Content uploaded by Ian Edwin Cock
Author content
All content in this area was uploaded by Ian Edwin Cock on Oct 03, 2014
Content may be subject to copyright.
A preview of the PDF is not available
Metabolomic Profiling of Kigelia africana Extracts with Anti-Cancer Activity by High Resolution Tandem Mass Spectroscopy
Abstract and Figures
Background: Kigelia africana is an African tree with a wide distribution across southern, central and western Africa. It has a history of therapeutic usage by multiple African ethnic groupings which inhabit the areas in which it grows. Amongst these groups there is a myriad of medicinal uses in the treatment of a wide variety of bacterial, fungal and protozoal infections, as well as in the treatment of inflammation and cancers. This study was undertaken to further examine K. africana fruit extracts for the ability to inhibit cancer cell growth, and to use an unbiased metabolomic profiling approach to detect and putatively identify as many individual components as possible, with the aim of developing a database of identified compounds. Materials and Methods: K. africana fruit powder was extracted and tested for inhibitory activity against the Jeg-3 choriocarcinoma cell line using a colorimetric cell proliferation assay. Toxicity was evaluated using an Artemia franciscana nauplii bioassay. Non-targeted HPLC separation of crude extracts coupled to high resolution time-of-flight (TOF) mass spectroscopy with screening against 3 compound databases was used for the identification and characterisation of individual components in crude plant extracts. Results: The methanol, water and ethyl acetate K. africana fruit extracts displayed significant anti-proliferative activity against Jeg-3 choriocarcinoma cells. The methanol and water extracts displayed the strongest anti-proliferative activity, inhibiting Jeg-3 growth to 42% and 46% of the untreated cell growth respectively. The ethyl acetate extract also significantly inhibited Jeg-3 cell proliferation, with decreases to 62% of the untreated control value. Neither the chloroform or hexane extracts had any effect on Jeg-3 cell proliferation. With the exception of the water extract (which displayed moderate toxicity), all extracts were non-toxic or of low toxicity. HPLC-MS/MS TOF analysis identified 356 unique mass signals in the extracts. The putative identities of 227 of these compounds are reported here. Conclusion: This report extends previous studies into the anti-cancer affects of K. africana fruit extracts. The generation of a database of the detected compounds will allow for rapid differentiation of compound profiles between active and less active extracts in future studies. This is expected to assist in the identification of the most important compounds for further separation and bioactivity studies.
Figures - uploaded by Ian Edwin Cock
Author content
All figure content in this area was uploaded by Ian Edwin Cock
Content may be subject to copyright.
... Thus, the aqueous solvent system significantly resulted in higher extraction of polar phytoconsitutents of the plant materials. The current observation was in line with studies by Ref. [59], where aqueous extraction of K. africana fruit produced the highest percentage yield greater than the methanol extract. ...
... These observations are expected since phenols and flavonoids contain significant numbers of hydroxyl groups, giving them more solubility in polar solvents compared to fatty acids, which are generally lipophilic. It is worth mentioning that a number of the compounds identified in this study (such as warfarin alcohol, heneicosane, verminoside, minsecoside, specioside, yohimbine, digoxigenin, eicosane, 5-hydroxymethylfurfural, kigelin and benzoic acid) have been reported and hence strong corroboration between our current findings and those in studies conducted previously [23,59,62]. In contrast, compounds like androstan-3-ol, citronellal, valeric acid octadecyl ester, ethyl iso-allocholate and coumaran identified from this study were reported for the first time in this plant specie. ...
