TY - JOUR
T1 - Ethnopharmacological exploration and isolation of HIV-1 latency-reversing agents from Sudanese medicinal plants
AU - Elamin, Khaled M.
AU - Kishimoto, Naoki
AU - Kawahara, Teppei
AU - Idris Elbashir, Sara Mustafa
AU - Yasutake, Tae
AU - Wada, Mikiyo
AU - Hitora, Yuki
AU - Kordofani, Maha
AU - Osman, Wadah
AU - Elbashir, Mustafa Idris
AU - Misumi, Shogo
N1 - Publisher Copyright:
Copyright © 2025 Elamin, Kishimoto, Kawahara, Idris Elbashir, Yasutake, Wada, Hitora, Kordofani, Osman, Elbashir and Misumi.
PY - 2025
Y1 - 2025
N2 - HIV-1 infection remains a major health challenge, especially in resource-limited settings such as Sudan, where traditional medicine is widely practiced for managing infectious diseases, including HIV/AIDS. In this study, we selected ten Sudanese medicinal plants traditionally used to treat immune-related and infectious diseases. The selection was based on ethnobotanical reports and local knowledge of HIV/AIDS-related treatments. Crude extracts were prepared using either absolute methanol or 50% ethanol via maceration, resulting in a total of 20 extracts. The extracts were then screened for HIV-1 latency reversal using a luciferase reporter assay in TZM-bl cells. The 50% ethanolic extract of G. kraussiana showed the highest LTR activation (EC50 = 3.75 μg/mL) with no significant cytotoxicity observed. Bioactivity-guided fractionation of the Gnidia kraussiana extract led to the isolation of gnidilatidin, a daphnane-type diterpenoid, using ultrahigh-performance liquid chromatography coupled with high-resolution mass spectrometry (UHPLC-HRMS). Gnidilatidin demonstrated potent latency-reversing activity (EC50 = 5.49 nM in J-Lat 10.6 cells) and downregulated CD4 and CXCR4, suggesting enhanced inhibition of HIV-1 entry. This study supports the ethnopharmacological relevance of G. kraussiana and validates its traditional use. It also identifies gnidilatidin as a promising lead compound for HIV-1 latency-reversal-based strategies. Further studies are needed to optimize its pharmacological profile and further elucidate its therapeutic potential, particularly as part of an optimized combination regimen with combination antiretroviral therapy (cART).
AB - HIV-1 infection remains a major health challenge, especially in resource-limited settings such as Sudan, where traditional medicine is widely practiced for managing infectious diseases, including HIV/AIDS. In this study, we selected ten Sudanese medicinal plants traditionally used to treat immune-related and infectious diseases. The selection was based on ethnobotanical reports and local knowledge of HIV/AIDS-related treatments. Crude extracts were prepared using either absolute methanol or 50% ethanol via maceration, resulting in a total of 20 extracts. The extracts were then screened for HIV-1 latency reversal using a luciferase reporter assay in TZM-bl cells. The 50% ethanolic extract of G. kraussiana showed the highest LTR activation (EC50 = 3.75 μg/mL) with no significant cytotoxicity observed. Bioactivity-guided fractionation of the Gnidia kraussiana extract led to the isolation of gnidilatidin, a daphnane-type diterpenoid, using ultrahigh-performance liquid chromatography coupled with high-resolution mass spectrometry (UHPLC-HRMS). Gnidilatidin demonstrated potent latency-reversing activity (EC50 = 5.49 nM in J-Lat 10.6 cells) and downregulated CD4 and CXCR4, suggesting enhanced inhibition of HIV-1 entry. This study supports the ethnopharmacological relevance of G. kraussiana and validates its traditional use. It also identifies gnidilatidin as a promising lead compound for HIV-1 latency-reversal-based strategies. Further studies are needed to optimize its pharmacological profile and further elucidate its therapeutic potential, particularly as part of an optimized combination regimen with combination antiretroviral therapy (cART).
KW - anti-HIV drugs
KW - HIV-1/AIDS
KW - latency-reversing agents
KW - Sudanese medicinal plants
KW - Sudanese traditional healers
UR - https://www.scopus.com/pages/publications/105013775940
U2 - 10.3389/fphar.2025.1587128
DO - 10.3389/fphar.2025.1587128
M3 - Article
AN - SCOPUS:105013775940
SN - 1663-9812
VL - 16
JO - Frontiers in Pharmacology
JF - Frontiers in Pharmacology
M1 - 1587128
ER -