申请人:Mori Masao
公开号:US20070066684A1
公开(公告)日:2007-03-22
An antiviral preparation comprising as an active ingredient, a phorbol derivative of formula 1:
wherein is R
1
—(CH
2
)
a
X(CH
2
)
b
CH
3
, —(CH
2
)
c
X(CH
2
)
d
YCH
3
, —CO(CH
2
)
e
CH
3
or —(CH
2
)
f
CH
3
R
2
is —CO(CH
2
)
n
CH
3
, R
3
, R
4
and R
5
are hydrogen atom, or an aliphatic or aromatic carboxylic acid residue, X and Y are O or S, and each of a-f and n is a number, and having a specific safety index S.I.=CC
50
/EC
50
of 10 or more wherein EC
50
means a concentration at which HIV-1 induced cytopathogenic effect (CPE) in MT-4 cell is inhibited by 50%, and CC
50
means a concentration at which survival of MT-4 cell in a cell proliferation test is reduced by 50%. These preparations are particularly effective for human immuno-deficiency virus (HIV).
一种抗病毒制剂,其活性成分为式1的一种佛波醇衍生物:
其中R
1
为—(CH
2
)
a
X(CH
2
)
b
CH
3, —(CH
2
)
c
X(CH
2
)
d
YCH
3, —CO(CH
2)
e
CH
3或—(CH
2)
f
CH
3,R
2
为—CO(CH
2)
n
CH
3,R
3,R
4
和R
5
为氢原子,或脂肪族或芳香族羧酸残基,X和Y为O或S,a-f和n中的每个是一个数字,并具有特定的安全指数S.I.=CC
50
/EC
50
大于或等于10,其中EC
50
表示HIV-1诱导的MT-4细胞中细胞病理效应(CPE)被抑制50%的浓度,CC
50
表示MT-4细胞在细胞增殖试验中存活率降低50%的浓度。这些制剂对人类免疫缺陷病毒(HIV)特别有效。