Anti-sickling Potential Research Articles

Anti-sickling effect of Vigna subterranean (L.) Verdc on sickle cell beta thalassemia

Sickle cell disease affects millions of people worldwide and has been recognized as a global health concern by WHO. Presently, there is no cure for sickle cell disease. Treatment options which include bone marrow, stem cell transplantation, blood transfusions, and hydroxyurea are not only expensive but have their side effects. Medicinal plants are often employed in the treatment of diseases because of the therapeutic effects of the secondary metabolites in them. Vigna subterranean an important leguminous crop in Africa, is used in some parts of the world for the treatment and management of sickle cell disease. However, there are no established link between the use of Vigna subterranean and their pharmacological effects. The present study investigated the therapeutic effect of Vigna subterranean on a variant of sickle cell disease known as sickle cell beta thalassemia. Parameters such as reversibility test, polymerization test, osmotic fragility test, deoxygenation test, beta synthesis and oxy-haemoglobin concentration were used to study the anti-sickling potentials of sickle cell beta thalassemia. The result showed that the plant extract reversed the sickled cells, reduced the rate of polymerization, maintained the stability of the cell membrane, increased beta globin synthesis and increased the oxy-haemoglobin concentration. This suggests that Vigna subterranean possesses anti-sicking properties and could be used as an effective therapeutic for the treatment and management of sickle cell beta thalassemia.

Phytochemistry, Mineral Estimation, Nutritional, and the In Vitro Anti-Sickling Potentials of Oil Extracted from the Seeds of Mucuna Flagellipes

Abstract. Sickle cell disease is an inherited blood disorder indicative of red blood cells becoming sickle-shaped. The study investigated the in vitro anti-sickling potentials of the seed oil of M. flagellipes. The phytochemistry (fatty acids, vitamins, and minerals) was also determined using standard protocols. Finally, nutritional calculations on the oil were performed to determine its suitability for nutritional purposes. The result showed high zinc content (780 ± 2.50 µg/ 100 mg), while low iron content was observed (170 ± 1.30 µg/ 100 mg). Vitamin analysis showed the presence of vitamins A, E and K with values of 220 ± 1.60, 370 ± 2.20, and 197 ± 0.23 µg/100 mg respectively. The fatty acid profile revealed oleic (31.87 %) and linoleic (18.30 %) fatty acids as the major unsaturated fat in the oil, while palmitic fatty acid (5.91 %) was the major saturated fatty acid. Nutritional calculations showed high PUFA/SFA (2.07), MUFA/SFA (3.62), and UI (68.47). However, the index of thrombogenicity (0.07) and atherogenicity (0.11) was low in the seed oil. Finally, the in vitro anti-sickling potentials of the seed oil showed the oil inhibited and reversed sickling in a dose-dependent manner. Hbs polymerization was also inhibited and Fe2+/Fe3+ was upregulated following treatment with the seed oil. Collectively, the oil showed good anti-sickling potentials, which can be labelled to the presence of zinc, vitamins and unsaturated fat. The nutritional calculations suggest that the seed oil is cardio-friendly and does not pose any nutritional threat.

Effect of Hibiscus Sabdariffa Calyx Extract on Derived Haematologic Indices in Sickle Cell Anaemia In-vitro

We hypothesised that the calyx extract of Hibiscus sabdariffa (HS) may have antisickling potential on account of its calcium antagonistic and antioxidants effects. Five ml of blood was collected from sickle cell anaemia (SCA) patients (n=11). 50µL ofblood was incubated with 50µL each of 0.l, 1 and 10mg/ml of HS before adding 50µL of 2% sodium metabisulphite (Na2S2O5) (protective assay). Also, 50µL Na2S2O5 was added to 50µL of blood and then incubated with 50µL each of 0.l, 1 and 10mg/ml of HS (reversal assay). In parallel, 50µL of blood each was incubated with 50µL of 5 mg/ml hydroxyurea and 50µL of 0.9% NaCl (control) respectively. The mean cell haemoglobin concentration (MCHC), mean cell volume (MCV) and mean platelet volume (MPV) were determined. In both the protective and reversal assays, a significant (p<0.01 and p<0.05 respectively) decrease in MCHC was observed in the presence of HS. However, there was a significant (P<0.05) increase in MCV in the presence of HS in the reversal assay only. In the protective and reversal assays the MPV increased significantly (P<0.05 and P<0.01 respectively) in the presence of HS. These parameters showed no significant change in the presence of hydroxyurea. These results suggest that in the reversal assay HS may have antisickling properties by lowering the MCHC and increasing MCV and thereby reducing haemoglobin S concentration and polymerization. This further suggests that HS may have a Gardos channel inhibitory effect. However, the increase in MPV suggests that HS may be toxic at these concentrations

Mitapivat increases ATP and decreases oxidative stress and erythrocyte mitochondria retention in a SCD mouse model