Kigelia africana herbal products are often used traditionally to treat erectile dysfunction and other sexual complaints, but the underlying mechanism is not yet understood. This study focused on profiling the bioactive
constituents of Kigelia africana fruit (KAF) using spectroscopic techniques and providing the computational
models of their interactions with phosphodiesterase (PDE5) and Rho-associated coiled-coil containing protein
kinase 2 (ROCK2) targets associated with erectile dysfunction. Integrated FT-IR, HPLC-MS, and GC-MS analysis
revealed 152 (C1–C152) KAF compounds with highly diverse functional groups and chemical properties. Molecular docking showed several hit compounds as potential inhibitors of PDE5 and ROCK2. Post docking
MMGBSA, QSAR, predictive physicochemical analysis and AdmetSAR analysis revealed that most of the hit
compounds are potential drug leads. Among these, hydroxydoxepin (C3) and ritodrine (C131) exhibited the
strongest interactions with PDE5, while epigallocatechin 3-O-p-coumarate (C9) and chlorogenic acid (C91) had
the strongest interaction with ROCK2. The thermodynamic parameters and trajectory clusters computed from the
trajectories obtained from the 100 ns full atomistic molecular dynamic (MD) simulation indicated the structural
stability and conformational flexibility of the selected complexes. The MD simulation-based MMPBSA calculation
further revealed strong binding affinity and energy contribution by active site residues of PDE5 towards binding
the selected KAF compounds. Various computational analyses employed revealed that the catalytic residues
Gln817, Val782 and Phe786 of PDE5 exhibited high interaction potential and flexibility towards C3 and C131.
Overall, hydroxydoxepin, ritodrine and other phytochemicals in Kigelia africana may account for the therapeutic
role of this plant in erectile dysfunction.
... The tentative compounds identified based fragments pattern as well as the m/z values are presented in supplementary Tables S4-S6. Among the compounds identified tentatively includes verminoside, specioside, 3-o-methylquercetin, minecoside, kigelinone, neamine and fluocinonide which aligns with previous reports (Arkhipov et al., 2014;Costa et al., 2017;Fagbohun et al., 2020aFagbohun et al., , 2020bFagbohun et al., , 2020cFagbohun et al., , 2021. Although, these studies were performed using fruit extracts, the current study focused on other parts of the plant which was shown to contain some phytochemical constituents previously reported in the fruit part. ...
Tumor Necrosis Factor Alpha Converting Enzyme (TACE) mediates inflammatory disorder and contributes to the pathophysiology of a variety of illnesses, such as chronic inflammation and cancer. This study identified metabolites in solvent extracts of Kigelia africana as putative TACE inhibitors due to the plant’s known anti-inflammatory properties. HPLC-MS/GCMS analysis was used to characterize tentative phytochemicals from K. africana. The identified metabolites (n = 123) were docked with TACE to reveal the lead compounds. Binding free energy, ADMET prediction, molecular dynamics simulation at 100 ns, and DFT calculation were further conducted. The results revealed that K. africana contains sterol, phenols, alkaloids, terpenes and flavonoids. The FTIR shows that the extracts had peaks that correspond to the presence of different functional groups. The quantum polarized ligand docking (QPLD) analysis identified compound (n = 3) with binding affinity higher than standard compound IK-682. The hits also had modest ADMET profiles, interacted with essential residues within TACE binding pockets, and formed stable complexes with the protein. The 100 ns MD simulation shows that the compounds formed fairly stable interactions and complex with the protein as evidenced through RMSF, RMSD and MM-GBA results. The HOMO/LUMO, global descriptive molecular electrostatic potential Fukui function aid in the identification of the compounds’ atomic sites prone to electrophilic/neutrophilic attacks, and non-covalent interactions. This study suggests that K. africana’s bioactive compounds are capable of mitigating inflammation by inhibiting TACE.
Communicated by Ramaswamy H. Sarma
... Hussain et al. (2016) employed the agar disc diffusion assay to show the antibacterial capacity of the aqueous, n-hexane and ethanol extracts of K. africana leaf, bark and fruit against a panel of microorganisms (Staphylococcus aureus, Proteus vulgaris, E. coli, Pseudomonas aeruginosa, Klebsiella pneumoniae and Citrobacter amalonaticus), which corroborated the findings of our study. Similarly, the results of the antibacterial potential of K. africana in the current study conforms with an earlier study by Arkhipov et al. (2014) where they investigated the methanol, ethyl acetate and water extracts of the fruit powder against 19 bacterial species. Previous studies (Naidoo, 2006;Mathabe et al., 2006;Mpofu et al., 2014a) on the antimicrobial activity of E. elephantina have been conducted. ...
