The in vitro and in vivo anti-flammatory properties and cytotoxicity of extracts of Euphorbia hirta

Asthma is considered one of the most common respiratory complaints in the world today but a medical cure for this condition is currently not available. The use of herbal medicines to treat asthma has however been reported and Euphorbia hirtais one such herb. The alkaloids, flavonoids, glycosides, sterols, tannins and triterpenoids in E. hirta appear to exert the anti-asthma effects reported. In the first part of this study, the aqueous, acetone, dichloromethane and hexane extracts of E. hirta were evaluated for their effects on the lysosomal membrane integrity, cell viability and cell number of MRC-5 cell-line using the NR/MTT/CV assay. Hydrocortisone was used as a pharmaceutical control. The differences between the effects of the different extracts were investigated and the effects of the extracts were compared with hydrocortisone. Results obtained showed that hydrocortisone was relatively toxic to the MRC-5 cells whereas all four extracts studied showed very limited cytotoxic effects, with the aqueous extracts generally exhibiting the least effects. In the second part of this study, the effects of the aqueous E. hirta extract on the blood coagulation system and general airway wall microstructure and ultrastructure were investigated using the BALB/c mouse asthma model. Hydrocortisone was also used as a pharmaceutical control. Parameters studied included inflammatory cell population in peripheral blood and their migration into the lung parenchyma; platelet aggregation and fibrin fibre morphology; fibroblast and mucous cell proliferation; alveolar cell numbers, lamellar body formation as well as filopodia formation. The animal weights were continuously being monitored throughout the study. Results from the animal studies showed that the aqueous extract of E. hirta had limited effects on changes in the animal weights and did not cause fragility of blood fibrin fibres nor change the integrity and morphology of the platelets in the mice as seen in those treated with hydrocortisone. E. hirta extracts also significantly reduced the number of active inflammatory cells (especially neutrophils, eosinophils and basophils); restored the histological alterations observed in respiratory structures studied and had diverse, dose-dependent beneficial ultrastructural effects like reduction of smooth muscle hypertrophy, inhibition of macrophages into the airway parenchyma, among others. The final judgment and conclusion of this study was that the aqueous E. hirta extract did not show cytotoxic effects and could be used for the treatment of asthma in the BALB/c mice at doses ranging 25-62.5mg/kg. Further research leading to clinical trials is recommended after testing the potency of equivalent doses of this extract in other animal asthma models.Thesis (PhD)--University of Pretoria, 2008.AnatomyPhDUnrestricte

Reproductive, antioxidant, anti-inflammatory, antimicrobial, protective and antidiabetic activities of Helichrysum Mill. species

South African Helichrysum species are known for diverse medicinal use and treatment of different illnesses. Ethnopharmacological studies have revealed the potential use of Helichrysum plants in drug discovery. Although some of these species have been documented, there is still paucity of information on most species. This review seeks to provide a compilation of documented traditional uses, reproductive potential, antioxidant, anti-inflammatory, antimicrobial, protective and antidiabetic activities and other therapeutic properties of some Helichrysum species of South Africa. Information on Helichrysum cymosum, H. foetidum, H. odoratissimum, H. patulum and H. petiolare were collected from such scientific databases as Google scholar, Scifinder, PubMed, Elsevier, Scopus, Science direct in the form of journal articles, scientific reports, theses and books from the Library of the Cape Peninsula University of Technology. Our findings show that these species have historic values in traditional medicine through their diverse use for the management and treatment of such illnesses as cold, diabetes, headaches, digestive problems, sores and wounds, HIV, cancer etc. Additionally, the reported bioactive constituents isolated from these species have been shown to indicate several activities such as antimicrobial, antioxidant, antidiabetic, neuroprotection, reproductive potentials and others. Thus, the current review highlights the phytochemical and bioactive constituents as well as some of the pharmacological properties of the five selected Helichrysum species with a view to providing validation for their use in the pharmaceutical drug development process

Cytotoxic and cell cycle arrest properties of two steroidal alkaloids isolated from Holarrhena floribunda (G. Don) T. Durand & Schinz leaves

