Phytochemical investigation and antidiabetic activity of cissampelos capensis and strychnos henningsii the Eastern Cape medicinal plants
- Authors: Latolla, Nehemiah Solomon
- Date: 2022-04
- Subjects: Medicinal plants -- Eastern Cape (South Africa) , Endemic plants -- South Africa
- Language: English
- Type: Doctoral theses , text
- Identifier: http://hdl.handle.net/10948/56145 , vital:55956
- Description: Diabetes mellitus is recorded as a significant health crisis in South Africa and various medicinal plants are used for the management of diabetes. However, the chemistry and bioactivity associated with these plants' antidiabetic activity are still lacking. Cissampelos capensis L.f. and Strychnos henningsii Gilg are among the plants utilised to manage diabetes in the Eastern Cape Province, South Africa. C. capensis and S. henningsii are known for their isoquinoline – and indole alkaloids, respectively. Other phytochemical groups associated with antidiabetic activity are the phenols, flavonoids, and terpenes. Thus, this study aimed to evaluate in-depth the phytochemical profiling, alkaloidal identification, and structural characterisation of phytochemicals isolated from these plants. Also, subsequent in vitro antidiabetic screening of the crude extracts and isolated compounds from both plants was done. The phytochemical profiling was performed by employing a qualitative and quantitative approach through high-performance thin layer chromatography (HPTLC) and UV-spectrometry. Further analysis for the identification of alkaloids was done by using LCMS. Fractionation and purification of crude extracts were achieved through crystallisation and various chromatographic techniques. NMR, HRMS, UV/Vis, FTIR, and XRD spectroscopic techniques were used to characterise isolated compounds. In vitro antidiabetic activity screening involved the investigation of cytotoxicity, antioxidant activity, alpha-amylase – and/or alpha-glucosidase inhibition (particular to type II diabetes). C. capensis and S. henningsii extracts tested positive for alkaloids, phenolics, flavonoids, and terpenes through HPTLC screening. Quantitative estimation by UV spectrometry of these phytochemical groups detected the highest concentration of alkaloids, followed by flavonoids, phenolics, and terpenes content. The in vitro antidiabetic biological screening of the various crude extracts suggested that the presence of alkaloids, flavonoids, phenolics, and terpenes fostered favourable biological activity. The LCMS of the known alkaloidal constituents from C. capensis detected the presence of ten alkaloids, including glaziovine, lauroscholtzine, pronuciferine and vi salutardine. Seven known alkaloids and one triterpene were detected from S. henningsii, including holtsiine, 23-hdroxyspermostrychnine, henningsiine, and the triterpene, friedelin. These findings suggest that C. capensis and S. henningsii have similar phytochemical constituents compared to the species reported in literature. However, the distribution of the phytochemicals in the various plant parts differed from previous accounts. , Thesis (PhD) -- Faculty of Science,School of Biomecular and Chemical Sciences , 2022
- Full Text:
- Date Issued: 2022-04
- Authors: Latolla, Nehemiah Solomon
- Date: 2022-04
- Subjects: Medicinal plants -- Eastern Cape (South Africa) , Endemic plants -- South Africa
- Language: English
- Type: Doctoral theses , text
- Identifier: http://hdl.handle.net/10948/56145 , vital:55956
- Description: Diabetes mellitus is recorded as a significant health crisis in South Africa and various medicinal plants are used for the management of diabetes. However, the chemistry and bioactivity associated with these plants' antidiabetic activity are still lacking. Cissampelos capensis L.f. and Strychnos henningsii Gilg are among the plants utilised to manage diabetes in the Eastern Cape Province, South Africa. C. capensis and S. henningsii are known for their isoquinoline – and indole alkaloids, respectively. Other phytochemical groups associated with antidiabetic activity are the phenols, flavonoids, and terpenes. Thus, this study aimed to evaluate in-depth the phytochemical profiling, alkaloidal identification, and structural characterisation of phytochemicals isolated from these plants. Also, subsequent in vitro antidiabetic screening of the crude extracts and isolated compounds from both plants was done. The phytochemical profiling was performed by employing a qualitative and quantitative approach through high-performance thin layer chromatography (HPTLC) and UV-spectrometry. Further analysis for the identification of alkaloids was done by using LCMS. Fractionation and purification of crude extracts were achieved through crystallisation and various chromatographic techniques. NMR, HRMS, UV/Vis, FTIR, and XRD spectroscopic techniques were used to characterise isolated compounds. In vitro antidiabetic activity screening involved the investigation of cytotoxicity, antioxidant activity, alpha-amylase – and/or alpha-glucosidase inhibition (particular to type II diabetes). C. capensis and S. henningsii extracts tested positive for alkaloids, phenolics, flavonoids, and terpenes through HPTLC screening. Quantitative estimation by UV spectrometry of these phytochemical groups detected the highest concentration of alkaloids, followed by flavonoids, phenolics, and terpenes content. The in vitro antidiabetic biological screening of the various crude extracts suggested that the presence of alkaloids, flavonoids, phenolics, and terpenes fostered favourable biological activity. The LCMS of the known alkaloidal constituents from C. capensis detected the presence of ten alkaloids, including glaziovine, lauroscholtzine, pronuciferine and vi salutardine. Seven known alkaloids and one triterpene were detected from S. henningsii, including holtsiine, 23-hdroxyspermostrychnine, henningsiine, and the triterpene, friedelin. These findings suggest that C. capensis and S. henningsii have similar phytochemical constituents compared to the species reported in literature. However, the distribution of the phytochemicals in the various plant parts differed from previous accounts. , Thesis (PhD) -- Faculty of Science,School of Biomecular and Chemical Sciences , 2022