Foodborne pathogens are a major cause of concern as they are responsible for food spoilage or microbial diseases, leading to economic loss to the food industry as well as health issues. The problem of increased resistance to available antimicrobial agents, and the ability of the microorganisms to form protective biofilms, strengthens their capacity to resist treatment. The antimicrobial, anti-biofilm and antioxidant activities and cytotoxicity of six South African plants, Carpobrotus edulis, Vachellia rehmanniana, Vachellia xanthophloea, Kigelia africana, Elephantorrhiza elephantina and Ochna pretoriensis, were investigated. Plants were selected based on traditional use against foodborne diseases or known antimicrobial activity. Serial microdilution and crystal violet assays were used to assess the antimicrobial and anti-biofilm potential of the extracts. Antioxidant activity of the extracts was determined against free radicals in vitro, and a tetrazolium-based cell viability assay was used to investigate cytotoxicity. Extracts were active against microorganisms implicated in causing foodborne diseases, with minimum inhibitory concentration (MIC) values ranging from 0.02 to 2.5 mg/ml. Acetone extracts of V. xanthophloea and C. edulis had noteworthy MIC values of 0.02 mg/ml against Enterobacter cloacae. Most extracts selectively reduced biofilm growth by at least 50% against the foodborne pathogens. The acetone extract of V. xanthophloea had the most significant anti-biofilm activity against Salmonella Typhimurium. The methanol extract of V. xanthophloea and the acetone extract of C. edulis had good antioxidant activity. Leaf extracts of the selected plants have useful bioactivities coupled with low cytotoxicity, providing impetus for further studies on possible development of these plants as protective food additives against microbial attack or oxidation.
... Hussain et al. (2016) employed the agar disc diffusion assay to show the antibacterial capacity of the aqueous, n-hexane and ethanol extracts of K. africana leaf, bark and fruit against a panel of microorganisms (Staphylococcus aureus, Proteus vulgaris, E. coli, Pseudomonas aeruginosa, Klebsiella pneumoniae and Citrobacter amalonaticus), which corroborated the findings of our study. Similarly, the results of the antibacterial potential of K. africana in the current study conforms with an earlier study by Arkhipov et al. (2014) where they investigated the methanol, ethyl acetate and water extracts of the fruit powder against 19 bacterial species. Previous studies (Naidoo, 2006;Mathabe et al., 2006;Mpofu et al., 2014a) on the antimicrobial activity of E. elephantina have been conducted. ...
Foodborne pathogens are a major cause of concern as they are responsible for food spoilage or microbial diseases, leading to economic loss to the food industry as well as health issues. The problem of increased resistance to available antimicrobial agents, and the ability of the microorganisms to form protective biofilms, strengthens their capacity to resist treatment. The antimicrobial, anti-biofilm and antioxidant activities and cytotoxicity of six South African plants, Carpobrotus edulis, Vachellia rehmanniana, Vachellia xanthophloea, Kigelia africana, Elephantorrhiza elephantina and Ochna pretoriensis, were investigated. Plants were selected based on traditional use against foodborne diseases or known antimicrobial activity. Serial microdilution and crystal violet assays were used to assess the antimicrobial and anti-biofilm potential of the extracts. Antioxidant activity of the extracts was determined against free radicals in vitro, and a tetrazolium-based cell viability assay was used to investigate cytotoxicity. Extracts were active against microorganisms implicated in causing foodborne diseases, with minimum inhibitory concentration (MIC) values ranging from 0.02 to 2.5 mg/ml. Acetone extracts of V. xanthophloea and C. edulis had noteworthy MIC values of 0.02 mg/ml against Enterobacter cloacae. Most extracts selectively reduced biofilm growth by at least 50% against the foodborne pathogens. The acetone extract of V. xanthophloea had the most significant anti-biofilm activity against Salmonella Typhimurium. The methanol extract of V. xanthophloea and the acetone extract of C. edulis had good antioxidant activity. Leaf extracts of the selected plants have useful bioactivities coupled with low cytotoxicity, providing impetus for further studies on possible development of these plants as protective food additives against microbial attack or oxidation.