Polymerization of deoxygenated sickle hemoglobin (HbS) leads to erythrocyte sickling. Enhancing activity of the erythrocyte glycolytic pathway has anti-sickling potential as this reduces 2,3-diphosphoglycerate (2,3-DPG) and increases ATP, factors that decrease HbS polymerization and improve erythrocyte membrane integrity. These factors can be modulated by mitapivat, which activates erythrocyte pyruvate kinase (PKR) and improves sickling kinetics in SCD patients. We investigated mechanisms by which mitapivat may impact SCD by examining its effects in the Townes SCD mouse model. Control (HbAA) and sickle (HbSS) mice were treated with mitapivat or vehicle. Surprisingly, HbSS had higher PKR protein, higher ATP, and lower 2,3-DPG levels, compared to HbAA mice, in contrast with humans with SCD, in whom 2,3-DPG is elevated compared to healthy subjects. Despite our inability to investigate 2,3-DPG-mediated sickling and hemoglobin effects, mitapivat yielded potential benefits in HbSS mice. Mitapivat further increased ATP without significantly changing 2,3-DPG or hemoglobin levels, and decreased levels of leukocytosis, erythrocyte oxidative stress, and the percentage of erythrocytes that retained mitochondria in HbSS mice. These data suggest that, even though Townes HbSS mice have increased PKR activity, further activation of PKR with mitapivat yields potentially beneficial effects that are independent of changes in sickling or hemoglobin levels.

Anti sickling potential and chemical profiling of traditionally used Woodfordia fruticosa (L.) Kurz leaves

Woodfordia fruticosa (L.) Kurz is a widely used plant in traditional medicine systems. The tribal communities of Amarkantak, Madhya Pradesh (India) are using this plant for the treatment of general weakness, blood related complications like blood deficiency, blood purification and for the treatment of symptoms related to sickle cell disease (SCD). SCD is a genetic disease with life threatening complications. In the absence of any drugs without any side effects, the alternative plant based therapies that may either reduce/ reverse the sickling of the red blood cells can be safe and effective therapeutic agents. We evaluated W. fruticosa extracts for phytoconstituents, anti-oxidant and anti-inflammatory properties. Anti-sickling properties of the extracts were evaluated by estimation of reverse sickling, polymerization inhibition and osmotic fragility assays. Chemical profiling of the methanol extract was done using LC-MS analysis. Phytochemicals such as alkaloids, steroids, tannin, and saponins were present in all the extracts. Methanol extract displayed maximum reversal (66 ± 1%) of sickled Red blood Cells (RBC) and significantly inhibited Hb polymerization. The hexane and methanol extracts led to minimum hemolysis of sickled RBC in the osmotic fragility assays. Total tannin (365 ± 2.4 TAE) content was highest in acetone extract, while the total flavonoid and phenolic content (156.9 ± 2.0 QE) and (113.7 ± 0.7 GAE) were highest in methanol extract. The methanol extract displayed minimum IC 50 (8.1 ± 1.5) in 2, 2-diphenylpicrylhydrazyl (DPPH) while the acetone extract had minimum IC 50 (215.8 ± 5.7) in 2,2′-azino-bis 3-ethylbenzothiazoline-6-sulfonic acid (ABTS) assay. The hexane extract displayed maximum Ferric reducing anti-oxidant power (FRAP) value (1.5 ± 0.5 mM Fe(II)/mg dry weight) that were higher than methanol and aqueous extracts (1.45 ± 0.1, 1.45 ± 0.05 mM Fe(II)/mg dry weight). The methanol extract provided maximum RBC protection from hemolysis (73.8 ± 0.8%). Maximum Lipoxygenase (LOX) inhibition was observed by the acetone and methanol extracts at 400 μg/mL while the hexane extract displayed maximum Xanthine oxidase (XO) inhibition (57.0 ± 0.5%). LC-MS profiling of the methanol extract identified several secondary metabolites that might be responsible for the observed activities. The results validate the traditional use of W. fruticosa and present us with potential compounds for further development of novel anti sickling agents.

Human Hemoglobin S Erythrocyte-Stabilizing and Antisickling Potential of Extract of Wood Ear Mushroom, Auricularia auricula (Agaricomycetes).

The increased prevalence and mortality of sickle cell disease necessitates more research on its management and treatment. This study investigated the antisickling potential of Auricularia auricula obtained from its natural environment within the University of Port Harcourt in Nigeria. Freshly harvested mushrooms were washed, air-dried, and ground and distilled water was added. The mixture was divided into two parts; one part was extracted by cold maceration and lyophilized to give cold maceration extract, while the filtrate obtained after boiling and cooling of the second part was dried in an autodesiccator to give decoction extract. Volumes of both extracts were obtained via serial dilution. Sickle cell hemoglobin S (HbS) erythrocytes were obtained by centrifuging HbS-blood in 0.9% physiological saline. The percentage of lysis decreased when 10 and 5 mg/mL of both extracts were added to erythrocytes suspended in hypotonic buffered saline, while the lowest median corpuscular fragility was observed for cold maceration extract at 5 mg/mL. The lowest negative percentage of stability and highest morphological stability were observed for decoction extract at 10 and 5 mg/mL after 5 min of culturing in decoction extract, respectively. The ability of A. auricula extracts (mainly the decoction extract) to reverse and stabilize erythrocyte membrane integrity and morphology is a clear indication that this mushroom may offer a valuable natural option for the treatment and management of sickle cell anemia.

