Abstract

Several plant extracts and isolated compounds have shown promising anti-HIV activity. In this chapter, the anti-HIV activity of alkaloids isolated from medicinal plants and other natural resources has been discussed. Though many extracts and compounds have shown significant activity, none has demonstrated the potency to qualify for clinical trials. For example, a semisynthetic derivative of a natural alkaloid, harman, has shown better EC50 (0.037 μM) than the FDA-approved drug azidothymidine (AZT) (EC50 = 0.045 μM). However, the therapeutic index (TI) for that compound was much lower (210) than that of AZT (41667). Similarly, the anti-HIV EC50 values for the alkaloids ptilomycalin A and crambescidine 800 were found to be quite low (0.11 μM and 0.4 μM, respectively) but, these compounds simultaneously displayed prominent cytotoxicity as well, at concentrations of between 0.03 μM and 10 μg/mL, respectively. Another alkaloid, waltherione C (78) exhibited improved anti-HIV cytoprotection activity (EC50 = 0.84 μM) than the positive control (AZT) (EC50 = 1.30 μM). A quinolone type alkaloid, buchapine (80) has been reported to protect CEM-SS cells from cytopathic effects of HIV-1 with an EC50 of 0.94 μM. However, the TI value for that compound was found to be only 31. Therefore, further discovery of more potent, safe and cost-effective anti-HIV natural products is noteworthy.

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