... Hussain et al. (2016) employed the agar disc diffusion assay to show the antibacterial capacity of the aqueous, n-hexane and ethanol extracts of K. africana leaf, bark and fruit against a panel of microorganisms (Staphylococcus aureus, Proteus vulgaris, E. coli, Pseudomonas aeruginosa, Klebsiella pneumoniae and Citrobacter amalonaticus), which corroborated the findings of our study. Similarly, the results of the antibacterial potential of K. africana in the current study conforms with an earlier study by Arkhipov et al. (2014) where they investigated the methanol, ethyl acetate and water extracts of the fruit powder against 19 bacterial species. Previous studies (Naidoo, 2006;Mathabe et al., 2006;Mpofu et al., 2014a) on the antimicrobial activity of E. elephantina have been conducted. ...
Foodborne pathogens are a major cause of concern as they are responsible for food spoilage or microbial diseases, leading to economic loss to the food industry as well as health issues. The problem of increased resistance to available antimicrobial agents, and the ability of the microorganisms to form protective biofilms, strengthens their capacity to resist treatment. The antimicrobial, anti-biofilm and antioxidant activities and cytotoxicity of six South African plants, Carpobrotus edulis, Vachellia rehmanniana, Vachellia xanthophloea, Kigelia africana, Elephantorrhiza elephantina and Ochna pretoriensis, were investigated. Plants were selected based on traditional use against foodborne diseases or known antimicrobial activity. Serial microdilution and crystal violet assays were used to assess the antimicrobial and anti-biofilm potential of the extracts. Antioxidant activity of the extracts was determined against free radicals in vitro, and a tetrazolium-based cell viability assay was used to investigate cytotoxicity. Extracts were active against microorganisms implicated in causing foodborne diseases, with minimum inhibitory concentration (MIC) values ranging from 0.02 to 2.5 mg/ml. Acetone extracts of V. xanthophloea and C. edulis had noteworthy MIC values of 0.02 mg/ml against Enterobacter cloacae. Most extracts selectively reduced biofilm growth by at least 50% against the foodborne pathogens. The acetone extract of V. xanthophloea had the most significant anti-biofilm activity against Salmonella Typhimurium. The methanol extract of V. xanthophloea and the acetone extract of C. edulis had good antioxidant activity. Leaf extracts of the selected plants have useful bioactivities coupled with low cytotoxicity, providing impetus for further studies on possible development of these plants as protective food additives against microbial attack or oxidation.
... Hussain et al. (2016) employed the agar disc diffusion assay to show the antibacterial capacity of the aqueous, n-hexane and ethanol extracts of K. africana leaf, bark and fruit against a panel of microorganisms (Staphylococcus aureus, Proteus vulgaris, E. coli, Pseudomonas aeruginosa, Klebsiella pneumoniae and Citrobacter amalonaticus), which corroborated the findings of our study. Similarly, the results of the antibacterial potential of K. africana in the current study conforms with an earlier study by Arkhipov et al. (2014) where they investigated the methanol, ethyl acetate and water extracts of the fruit powder against 19 bacterial species. Previous studies (Naidoo, 2006;Mathabe et al., 2006;Mpofu et al., 2014a) on the antimicrobial activity of E. elephantina have been conducted. ...
... The sample for GC-MS analyses was prepared by a simple modified method [11] . The ethyl acetate fraction was mixed in 2 mL each of pyridine and N -methyl-N -(trimethylsilyl)trifluoroacetamide (MSTFA), respectively. ...
The present study profiled various chemical constituents from the ethyl acetate fraction of Kigelia africana fruit extract in a comparative manner using modern chromatographic methods coupled with mass spectrometric techniques. K. africana plant has a wide usage in folklore medicine for numerous ailments with the ethyl acetate fraction having high antifungal and anti-plasmodial activities. Dried fruits were extracted with ethanol and partitioned using ethyl acetate. The fraction was analyzed using GC-MS, GC-TOF-MS and UHPLC-TOF-MS/MS. Fifteen compounds consisting of 2-methoxy-4-vinylphenol, phenol-2,4-bis(1,1-dimethylethyl), - and 9,12,15-octadecatrienoic acid ethyl ester, (Z, Z, Z) – were obtained from GC-MS while 441 metabolites ranging from flavonoids, cardiac glycosides, and polyphenols were profiled from GC-TOF-MS whereas 235 metabolites were fingerprinted from UHPLC-TOF-MS/MS analysis by measuring m/z values and analyzing MS fragmentation pattern. From the identified phytochemicals through ultra-high-pressure liquid chromatography tandem mass spectrometer (UHPLC-TOF-MS/MS), 14 of them were confirmed and these include gemfibrozil, trimetazidine, and leucomalachite green.