The plant Holarrhena floribunda (H. floribunda; G. Don) is indigenous to sub-Saharan Africa and is traditionally used to treat several ailments. The present study was carried out to isolate and characterize bioactive compounds with anti-proliferative activity present in H. floribunda extracts. Compounds were isolated from H. floribunda using the bioassay-guided fractionation technique of repeated column chromatography and the step-wise application of the MTT reduction assay to assess antiproliferative bioactivity. The structures of the compounds were identified mainly using NMR. The effects of the isolated compounds on the viability, cell cycle and proliferation of human cancer cell lines (MCF-7, HeLa and HT-29) as well as the non-cancerous human fibroblast cell line (KMST-6) were investigated

In vitro evaluation of the antiproliferative activity of Carpobrotus edulis on human neuroblastoma cells

Neuroblastoma is a solid neuroendocrine tumour located outside the cranial cavity and contributes about 15% of all cancer‑associated deaths in children. Treatment of neuroblastoma is quite challenging and involves the use of chemotherapy, surgery and radiotherapy. Despite treatment strategies, systemic toxicity are setbacks to patient well-being, hence the need for a new and affordable approach. Medicinal plants are of importance in the field of drug discovery for cancer as some notable anti-cancer agents have been isolated from them. In the present study, the anti-cancer activity of aqueous extract of Carpobrotus edulis (C. edulis), a ground-creeping edible medicinal plant was investigated in SK-N-BE(2) and SH-SY5Y neuroblastoma cells. The effect of C. edulis on cell viability and survival was determined using MTT (3-[4,5-dimethylthiazol-2-yl] 2,5 diphenyltetrazolium bromide) and clonogenic assays respectively. Apoptosis was determined using a Caspase-9 assay kit and flow cytometry was used to measure intracellular reactive oxygen species (ROS) and depolarization of mitochondrial membrane potential. The results show that C. edulis inhibits cell viability (IC50 of 0.86 mg/ml and 1.45 mg/ml for SK-N-BE (2) and SHSY5Y cells respectively) and colony formation in the neuroblastoma cells as well as induce apoptosis, which is evidenced by an increase in caspase-9 activity in the cells. C. edulis also led to a loss of mitochondrial membrane potential and increased production of ROS. Collectively, these results suggest that C. edulis induces cell death via induction of mitochondrial-mediated apoptosis and accumulation of intracellular ROS, thus providing a rationale for further investigations

Comparative study of the antioxidant constituents, activities and the gc-ms quantification and identification of fatty acids of four selected helichrysum species

Helichrysum Mill. (Asteraceae) is a plant genus comprising distinctively of aromatic plants of about 500–600 species. Since most of these plants have not been previously studied, extensive profiling helps to validate their folkloric uses and determine their potential value as sources of plantderived drug candidates. This study, therefore, aims to investigate the antioxidant activity (DPPH, NO, FRAP); total antioxidant capacity, total phenolic, total flavonoid, and fatty acid compositions of the aqueous acetone extracts from four Helichrysum plants namely, Helichrysum pandurifolium, Helichrysum foetidum, Helichrysum petiolare, and Helichrysum cymocum. The results obtained showed that the H. cymocum extract had the best DPPH radical scavenging activity (IC50 = 11.85 ± 3.20 µg/mL) and H. petiolare extract had the best nitric oxide scavenging activity (IC50 = 20.81 ± 3.73 µg/mL), while H. pandurifolium Schrank extract (0.636 ± 0.005 µg/mL) demonstrated the best ferrous reducing power, all of which are comparable with results from ascorbic acid used as the standard. The IC50 values of the radical scavenging activity ranged from 11.85–41.13 µg/mL (DPPH), 20.81–36.19 µg/mL (NO), and 0.505–0.636 µg/mL (FRAP), for all the plants studied. The H. petiolare has the highest total antioxidant capacity (48.50 ± 1.55 mg/g), highest total phenolic content (54.69 ± 0.23 mg/g), and highest total flavonoid content (56.19 ± 1.01 mg/g) compared with other species

