Chemistry Reference
In-Depth Information
(100). In continuing work in the laboratories of the authors, dimethoxy-4-
ethoxycarbonylethylenyl-curcumin (
J3
) showed potent anti-androgenic activity
and therefore is a promising prostate cancer drug candidate (101, 102). A
recent review from the laboratories of the authors discusses the design and
development of curcumin analogs as promising candidates for chemotherapy of
prostate cancer (103). In addition, the sesquiterpene curcumol (
J4
), obtained
from
Curcuma aromatica
Salisb., was effective against cervical cancer (104).
14.1.11 Euphorbia species
Euphorbia kansui
Liou (Euphorbiaceae family) is distributed widely in northwest
China. The dried roots of the plant are known as “kansui” and classified as a
lower-class medicine. It is used as an herbal remedy for ascites (abdominal fluid
accumulation) and cancer in China.
Ingenol diterpenoids are among the bioactive chemical constituents. Kan-
suiphorins A-D (
K1
-
K4
) were isolated as cytotoxic principles of
E. kansui
by the laboratories of the authors (105, 106). In particular,
K1
and
K2
demon-
strated potent antileukemic activity against P-388 leukemia in mice (105). A
related ingenol-type diterpene (DBDI,
K5
) showed unique suppression of mast
cell activation, a process that occurs during inflammation, and thus, might have
the potential to treat allergic diseases (107). In other pharmacological studies,
two isolated ingenols from an immuno-enhancing
E. kansui
extract increased
immune activity in a dose-dependent manner (108). Three new cytotoxic diter-
penoids, yuexiandajisus D (
K6
), E (
K7
), and F (
K8
), were isolated from the
species
E. ebrateolata
Hayata. (109). In additional studies,
K6
showed moderate
cytotoxicity against additional (HCT-8 and Bel-7402) cell lines (110).
14.2 ANTI-HIV COMPOUNDS
Acquired immunodeficiency syndrome (AIDS), a degenerative disease of the
immune system, is caused by the human immunodeficiency virus (HIV) and
results in life-threatening opportunistic infections and malignancies. Antiviral
and immunomodulating natural products have been investigated as treatments
for AIDS (111).
14.2.1 Lomatium suksdorfii (coumarin derivatives)
Suksdorfin (
L1
), a dihydroseselin-type angular pyranocoumarin isolated from
Lomatium suksdorfii
Coult. Rose (Apiaceae family) was identified as a lead anti-
HIV natural product through BDFI (112). Substitution of two camphanoyl esters
for the acetate and isovaleroyl groups in the natural product lead to the extremely
potent lead compound 3
R
,4
R
-di-
O
-(
−
)-camphanoyl-(+)-
cis
-khellactone (DCK)
(
L2
) (113).