... Inhibition of cell growth was dose dependent for both extracts, with the level of inhibitory activity decreasing at lower concentrations. Our findings are in agreement with previous studies which have also reported potent anticancer properties for K. africana extracts against other cell lines [16,17,18]. The half-maximal inhibitory concentrations (IC 50 ) of the two extracts were determined by non-linear regression in Graphpad prism 4 ( Figure 1). ...
... Inhibition of cell growth was dose dependent for both extracts, with the level of inhibitory activity decreasing at lower concentrations. Our findings are in agreement with previous studies which have also reported potent anticancer properties for K. africana extracts against other cell lines [16,17,18]. The half-maximal inhibitory concentrations (IC 50 ) of the two extracts were determined by non-linear regression in Graphpad prism 4 ( Figure 1). ...
Background and objectives: Kigelia africana is a medicinal plant growing naturally in many parts of Africa. In Kenya, a water concoction of the plant is used to treat breast and prostate cancers. Laboratory data on its anti-cancer activity and active principles is limited, hence no scientific rationale for its medicinal use. This study reports on in-vitro toxic activities of dichloromethane and methanol extracts of the plant against human breast cancer cells and phytochemical screening of the two extracts. Methodology: Plant extracts were obtained by sequential solvent extraction of dry plant material (stem bark) using analytical grade dichloromethane: methanol (1:1) and methanol (Sigma Aldrich). In-vitro anti-cancer activities of the extracts were determined using the suphorhodamine (SRB) assay against a human breast cancer cell line (HCC 1937). Preliminary Thin layer chromatography of plant extracts was done using POLYGRAM® SIL G/UV 254 plates (Merck) to establish presence of different classes of secondary metabolites. Results: In-vitro cytotoxic activities of the two extracts were significantly different (P ¼ 0.05). The methanol extract exhibited higher activity (IC 50 ¼ 26.02 μg/ml) compared to that of dichloromethane: methanol (1:1) (IC 50 ¼ 55.01 μg/ml). Phyto-chemical screening of the two extracts revealed the presence of terpenoids, phenols, steroids and flavonoids. Conclusion: The high in-vitro anti-cancer activities of solvent extracts of Kigelia africana justify its use in traditional medicine to manage breast cancer. Phytochemical analysis of the extracts reveal similar profiles hence the differences in their anti-cancer activities can be attributed to quantitative variations of various classes of secondary metabolites.
Foodborne pathogens are a major cause of concern as they are responsible for food spoilage or microbial diseases, leading to economic loss to the food industry as well as health issues. The problem of increased resistance to available antimicrobial agents, and the ability of the microorganisms to form protective biofilms, strengthens their capacity to resist treatment. The antimicrobial, anti-biofilm and antioxidant activities and cytotoxicity of six South African plants, Carpobrotus edulis, Vachellia rehmanniana, Vachellia xanthophloea, Kigelia africana, Elephantorrhiza elephantina and Ochna pretoriensis, were investigated. Plants were selected based on traditional use against foodborne diseases or known antimicrobial activity. Serial microdilution and crystal violet assays were used to assess the antimicrobial and anti-biofilm potential of the extracts. Antioxidant activity of the extracts was determined against free radicals in vitro, and a tetrazolium-based cell viability assay was used to investigate cytotoxicity. Extracts were active against microorganisms implicated in causing foodborne diseases, with minimum inhibitory concentration (MIC) values ranging from 0.02 to 2.5 mg/ml. Acetone extracts of V. xanthophloea and C. edulis had noteworthy MIC values of 0.02 mg/ml against Enterobacter cloacae. Most extracts selectively reduced biofilm growth by at least 50% against the foodborne pathogens. The acetone extract of V. xanthophloea had the most significant anti-biofilm activity against Salmonella Typhimurium. The methanol extract of V. xanthophloea and the acetone extract of C. edulis had good antioxidant activity. Leaf extracts of the selected plants have useful bioactivities coupled with low cytotoxicity, providing impetus for further studies on possible development of these plants as protective food additives against microbial attack or oxidation.
