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Isolation and Characterization of Cytotoxic Compounds from Detarium microcarpum Guill. and Perr. Stem Bark
Kayode Muritala Salawu1, Omonike Oluyemisi Ogbole2, Oyindamola Oduola Abiodun3
1Department of Pharmacognosy and Drug Development, University of Ilorin, Ilorin, Nigeria.
Introduction:
Globally, about 8.2 million cancer-related deaths are recorded annually. Sadly, most of the deaths result from the toxicity of most chemotherapeutic agents. Hence, there are growing demands for chemotherapeutic agents with high specificity and selectivity. This study was designed to assess the cytotoxic potential of Detarium microcarpum and isolate cytotoxic compounds with better selectivity profiles.
Methods:
Detarium microcarpum Stem bark (DMS) was collected and authenticated at the Forest Herbarium Ibadan (FHI), and a voucher (FHI-111954) was issued. Dried DMS was pulverized and extracted into 70% methanol. The extract was partitioned into hexane, dichloromethane, and ethyl acetate fractions. The cytotoxicities of the extract, fractions, and isolated compounds were determined. The cytotoxicity of the isolated compounds was tested against different cell lines, including human breast (AU565 and MDA MB231), oral adenosquamous (CAL27), and cervical (HeLa) cancer cells, as well as healthy (3T3) non-cancer cells.
Results:
Methyl gallate, eriodictyol, quercetin, quebrachitol, catechin, catechin gallate, and gallic acid, isolated from dichloromethane and ethyl acetate fractions, displayed weak cytotoxicity against breast (AU565 and MDAMD- 231) and cervical (HeLa) cancer cell lines. Interestingly, all the compounds, except gallic acid (48.91±4.51% inhibition), displayed potent cytotoxicity on oral cancer cells. Methyl gallate and quercetin displayed the highest activity, with IC50 values of 89.57±1.98μM and 78.19±1.49μM, respectively. Interestingly, all the compounds were not toxic to healthy non-cancer (3T3) cells.
Conclusion:
The compounds displayed anticancer activity specific to oral cancer cells and were highly selective for cancer cells without causing significant toxicity to healthy non-cancer cells.
Insights
Detarium microcarpum compounds show potent oral cancer cell cytotoxicity and selectivity. These natural agents offer a promising, less toxic alternative to conventional chemotherapy.
Area of Science:
- Phytochemistry
- Pharmacology
- Cancer Research
Background:
- High cancer mortality necessitates safer chemotherapeutic agents with improved specificity.
- Current treatments often cause toxicity, driving demand for selective anticancer drugs.
Purpose of the Study:
- To evaluate the cytotoxic potential of Detarium microcarpum (DMS).
- To isolate and characterize cytotoxic compounds from DMS with enhanced selectivity profiles.
Main Methods:
- Detarium microcarpum stem bark was extracted and fractionated.
- Cytotoxicity of extracts, fractions, and isolated compounds was assessed against human oral, breast, and cervical cancer cell lines, alongside healthy non-cancer cells.
- Compounds were isolated from dichloromethane and ethyl acetate fractions.
Main Results:
- Seven compounds were isolated: methyl gallate, eriodictyol, quercetin, quebrachitol, catechin, catechin gallate, and gallic acid.
- Compounds showed potent cytotoxicity against oral cancer cells (CAL27), with methyl gallate and quercetin exhibiting the highest activity (IC50 values 89.57±1.98μM and 78.19±1.49μM, respectively).
- All tested compounds demonstrated selectivity, with no significant toxicity observed in healthy non-cancer (3T3) cells.
Conclusions:
- Isolated compounds from Detarium microcarpum exhibit specific anticancer activity against oral cancer.
- These compounds display high selectivity, targeting cancer cells while sparing healthy cells, indicating a favorable safety profile.
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