220
N. N. Win and H. Morita
Fig. 86 The crude drug Swertia chirata (whole plant). The original plant is known as Pan-khar or
Thinbaw-sega-gyi, and the whole plant is used in traditional medicine in Myanmar
potent activity than that of the positive control, damnacanthal. In another investigation, Kashiwada et al. reported [543] that 382 inhibited HIV-1 replication in acutely
infected H9 cells (EC 50 value of 1.7 μg/cm
3 ) and inhibited H9 cell growth (IC 50 value
of 21.8 μg/cm
3 ). The finding of oleanolic acid as a Vpr inhibitor is supportive of
further studies being carried out on compound 382 and/or its derivatives as possible
anti-HIV agents.
Naturally occurring xanthones have emerged as an important class of organic
compounds in terms of their documented pharmacological and biological activities.
The structure-activity relationship conclusions among the isolated xanthones (decussatine (429), methylbellidifolin (430), and bellidifolin (432)), suggested that the presence of hydroxy groups at C-5 and C-8 in 432 favored the inhibition of the expression
of Vpr, rather than the presence of the methoxy substituents at C-5, C-7, and C-8 in
429 and 430, which led to decreases in their activities. Bellidifolin (432) is a simple
oxygenated xanthone that reportedly possesses strong hypoglycemic activity [539]
and monoamine oxidase inhibitory activity [544]. This compound also reportedly
inhibits the production of the proinflammatory cytokines IL-6 and tumor necrosis
factor-α (TNF-α) and the production of prostaglandin E2 (PGE2) by suppressing
the protein expression of COX-2 in LPS-stimulated RAW264.7 macrophages [545].
Treatment with 432 also reportedly suppressed the phosphorylation of the inhibitor
κB kinase-β (IKK-β), Akt, and the p65 subunit of NF-κB [546]. Thus, these Vpr inhibition findings of 432 have provided a new insight into its bioactivity. The detection
N. N. Win and H. Morita
Fig. 86 The crude drug Swertia chirata (whole plant). The original plant is known as Pan-khar or
Thinbaw-sega-gyi, and the whole plant is used in traditional medicine in Myanmar
potent activity than that of the positive control, damnacanthal. In another investigation, Kashiwada et al. reported [543] that 382 inhibited HIV-1 replication in acutely
infected H9 cells (EC 50 value of 1.7 μg/cm
3 ) and inhibited H9 cell growth (IC 50 value
of 21.8 μg/cm
3 ). The finding of oleanolic acid as a Vpr inhibitor is supportive of
further studies being carried out on compound 382 and/or its derivatives as possible
anti-HIV agents.
Naturally occurring xanthones have emerged as an important class of organic
compounds in terms of their documented pharmacological and biological activities.
The structure-activity relationship conclusions among the isolated xanthones (decussatine (429), methylbellidifolin (430), and bellidifolin (432)), suggested that the presence of hydroxy groups at C-5 and C-8 in 432 favored the inhibition of the expression
of Vpr, rather than the presence of the methoxy substituents at C-5, C-7, and C-8 in
429 and 430, which led to decreases in their activities. Bellidifolin (432) is a simple
oxygenated xanthone that reportedly possesses strong hypoglycemic activity [539]
and monoamine oxidase inhibitory activity [544]. This compound also reportedly
inhibits the production of the proinflammatory cytokines IL-6 and tumor necrosis
factor-α (TNF-α) and the production of prostaglandin E2 (PGE2) by suppressing
the protein expression of COX-2 in LPS-stimulated RAW264.7 macrophages [545].
Treatment with 432 also reportedly suppressed the phosphorylation of the inhibitor
κB kinase-β (IKK-β), Akt, and the p65 subunit of NF-κB [546]. Thus, these Vpr inhibition findings of 432 have provided a new insight into its bioactivity. The detection