Rutin as a potent antioxidant: implications for neurodegenerative disorders

A wide range of neurodegenerative diseases (NDs), including Alzheimer’s disease, Parkinson’s disease, Huntington’s disease, and prion diseases, share common mechanisms such as neuronal loss, apoptosis, mitochondrial dysfunction, oxidative stress, and inflammation. Intervention strategies using plant-derived bioactive compounds have been offered as a form of treatment for these debilitating conditions, as there are currently no remedies to prevent, reverse, or halt the progression of neuronal loss. Rutin, a glycoside of the flavonoid quercetin, is found in many plants and fruits, especially buckwheat, apricots, cherries, grapes, grapefruit, plums, and oranges. Pharmacological studies have reported the beneficial effects of rutin in many disease conditions, and its therapeutic potential in several models of NDs has created considerable excitement. Here, we have summarized the current knowledge on the neuroprotective mechanisms of rutin in various experimental models of NDs. The mechanisms of action reviewed in this article include reduction of proinflammatory cytokines, improved antioxidant enzyme activities, activation of the mitogen-activated protein kinase cascade, downregulation of mRNA expression of PD-linked and proapoptotic genes, upregulation of the ion transport and antiapoptotic genes, and restoration of the activities of mitochondrial complex enzymes. Taken together, these findings suggest that rutin may be a promising neuroprotective compound for the treatment of NDs

Medicinal properties and in vitro biological activities of selected helichrysum species from South Africa: A review

The genus Helichrysum Mill comprises hundreds of species that are mostly flowering perennial shrubs. Some of these plants that belong to the Helichrysum species are used in traditional medicine to treat cough, back pain, diabetes, asthma, digestive problems, menstrual pain, chest pain, kidney disorders, skin disorders, wounds, open sores, among other conditions, but, only a few scientific studies are reported in the literature with sufficient information that validates the acclaimed folkloric benefits of these plants. This review, therefore, provides a comprehensive update of the available information on the cytotoxicity, genotoxicity, anti-proliferative, anti-bacterial, anti fungal, anti-viral, anti-HIV, anti-malarial, anti-ulcerogenic, anti-tyrosinase, anti-inflammatory, and anti-oxidant activities of selected Helichrysum species of interest: H. petiolare, H. cymocum, H. foetidum, and H. pandurifolium Schrank, using scientific databases as well as electronic and print sources. The ethnobotanical and morphological characteristics as well as the phytochemical composition and biological activities of these plants are elucidated. The scientific rationale for their current use is discussed based on the evidence in the literature

In vitro evaluation of the anti-diabetic potential of aqueous acetone Helichrysum petiolare extract (AAHPE) with molecular docking relevance in diabetes mellitus

Diabetes mellitus (DM) is a chronic metabolic condition that can lead to significant complications and a high fatality rate worldwide. Efforts are ramping up to find and develop novel α-glucosidase and α-amylase inhibitors that are both effective and potentially safe. Traditional methodologies are being replaced with new techniques that are less complicated and less time demanding; yet, both the experimental and computational strategies are viable and complementary in drug discovery and development. As a result, this study was conducted to investigate the in vitro anti-diabetic potential of aqueous acetone Helichrysum petiolare and B.L Burtt extract (AAHPE) using a 2-NBDG, 2-(N-(7-Nitrobenz-2-oxa-1,3-diazol-4-yl) amino)-2-deoxy-D-glucose uptake assay. In addition, we performed molecular docking of the flavonoid constituents identified and quantified by liquid chromatography-mass spectrometry (LC-MS) from AAHPE with the potential to serve as effective and safe α-amylase and α-glucosidase inhibitors, which are important in drug discovery and development. The results showed that AAHPE is a potential inhibitor of both α-amylase and α-glucosidase, with IC50 values of 46.50 ± 6.17 (µg/mL) and 37.81 ± 5.15 (µg/mL), respectively. This is demonstrated by a significant increase in the glucose uptake activity percentage in a concentrationdependent manner compared to the control, with the highest AAHPE concentration of 75 µg/mL of glucose uptake activity being higher than metformin, a standard anti-diabetic drug, in the insulinresistant HepG2 cell line. The molecular docking results displayed that the constituents strongly bind α-amylase and α-glucosidase while achieving better binding affinities that ranged from ∆G = −7.2 to −9.6 kcal/mol (compared with acarbose ∆G = −6.1 kcal/mol) for α-amylase, and ∆G = −7.3 to −9.0 kcal/mol (compared with acarbose ∆G = −6.3 kcal/mol) for α-glucosidase. This study revealed the potential use of the H. petiolare plant extract and its phytochemicals, which could be explored to develop potent and safe α-amylase and α-glucosidase inhibitors to treat postprandial glycemic levels in diabetic patients

