In vitro anti-HIV and cytotoxic effects of pure compounds isolated from Croton macrostachyus Hochst. Ex Delile
Abstract Croton macrostachyus is an important plant in traditional African medicine, widely utilized to treat a variety of diseases. In Kenya, HIV-infected patients use leaf and root decoctions of the plant as a cure for cough, back pain, bleeding, skin diseases, warts, pneumonia, and wounds. This s...
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| Format: | Article |
| Language: | English |
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BMC
2022-06-01
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| Series: | BMC Complementary Medicine and Therapies |
| Subjects: | |
| Online Access: | https://doi.org/10.1186/s12906-022-03638-6 |
| _version_ | 1818240757784379392 |
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| author | Ermias Mergia Terefe Faith A. Okalebo Solomon Derese Moses K. Langat Eduard Mas-Claret Nada H. Aljarba Saad Alkahtani Gaber El-Saber Batiha Arabinda Ghosh Eman A. El-Masry Joseph Muriuki |
| author_facet | Ermias Mergia Terefe Faith A. Okalebo Solomon Derese Moses K. Langat Eduard Mas-Claret Nada H. Aljarba Saad Alkahtani Gaber El-Saber Batiha Arabinda Ghosh Eman A. El-Masry Joseph Muriuki |
| author_sort | Ermias Mergia Terefe |
| collection | DOAJ |
| description | Abstract Croton macrostachyus is an important plant in traditional African medicine, widely utilized to treat a variety of diseases. In Kenya, HIV-infected patients use leaf and root decoctions of the plant as a cure for cough, back pain, bleeding, skin diseases, warts, pneumonia, and wounds. This study aimed to evaluate the anti-HIV activities and cytotoxic effects of extracts and chemical constituents isolated from C. macrostachyus. In our previous study we demonstrated that the hexane, CH2Cl2, ethyl acetate and methanol soluble fractions of a 1:1 v/v/ CH2Cl2/MeOH crude extracts of the leaves and stem bark of C. macrostachyus exhibited potent anti-HIV activities against HIV-1 with IC50 values ranging from 0.02–8.1 μg/mL and cytotoxicity effects against MT-4 cells ranging from IC50 = 0.58–174 μg/mL. Hence, hexane soluble extract of 1:1 v/v/ CH2Cl2/MeOH crude extract of the leaves of C. macrostachyus, that was more potent against HIV-1 at IC50 = 0.02 μg/mL was subjected to column chromatography leading to the isolation of 2-methoxy benzyl benzoate (1), lupenone (2), lupeol acetate (3), betulin (4), lupeol (5), sitosterol (6) and stigmasterol (7). Lupenone (2), lupeol acetate (3) and betulin (4) exhibited anti-HIV-1 inhibition at IC50 = 4.7 nM, 4.3 and 4.5 μg/mL respectively. The results obtained from this study support the potential of C. macrostachyus, as a source of anti-HIV constituents. |
| first_indexed | 2024-12-12T13:18:31Z |
| format | Article |
| id | doaj.art-b31c6036803340eb85a4300b7b9586ad |
| institution | Directory Open Access Journal |
| issn | 2662-7671 |
| language | English |
| last_indexed | 2024-12-12T13:18:31Z |
| publishDate | 2022-06-01 |
| publisher | BMC |
| record_format | Article |
| series | BMC Complementary Medicine and Therapies |
| spelling | doaj.art-b31c6036803340eb85a4300b7b9586ad2022-12-22T00:23:21ZengBMCBMC Complementary Medicine and Therapies2662-76712022-06-0122111010.1186/s12906-022-03638-6In vitro anti-HIV and cytotoxic effects of pure compounds isolated from Croton macrostachyus Hochst. Ex DelileErmias Mergia Terefe0Faith A. Okalebo1Solomon Derese2Moses K. Langat3Eduard Mas-Claret4Nada H. Aljarba5Saad Alkahtani6Gaber El-Saber Batiha7Arabinda Ghosh8Eman A. El-Masry9Joseph Muriuki10Department of Pharmacology and Pharmacognosy, School of Pharmacy and Health Sciences, United