Non-targeted HPLC separation of crude extracts coupled to high resolution time-of-flight (TOF) mass spectroscopy is a powerful tool for the identification and characterisation of individual components in crude plant extracts. This technique allows for metabolite fingerprinting studies between extracts to compare their overall metabolic compositions and identify possible lead compounds. Scaevola spinescens is an endemic Australian plant with a history of therapeutic use by Australian Aborigines as an anti-infective and anti-cancer medicine. The medicinal bioactivities of this plant are poorly studied. S. spinescens extract antiviral activity was examined using an MS2 bacteriophage plaque reduction model system. Toxicity was determined using the Artemia franciscana nauplii bioassay. All extracts displayed antiviral activity in the MS2 plaque reduction assay with methanol, water, ethyl acetate, chloroform and hexane extracts inhibiting 95.2 ± 1.8 %, 72.3 ± 6.3 %, 82.6 ± 4.5 %, 100 ± 0 % and 47.7 ± 12.9 % of plaque formation respectively. All extracts were nontoxic in the A. fransiscana bioassay, indicating their potential as medicines for the control of RNA viruses. HPLC-MS/MS TOF analysis identified several hundred unique mass signals in the extracts. The molecular masses and putative empirical formulas are reported here, allowing for comparison between highly active and less active extracts. Furthermore, the putative identities of several compounds are reported. Through the generation of databases of the detected compounds, this metabolic profiling has allowed for rapid differentiation of compound profiles between active and less active extracts. This is expected to assist in the identification of the most important compounds for further separation and bioactivity studies.
Introduction: Rheumatoid Arthritis (RA) is a chronic inflammatory disorder of the joints which afflicts 0.5 - 1 % of the world’s population, with approximately three times as many women affected as men. The causes of RA are poorly understood although it is generally accepted that it is an autoimmune disorder triggered by microbial infection (particularly by Proteus spp.). Whilst there is currently no known cure for RA, a wide variety of herbal remedies are used in traditional African medicine to treat (RA) and inflammation.
Methods: Thirty four extracts from 13 South African plant species with a history of ethnobotanical usage in the treatment of inflammation were investigated for their ability to control two microbial triggers for RA (P. mirabilis and P. vulgaris). The Artemia nauplii bioassay was used to screen the extracts for toxicity.
Results: Twenty nine of the extracts (85.3 %) inhibited the growth of P. mirabilis and 23 of them tested (67.7 %) inhibited the growth of P. vulgaris. Methanol and water extracts of Carpobrotus edulis, Lippia javanica, Pelargonium viridflorum, Ptaeroxylon obliquum, Syzygium cordatum leaf and bark, Terminalia pruinoides, Terminalia sericea, Warburgia salutaris bark and an aqueous extract of W. salutaris leaf were effective Proteus inhibitors, with MIC values < 2000 µg/ml. The most potent extracts were examined by RP-HPLC and UV-Vis spectroscopy for the presence of resveratrol. Only extracts from T. pruinoides and T. sericea contained resveratrol, indicating it was not responsible for the anti-Proteus properties reported here. All extracts with Proteus inhibitory activity were also either non-toxic, or of low toxicity in the Artemia nauplii bioassay.
Conclusions: The low toxicity of these extracts and their inhibitory bioactivity against Proteus spp. indicate their potential for blocking the onset of rheumatoid arthritis.
Introduction: Petalostigma (known locally as quinine tree), an Australian genus of the Euphorbiaceae family, has a long history of ethnopharmacological usage in the treatment of sore eyes and toothaches, as well as usage as a general antiseptic agent.
Methods: P. pubescens, and P. triloculare solvent extracts were tested for antimicrobial activity, antiviral activity and toxicity in vitro by disc diffusion assays, MS2 bacteriophage plaque reduction assays and Artemia nauplii mortality bioassays respectively.
