| Article: Au, T.K.; Lam, T.L.; Ng, T.B.; Foung, W.P.; Wan, D.C.C. A
comparison of HIV-1 integrase inibition by aqueous and methanol extracts of
Chinese medicinal herbs. Life Sciences 2001 68: 1687-1694. Au et al. found that when the aqueous and methanol extracts of twenty Chinese
herbs were screened for anti-HIV-1-integrase activity, most
exhibited strong inhibition. Furthermore, Au et al found that the
inhibitor substance in these herbs was most likely a tannin (using a similar
technique to Liu), and most lost their anti-integrase activity when the tannin
was removed. However, to herbs in particular, Paeonia suffruticosa
(PS) and Prunella vulgaris (PV), still exerted potent inhibition
of HIV-1 integrate even with the tannin removed.
The details of the study:
- The viral enzyme integrase is necessary for HIV to complete it's life
cycle. Specifically, it is needed to integrate viral DNA (constructed
during earlier steps of the lifecycle) into the host's DNA
- The dried herbs used in this study were obtained from local Hong-Kong
vendors. The herbs used included the following: The dried herbs were
obtained from local vendors. For Viola yedoensis, Andrographis paniculata,
Senecio scandens and Oldenlandia diffusa, the whole plant was used. For
Fritillaria cirrhosa, Coptis chinesis, Woodwardia unigemmata and Spatholobus
suberectus, therhizome was used. For Sophora flavescens, Radix notoginseng,
Polygonum multiflorum and Paeonia suffruticosa, the root was used. For
Chrysanthemum indicum, Chrysanthemum morifolium, Prunella vulgaris and
Lonicera japonica, the flower was used. For Arctium lappa and Ligustrum
lucidum , the seed was used. For Lithospermum erythrorhizon both root and
seed were used, respectively.14
- HIV-1 integrase was produced by expression
plasmids in E.Coli, then purified into solution
- Researchers used a ELIZA-based technique as
follows:
- Wells were coated with standard lab target DNA
- Integrase was added to well, along with
biotin-labeled donor DNA, and herb extract. This mixture was incubated
for one hour. During this time, integrase would attach the
biotin-labeled DNA to the target DNA, unless inhibited by the herbal
extract.
- Wells were then washed with distilled water
and an enzyme that would react with the biotin-labeled donor DNA to produce
a fluorescence that could be measured by spectrophotometry.
- Thus, a strong fluorescent reaction would
indicate that the biotin-label DNA was present, which meant that integrase
had done its job. On the other hand, a low fluorescent reaction would
mean that the herbal extract successful inhibited integrase.
- Inhibition was measured before and after the
researcher used additional techniques to separate tannins from each extract.
- Results for the aqueous extracts are shown
graphically below:

- Fig. 1. The inhibitory effects of aqueous herb extracts (mean 6 S. D.)
on the activity of HIV-1 integrase before (h) and after (j) passing through
the polyamide resin mini-column. Each data represented a mean of three
separate measurements. The vertical bars indicate the standard deviations.
- PV and PS extracts continued to show HIV-1-integrase inhibition despite
having the tannins removed

- Study Conclusion: Several Chinese herbs (see above for names)
contain potent anti HIV-1-integrase activity. The active compounds are
likely tannins, supported by the fall in their anti-integrase activity after
the tannin was removed. However, to herbs in particular, Paeonia
suffruticosa (PS) and Prunella vulgaris (PV), still
exerted potent inhibition of HIV-1 integrate even with the tannin removed,
suggesting a unrelated compound within these often-use Chinese herbs that
displays anti-integrase activity.
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