States International University-AfricaDepartment of Pharmacology and Pharmacognosy, College of Health Sciences, University of NairobiDepartment of Chemistry, University of NairobiRoyal Botanic Gardens, Kew, Kew GreenRoyal Botanic Gardens, Kew, Kew GreenDepartment of Biology, College of Science, Princess Nourah bint Abdulrahman UniversityDepartment of Zoology, College of Science, King Saud UniversityDepartment of Pharmacology and Therapeutics, Faculty of Veterinary Medicine, Damanhour UniversityMicrobiology Division, Department of Botany, Gauhati UniversityMicrobiology and Immunology unit, Department of Pathology, College of Medicine, Jouf UniversityCentre for Virus Research, Kenya Medical Research InstituteAbstract Croton macrostachyus is an important plant in traditional African medicine, widely utilized to treat a variety of diseases. In Kenya, HIV-infected patients use leaf and root decoctions of the plant as a cure for cough, back pain, bleeding, skin diseases, warts, pneumonia, and wounds. This study aimed to evaluate the anti-HIV activities and cytotoxic effects of extracts and chemical constituents isolated from C. macrostachyus. In our previous study we demonstrated that the hexane, CH2Cl2, ethyl acetate and methanol soluble fractions of a 1:1 v/v/ CH2Cl2/MeOH crude extracts of the leaves and stem bark of C. macrostachyus exhibited potent anti-HIV activities against HIV-1 with IC50 values ranging from 0.02–8.1 μg/mL and cytotoxicity effects against MT-4 cells ranging from IC50 = 0.58–174 μg/mL. Hence, hexane soluble extract of 1:1 v/v/ CH2Cl2/MeOH crude extract of the leaves of C. macrostachyus, that was more potent against HIV-1 at IC50 = 0.02 μg/mL was subjected to column chromatography leading to the isolation of 2-methoxy benzyl benzoate (1), lupenone (2), lupeol acetate (3), betulin (4), lupeol (5), sitosterol (6) and stigmasterol (7). Lupenone (2), lupeol acetate (3) and betulin (4) exhibited anti-HIV-1 inhibition at IC50 = 4.7 nM, 4.3 and 4.5 μg/mL respectively. The results obtained from this study support the potential of C. macrostachyus, as a source of anti-HIV constituents.https://doi.org/10.1186/s12906-022-03638-6Croton macrostachyusHIV-1Anti-HIVLupenoneLupeol acetateBetulin and cytotoxicity effects |
| spellingShingle | Ermias Mergia Terefe Faith A. Okalebo Solomon Derese Moses K. Langat Eduard Mas-Claret Nada H. Aljarba Saad Alkahtani Gaber El-Saber Batiha Arabinda Ghosh Eman A. El-Masry Joseph Muriuki In vitro anti-HIV and cytotoxic effects of pure compounds isolated from Croton macrostachyus Hochst. Ex Delile BMC Complementary Medicine and Therapies Croton macrostachyus HIV-1 Anti-HIV Lupenone Lupeol acetate Betulin and cytotoxicity effects |
| title | In vitro anti-HIV and cytotoxic effects of pure compounds isolated from Croton macrostachyus Hochst. Ex Delile |
| title_full | In vitro anti-HIV and cytotoxic effects of pure compounds isolated from Croton macrostachyus Hochst. Ex Delile |
| title_fullStr | In vitro anti-HIV and cytotoxic effects of pure compounds isolated from Croton macrostachyus Hochst. Ex Delile |
| title_full_unstemmed | In vitro anti-HIV and cytotoxic effects of pure compounds isolated from Croton macrostachyus Hochst. Ex Delile |
| title_short | In vitro anti-HIV and cytotoxic effects of pure compounds isolated from Croton macrostachyus Hochst. Ex Delile |
| title_sort | in vitro anti hiv and cytotoxic effects of pure compounds isolated from croton macrostachyus hochst ex delile |
| topic | Croton macrostachyus HIV-1 Anti-HIV Lupenone Lupeol acetate Betulin and cytotoxicity effects |
| url | https://doi.org/10.1186/s12906-022-03638-6 |
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