells (%) |
CC50 | EC50-I | EC50-II | Anti- HSV Activity |
Max. Cell Recovery (%) |
|
|---|---|---|---|---|---|---|---|
| SI-I | SI-II | ||||||
| Kampo formula (Supplementary Figure S2) (mg/mL) | |||||||
| S1 Unkeito | 27 | >3.0 | (-) | 1 | (-) | >3.0 | 51 |
| S2 Chotosan | 25 | 2.6 | (-) | >3.0 | (-) | <0.87 | 48 |
| S3 Hochuekkito | 25 | >3.0 | (-) | >3.0 | (-) | ><1.0 | 44 |
| S4 Hangebyakujutsutemmato | 26 | 1.35 | (-) | >3.0 | (-) | <0.45 | 41 |
| S5 Kakkonto | 29 | 1.65 | 0.58 | 0.56 | >5.2 | >5.4 | 78 |
| S6 Shomakakkonto | 34 | 2.1 | (-) | >3.0 | (-) | <0.70 | 46 |
| S7 Sokeikakketsuto | 29 | >3.0 | (-) | >3.0 | (-) | ><1.0 | 46 |
| S8 Seijobofuto | 34 | 0.58 | (-) | >3.0 | (-) | <0.19 | 39 |
| S9 Yokukansan | 31 | >3.0 | 2.9 | 1.9 | >1.0 | >1.6 | 66 |
| S10 Orengedokuto | 22 | 0.76 | (-) | >3.0 | (-) | <0.25 | 30 |
| S11 Jumihaidokuto | 25 | 3 | (-) | 2.8 | (-) | 1.1 | 52 |
| S12 Yokuininto | 21 | >3.0 | (-) | 2.4 | (-) | 1.3 | 55 |
| S13 Shofusan | 21 | 2.5 | (-) | >3.0 | (-) | <0.83 | 34 |
| S14 Hainosankyuto | 24 | 2.6 | (-) | >3.0 | (-) | <0.87 | 33 |
| S15 Jizusoippo | 23 | 1.3 | (-) | >3.0 | (-) | <0.43 | 33 |
| S16 Unseiin | 23 | 1.5 | (-) | >3.0 | (-) | <0.5 | 29 |
| S17 Rikkosan | 21 | 1.8 | (-) | >3.0 | (-) | <0.60 | 34 |
| S18 Keigairengyoto | 26 | 1.6 | (-) | >3.0 | (-) | <0.53 | 34 |
| S19 Sansoninto | 23 | 1.6 | (-) | >3.0 | (-) | <0.53 | 47 |
| S20 Kakkontokasenkyushin’I | 32 | 2 | (-) | >3.0 | (-) | <0.67 | 45 |
| Alkaline extracts (mg/mL) | |||||||
| SE (Supplementary Table S1) | 20 | 2.6 | 0.7 | 0.5 | 4.5 | 6.8 | 90 |
| PCE | 19 | 2 | 0.19 | 0.17 | 13.1 | 14.7 | 82 |
| Polyphenols (µM) | |||||||
| Resveratrol | 16 | 18 | (-) | >1000 | (-) | <0.018 | 20 |
| p-Coumaric acid | 42 | 170 | (-) | >1000 | (-) | <0.17 | 43 |
| Curcumin | 22 | 16 | (-) | >100 | (-) | <0.16 | 42 |
| Chromones (µM) (Supplementary Table S2) | |||||||
| (2a) (Ref. 20) | 9 | >600 | 450 | 400 | >1.3 | >1.5 | 59 |
| (3c) (Ref. 20) | 9 | 310 | NT | 300 | NT | 1.0 | 50 |
| (14) (Ref. 21) | 11 | 31 | NT | 29 | NT | 1.1 | 51 |
| (2) (Ref. 24) | 11 | >1000 | 820 | 640 | >1.2 | >1.6 | 61 |
| (8) (Ref. 25) | 23 | 86 | ND | 180 | ND | >3.3 | 54 |
| (12) (Ref. 25) | 23 | >600 | ND | 370 | ND | >1.6 | 64 |
| Positive controls (µM) | |||||||
| ACV | 23 | >30 | 1.3 | 1.1 | >23.1 | >27.3 | 108 |
| Tricin | 18 | 10 | (-) | 1.4 | (-) | 7.1 | 68 |
Data were derived from Supplementary Figure S2 (for all 20 Kampo formula) and from Figure 4. (2a), 2-(1H-pyrazol-1-yl)-4H-1-benzopyran-4-one; (3c), 2-(1H-imidazol-1-yl)-6-methoxy-4H-1-benzopyran-4-one; (14), (3E)-2,3-dihydro-3-[(4-hydroxyphenyl)methylene]-7-methoxy-4H-1-benzopyran-4-one; (2), (2E,4E)-5-(3,4-methylenedioxyphenyl)-2,4-pentadienoic acid (4-hydroxy-3-methoxyphenyl)methyl ester; (8), 2-[(1E)-2-(4-fluorophenyl)ethenyl]-6-methoxy-4H-1-benzopyran-4-one; (12), 2-[(1E)-2-(3,4-dimethoxy) ethenyl]-6-methoxy-4H-1-benzopyran-4-one. Supplementary Tables S2 and S3 show the anti-HSV activity of SE (assayed 52 times) and a total of 119 chromone derivatives, esters, and amides.