Ethnopharmacology, therapeutic properties and nutritional potentials of Carpobrotus edulis: A comprehensive review

Carpobrotus edulis, formerly known as Mesembryanthemum edule L, belongs to the Aizoaceae family of plants. It is a facultative halophytic invasive medicinal and edible succulent plant that is native to South Africa and is distributed worldwide. Hitherto, this plant appears to be mainly known for its ornamental use in decorations, soil stabilization, and erosion control, and not for its many potential medicinal and nutritional benefits, thus suggesting its underutilization. This review presents cogent and comprehensive information on the distribution, ethnomedicinal use, phytochemistry, pharmacology, toxicology, and nutritional value of Carpobrotus edulis and provides the rationale for further pharmacognostic research that will validate its many folkloric medicinal and nutraceutical claims, and promote its standardization into a commercially available product

Comparative Study of the Antioxidant Constituents, Activities and the GC-MS Quantification and Identification of Fatty Acids of Four Selected <i>Helichrysum</i> Species

Helichrysum Mill. (Asteraceae) is a plant genus comprising distinctively of aromatic plants of about 500–600 species. Since most of these plants have not been previously studied, extensive profiling helps to validate their folkloric uses and determine their potential value as sources of plant-derived drug candidates. This study, therefore, aims to investigate the antioxidant activity (DPPH, NO, FRAP); total antioxidant capacity, total phenolic, total flavonoid, and fatty acid compositions of the aqueous acetone extracts from four Helichrysum plants namely, Helichrysum pandurifolium, Helichrysum foetidum, Helichrysum petiolare, and Helichrysum cymocum. The results obtained showed that the H. cymocum extract had the best DPPH radical scavenging activity (IC50 = 11.85 ± 3.20 µg/mL) and H. petiolare extract had the best nitric oxide scavenging activity (IC50 = 20.81 ± 3.73 µg/mL), while H. pandurifolium Schrank extract (0.636 ± 0.005 µg/mL) demonstrated the best ferrous reducing power, all of which are comparable with results from ascorbic acid used as the standard. The IC50 values of the radical scavenging activity ranged from 11.85–41.13 µg/mL (DPPH), 20.81–36.19 µg/mL (NO), and 0.505–0.636 µg/mL (FRAP), for all the plants studied. The H. petiolare has the highest total antioxidant capacity (48.50 ± 1.55 mg/g), highest total phenolic content (54.69 ± 0.23 mg/g), and highest total flavonoid content (56.19 ± 1.01 mg/g) compared with other species. The fatty acid methyl esters were analysed using gas chromatography-mass spectrometry (GC-MS). The results obtained showed variations in the fatty acid composition of the plant extracts, with H. petiolare having the highest saturated fatty acid (SFA) content (7184 µg/g) and polyunsaturated fatty acid (PUFA) content (7005.5 µg/g). In addition, H. foetidum had the highest monounsaturated fatty acid (MUFA) content (1150.3 µg/g), while H. cymocum had the highest PUFA:SFA ratio of 1.202. In conclusion, the findings from this study revealed that H. pandurifolium Schrank, H. foetidum, H. petiolare, and H. cymocum are repositories of natural bioactive compounds with potential health-promoting benefits that need to be investigated, for both their antioxidant activity in a number of disease conditions and for further exploration in drug discovery and development projects