Garg A, Sinha VR, Zaneveld LJ, Anderson RA, Garg S; International Conference on AIDS (15th : 2004 : Bangkok, Thailand).

Int Conf AIDS. 2004 Jul 11-16; 15: abstract no. TuPeB4654.

University of Auckland, Auckland, New Zealand

Background: An abundant, inexpensive and easily available citrus flavonoid, Hesperidin, was sulphonated and the active identified for inhibiting various sexually transmitted pathogens including HIV, based on their hyaluronidase inhibiting (HI) activity. The purified and characterised compound was then formulated into novel vaginal dosage forms. Methods: Hesperidin (97% pure) was sulphonated under strictly controlled conditions of temperature, time, sulphonating agent and solvents. The product with best HI properties was purified and the active component isolated and characterised. Reproducibility of the synthetic method was established. The active compound (SH) was then subjected to extensive biological evaluation including HI, dose response and reversibility, inhibition of C.trachomatis, N.gonorrhoea, HSV-2, HIV, and cervical mucus penetration. Safety assessment was based on its effect on the growth of lactobacillus, toxicity to host cells for HIV (MT-2 cells) and performing sperm function tests. SH was subjected to preformulation study and formulated into novel fast dispersing tablets and bioadhesive gel. These were then evaluated pharmaceutically and bioactivity and the formulation stability established. Results: SH prepared under controlled conditions and then isolated and purified, was found to highly active against all pathogens tested, It completely inhibited sheep testicular hyaluronidase at 200 mug per ml(reversible and dose dependant) and was highly active against Chlamydia, gonorrhoea, HSV and HIV. It was found to be non-toxic to the host cells, lactobacillus (normal vaginal flora) and to the sperm. It possessed excellent preformulation characteristics and was easily amenable to formulate as a vaginal microbicide. Conclusions: Sulphonated hesperidin (SH) can be reproducibely synthesised and is very active against a range of sexually transmitted pathogens, including HIV. It possesses great potential for development as a vaginal microbicide.

Publication Types:

• Meeting Abstracts

Keywords:

• Acquired Immunodeficiency Syndrome
• Alkanesulfonates
• Anti-Infective Agents
• Chlamydia Infections
• Female
• Gonorrhea
• HIV
• HIV Infections
• HIV Seropositivity
• Herpesvirus 2, Human
• Hesperidin
• Lactobacillus

Other ID:

• GWAIDS0038260

UI: 102282476

From Meeting Abstracts