Results: The methanol, water and ethyl acetate leaf and fruit extracts of P. pubescens, and P. triloculare displayed potent antibacterial activity in the disc diffusion assay. The methanol and ethyl acetate extracts proved to have the broadest specificity, inhibiting the growth of 10 of the 14 bacteria tested (71 %) for the leaf extract and 9 of the 14 bacteria tested (64 %) for the fruit extracts. The water extracts of the leaf and fruit also had broad spectrum antibacterial activity, inhibiting the growth of 8 (57 %) and 7 (50 %) of the 14 bacteria tested respectively. All extracts which displayed antibacterial activity were approximately equally effective against Gram-positive and Gram-negative bacteria, each inhibiting the growth of 50-75% of the Gram-positive and Gram-negative bacteria tested. The methanol, water and ethyl acetate extracts also displayed antiviral activity in the MS2 plaque reduction assay. The methanol and water extracts inhibited 26.6 - 49.0 % and 85.4 - 97.2 % of MS2 plaque formation respectively, with the fruit extracts being more potent inhibitors. All ethyl acetate extracts inhibited 100 % of MS2 plaque formation. All P. pubescens, and P. triloculare extracts were also shown to be non-toxic or of low toxicity in the Artemia fransiscana bioassay. Analysis of these extracts by RP-HPLC showed that the P. triloculare ethyl acetate fruit extract was the least complex of the bioactive extracts. Subsequent analysis of this extract by GC-MS revealed that it contained 9 main compounds: acetic acid; 2,2-dimethoxybutane; 4-methyl-1,3-dioxane; decane; unadecane; 2-furanmethanol; 1,2-benzenediol; 1,2,3-benzenetriol; and benzoic acid.
Conclusions: The lack of toxicity of the P. pubescens, and P. triloculare extracts and their inhibitory bioactivity against bacteria and viruses validate Australian Aboriginal usage of Petalostigma species and indicates its medicinal potential.
Extracts obtained from fruit of Kigelia pinnata (family: Bignoniaceae) are used as folk remedy worldwide for the treatment of various inflammatory ailments and rheumatism. Effects of the methanolic extract of Kigelia pinnata fruit was studied using various in vivo models of inflammation in mice and rats and observed potent inhibiting activity in formaldehyde-induced paw edema, acetic acid-induced vascular permeability, cotton pellet-induced granuloma, estimation of plasma MDA levels and carrageenan induced peritonitis models. MEKP (100, 200 and 400 mg/kg, p.o) exhibited a dose-dependent and significant inhibition (p<0.01) in all the experimental models. The anti-inflammatory activity observed was comparable to the respective standard drugs. Preliminary phytochemical screening revealed the presence of flavonoids, carbohydrates, glycosides, proteins and alkaloids. Acute toxicity studies were performed and produced no mortality in dose up to 2000 mg/ kg, p.o. The results gave a scientific basis to the traditional uses of K.pinnata particularly involved in inflammation.
Kigelia pinnata (Bignoniaceae), colloquially called the Sausage Tree, or Worsboom, on account of its large fruits, has a variety of medicinal uses throughout Africa where it grows as an endemic species in many areas. Chemical examination has resulted in the isolation of iridoids and naphthoquinoids as important secondary metabolites but flavonoids and lignans have also been isolated. Investigation into the biological activity of K. pinnata has focussed on its antibacterial activity and its cytotoxic effects against cancer cell lines. These are related to the traditional uses of bark and fruit extracts for treating diseases caused by micro-organisms and as a remedy for skin cancer. The iridoids and naphthoquinones have been shown to display antibacterial activity and also the ability to inhibit the growth of yeasts. Considerable in vitro cytotoxicity has been demonstrated by extracts of the fruits and barks and the iridoid-related compound norviburtinal and the naphthoquinone isopinnatal have been shown to be two of the compounds responsible. Although little ethnopharmacological evidence exists, the naphthoquinones are active against several protozoal species associated with disease. The compounds also show cytotoxicity against mammalian cell lines. More research is needed to investigate further the reputed effects on the skin of extracts of this plant.
3b, 19a-dihydroxyurs-12-ene-28oic acid, caffeic acid, and chlorgenic were isolated from the fruits and 3b, 19a-hydroxyurs-12-ene-28-oic acid, ferulic acid and p-coumaric acid from the roots of Kigelia pinnata. Key Words: Kigelia pinnata, Bignoniaceae, Triterpenoids, Phenolic acids Nig. J. Nat. Prod. And Med. Vol.1 1997: 40-41