- Full Text:
- Date Issued: 2022-04
An investigation of the potential anti-diabetic (insulinomimetic) activity of anti-oxidant compounds derived from Sargassum heterophyllum
- Authors: Nyambe, Mutenta Nsokolo
- Date: 2014
- Subjects: Sargassum , Diabetes -- Chemotherapy , Diabetes -- Africa , Antioxidants -- Therapeutic use , Marine algae , Endemic plants -- South Africa
- Language: English
- Type: Thesis , Masters , MSc
- Identifier: vital:3874 , http://hdl.handle.net/10962/d1021020
- Description: In Africa, non-communicable diseases such as diabetes mellitus have been generally neglected. This problem has worsened over the years owing to continuous threats from infectious diseases such as HIV/AIDS, tuberculosis and malaria. Despite this, statistics have shown that by 2030, the African region will have the highest proportional increase in diabetes prevalence. Over 80% of all diabetic deaths occur in developing countries probably not only due to poor equity of access to medication but also due to limited efficacy and side effects associated with the commonly available anti-diabetic agents. Therefore, this creates the desperate need for the development of new anti-diabetic agents that are more efficacious and can be sourced from within the continent. With oxidative stress as a suggested mechanism underlying the cause of diabetes mellitus and diabetic complications, the discovery of natural anti-oxidants that prevent free radical mediated damage is important for developing new treatment strategies. Marine algae have been identified as good sources for natural anti-oxidants. Unfortunately, very few studies have embarked on the discovery of marine-derived anti-oxidant compounds with potential anti-diabetic activity. In this project, we investigated the potential anti-oxidant activity of the South African endemic algae Stypopodium multipartitum, Dictyopterus ligulata, Cystophora fibriosa, Bifurcariopsis capensis, Sargassum sp. and Sargassum heterophyllum. From these studies, Sargassum heterophyllum yielded prenylated compounds, the main compound being sargahydroquinoic acid (3.6) and the carotenoid metabolite fucoxanthin (3.8), which are in part responsible for the radical scavenging activity of the crude extract. Sargahydroquinoic acid (3.6) and fucoxanthin (3.8) also exhibited significant anti-inflammatory activity. Sargaquinoic acid (3.1), sargachromenoic acid (3.9) and sarganaphthoquinoic acid (3.10) were then semi-synthesized from sargahydroquinoic acid (3.6) and their in-vitro cytotoxicity profiles evaluated using Chang Liver, HT-29, Caco-2 and 3T3-L1 cell lines prior to antidiabetic testing. From the semi-synthetic derivatives, sargachromenoic acid (3.9) exhibited the most potent anti-oxidant activity (IC₅₀ = 6.99 μg/mL). After the evaluation of antidiabetic activity using 3T3-L1 preadipocyte differentiation, sarganaphthoquinoic acid (3.10) showed the most potent insulinomimetic activity at 1.19 μM by inducing a PPARγ response similar to that of rosiglitazone at 1 μM.
- Full Text:
- Date Issued: 2014
- Authors: Nyambe, Mutenta Nsokolo
- Date: 2014
- Subjects: Sargassum , Diabetes -- Chemotherapy , Diabetes -- Africa , Antioxidants -- Therapeutic use , Marine algae , Endemic plants -- South Africa
- Language: English
- Type: Thesis , Masters , MSc
- Identifier: vital:3874 , http://hdl.handle.net/10962/d1021020
- Description: In Africa, non-communicable diseases such as diabetes mellitus have been generally neglected. This problem has worsened over the years owing to continuous threats from infectious diseases such as HIV/AIDS, tuberculosis and malaria. Despite this, statistics have shown that by 2030, the African region will have the highest proportional increase in diabetes prevalence. Over 80% of all diabetic deaths occur in developing countries probably not only due to poor equity of access to medication but also due to limited efficacy and side effects associated with the commonly available anti-diabetic agents. Therefore, this creates the desperate need for the development of new anti-diabetic agents that are more efficacious and can be sourced from within the continent. With oxidative stress as a suggested mechanism underlying the cause of diabetes mellitus and diabetic complications, the discovery of natural anti-oxidants that prevent free radical mediated damage is important for developing new treatment strategies. Marine algae have been identified as good sources for natural anti-oxidants. Unfortunately, very few studies have embarked on the discovery of marine-derived anti-oxidant compounds with potential anti-diabetic activity. In this project, we investigated the potential anti-oxidant activity of the South African endemic algae Stypopodium multipartitum, Dictyopterus ligulata, Cystophora fibriosa, Bifurcariopsis capensis, Sargassum sp. and Sargassum heterophyllum. From these studies, Sargassum heterophyllum yielded prenylated compounds, the main compound being sargahydroquinoic acid (3.6) and the carotenoid metabolite fucoxanthin (3.8), which are in part responsible for the radical scavenging activity of the crude extract. Sargahydroquinoic acid (3.6) and fucoxanthin (3.8) also exhibited significant anti-inflammatory activity. Sargaquinoic acid (3.1), sargachromenoic acid (3.9) and sarganaphthoquinoic acid (3.10) were then semi-synthesized from sargahydroquinoic acid (3.6) and their in-vitro cytotoxicity profiles evaluated using Chang Liver, HT-29, Caco-2 and 3T3-L1 cell lines prior to antidiabetic testing. From the semi-synthetic derivatives, sargachromenoic acid (3.9) exhibited the most potent anti-oxidant activity (IC₅₀ = 6.99 μg/mL). After the evaluation of antidiabetic activity using 3T3-L1 preadipocyte differentiation, sarganaphthoquinoic acid (3.10) showed the most potent insulinomimetic activity at 1.19 μM by inducing a PPARγ response similar to that of rosiglitazone at 1 μM.
- Full Text:
- Date Issued: 2014
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