Anti-HIV-1 and cytotoxicity of the alkaloids ofErythrina abyssinicaLam. growing in Sudan

Abstract

Erythrina abyssinica Lam. is an important medicinal plant growing in Sudan; its seeds were investigated for the first time for their alkaloidal constituents and biological activity. The in vitro cytotoxicity of the crude alkaloidal fraction (CAF) against the cell lines HeLa, Hep-G2, HEP-2, HCT116, MCF-7 and HFB4 showed promising activity, with IC₅₀ values of 13.8, 10.1, 8.16, 13.9, 11.4 and 12.2 µg mL⁻¹, respectively. Doxorubicin (positive control) showed in vitro cytotoxic activity with IC₅₀ values 3.64, 4.57, 4.89, 3.74, 2.97 and 3.96 µg mL⁻¹, respectively. Bioassay-guided fractionation and isolation of the CAF led to the isolation of five Erythrina alkaloids, identified as erythraline, erysodine, erysotrine, 8-oxoerythraline and 11-methoxyerysodine. These were evaluated for their in vitro cytotoxic activity against Hep-G2 which resulted in IC₅₀ values 17.60, 11.80, 15.80, 3.89 and 11.40 µg mL⁻¹, respectively. Furthermore, in vitro cytotoxic activity against HEP-2 was evaluated, which resulted in IC₅₀ values 15.90, 19.90, 21.60, 18.50 and 11.50 µg mL⁻¹, respectively. The CAF caused a reduction in the viability of mock-infected MT-4 cells with a CC₅₀ of 53 µM and a 50% protection of MT-4 cells against HIV-1 induced cytopathogeneticy with a EC₅₀ of >53 µM, compared with EFV as a positive control, which had a CC₅₀ of 45 µM and an EC₅₀ of 0.003 µM. We concluded that the isolated alkaloids were responsible for the anti-carcinogenic [corrected] actions of the plant extract previously reported in the literature.

Virtual screening of Indonesian herbal database as HIV-1 reverse transcriptase inhibitor

“…Eventhough it is more famous for its bacteriostatic and antiplaque activities, its aglycone was also exhibit antiviral and HIV-1 inhibitor [10, 49], erycristagallin is a pterocarpane from Erythrina genus plants such as Erythrina orientalis [13, 23]. The plant species of Erythrina abyssinica was suggested to have anti-HIV activities [50]. However, no recent research seems to directly relate the plant activities with erycristagallin.…”

In vitro metabolism studies of erythraline, the major spiroalkaloid from Erythrina verna

“…Considering these problems, investigations of cultivars that storage erythrina alkaloids in high amounts are fundamental for a pre-clinical trial and recently it was describe a commercial sample that accumulates high levels of erythraline (Figure 1) [13]. In addition, previous investigation described a weak cytotoxicity for Erythrina alkaloids [14], which suggest also the necessity to confirm the cytotoxicity effects of pure compounds and justify the isolation for all assays.…”

Effect of erythrinaline alkaloids from Erythrina lysistemon on human recombinant caspase-3

“…Under the same conditions, the standard doxorubicin gave the IC 50 values of 3. 64, 4.57, 4.89, 3.74, 2.97 and 3.96 µg/ml respectively, for the same alkaloids (Mohammed et al, 2012). to 3 to activate caspase-3, these compounds may be significant lead compounds as potential therapeutics for the treatment of cancer as inducers of apoptosis in cancer.…”

“…LNCaP, PC-3, Du-145 human prostrate cancer lines) including over expression of caspace-3, has been reported (Liew et al, 2016;Christodoulou et al, 2014;Griffin et al, 2011). Potential anticancer extractives from Erythrina species including flavonoids (Kumar et al, 2013) and erythrinaline alkaloids (Mohammed et al, 2012) have also been reported. It was therefore hypothesized that erythrinaline alkaloids may directly activate human recombinant caspase-3.…”