Potential of radioiodinated anticancer compounds of traditional Chinese medicine for cancer therapy

23-Hydroxybetulinic acid (23-HBA) is the efficient antitumor compound extracted from the roots of a Chinese Medicinal Herb, Pulsatilla chinensis (Bge) Regel. To evaluate the effect of radioiodination on cytotoxicity, 23-HBA was radioiodinated with ¹²⁵I. ¹²⁵I-23-HBA could be prepared in high yields and good radiochemical purity and was characterized using reverse phase HPLC. In ICR mice bearing Liver Cancer HepA tumor, ¹²⁵I-23-HBA showed a tumor uptake of 2.1% ID/g at 2 h p.i. and 0.15% ID/g at 48 h p.i on i.v. injection. When injected intratumorally, greater tumor uptake and retention was observed (20% ID/g at 2 h p.i. and 4.6% ID/g at 48 h p.i. respectively).