Comparative evaluation of proximate composition and anti-sickling potential of Annona muricata Linn seeds and leaves

Background: Annona muricata Linn is a notable, well-studied plant of therapeutic value. Based on the abundant pharmacological constituents contained in the understudied plant, it is imperative that the plant parts are investigated for nutritional value and anti-sickling potentials. Sickle cell anaemia (SCA) is an inheritable haematological disorder, caused by an amino acid substitution on the haem protein. The outcomes for SCA are poor health indices and high mortality. Therefore, the use of natural products is necessary and widely promoted in countries with poor health infrastructure. Methods: In this study, A. muricata seeds and leaves were comparatively analysed for the proximate compositions. In addition, aqueous and ethanol extracts of A. muricata seeds and leaves were respectively analysed for anti-sickling potentials with the use of spectrophotometry. Results: Proximate composition of A. muricata seeds and leaves showed that both plant parts contain ash, carbohydrate, fat, fibre, moisture and protein. However, percentage proximate composition of A. muricata seeds was not significantly different from the percentage proximate composition of A. muricata leaves (p ≤ 0.05). From anti-sickling analysis, the aqueous extracts of A. muricata seeds and leaves were observed to inhibit HbSS polymerisation, while the ethanol extracts of A. muricata seeds and leaves showed limitations to the inhibition of HbSS polymerisation. Conclusion: A. muricata seeds and leaves possess potentials as health or nutritional supplements for the management of SCA. Further studies are necessary in order to ascertain efficacy and safety in in vivo models

Sickle hemoglobin polymerization and antisickling medicinal plants

Sickle cell disease (SCD) is a dilapidating disorder that is associated with organ destruction and decreased life expectancy. Therapeutic remedies that lead to fundamental cure of SCD such as, bone marrow and stem cell transplantations, as well as gene replacement therapy, are very costly and unaffordable to the disease sufferers in developing countries. In regions where these therapeutic approaches are possible, there are also limitations such as immunologic transplant rejection, difficulty in prognosis, difficulty in obtaining a suitable donor, end-organ dysfunction, and adverse health effects, especially among the older sufferers of this disease. The eagerness of researchers to develop new drugs for the amelioration of the crisis associated with SCD and a possible cure of the disease has led to the discovery of biomolecular agents that inhibit the mechanisms of HbS polymerization as well as medicinal plants with antisickling potentials. The antisickling potency of medicinal plants should be harnessed through research funding and efforts geared towards the discovery of molecules in such plants with HbS polymerization inhibitory effects.

Anti-sickling activities of two isolated compounds from the root of Combretum racemosum P. beauv. (Combretaceae)

Ethnopharmacological relevanceEvaluation of plants such as Combretum racemosum with claimed traditional use in the management of sickle cell anaemia in Nigeria and other parts of West Africa could serve as a useful research strategy in the search for potential anti-sickling drugs and templates.Aim of the study: This study aimed at evaluating the antisickling potential of C. racemosum by activity-guided purification and isolation of its active constituents. Materials and methodsCrude methanol extract of the root of C. racemosum and the fractions obtained by partitioning with chloroform, ethyl acetate, and aqueous were investigated for anti-sickling activity against sodium metabisulphite induced sickling of sickle cell haemoglobin (HbSS). Repeated chromatographic separations were conducted on the most active chloroform fraction to purify and isolate bioactive compounds for further tests for anti-sickling activity. The characterization of the isolated compounds was done by mass spectrometry (FD+MS) and nuclear magnetic resonance (1HNMR) spectroscopy. ResultsThe chloroform fraction (FA) (% sickled erythrocyte ranged from 3.0 to 34.1) exhibited better anti-sickling activity than aqueous (% sickled erythrocyte ranged from 38.9 to 51.5) as well as the crude methanol (% sickled erythrocyte ranged from 19.1 to 30.4). Hence, the phytochemical investigation was focused on the chloroform fraction, which led to the identification of two ellagic acid derivatives (3,3′,4′-tri-O-methyl ellagic acid (A) and 3,3′-di-O- methyl ellagic acid (B). The two isolated compounds possessed good, comparable anti-sickling activities with compound A exhibiting a slightly better in vitro activity. ConclusionThis paper reports for the first time anti-sickling principles from C. racemosum and therefore, provided some justification for the ethnomedicinal use of the plant in the management of sickle cell disease.

In vitro investigation of the antisickling properties of aqueous fruits extracts of Citrus paradisi, Musa acuminata and Malus domestica

Sickle cell disease (SCD) is a genetic blood disorder that affects the shape and transportation of red blood cells (RBCs) in blood vessels, leading to various clinical complications. Many drugs that are available for treating the disease are insufficiently effective, toxic, or too expensive. Therefore, there is a pressing need for safe, effective, and inexpensive therapeutic agents from indigenous plants used in ethnomedicine. In the current study, the potentials of aqueous extracts of Citrus paradisi, Musa acuminata, Malusdomestica fruit in sickle cell disease management were investigated in vitro using P-hydroxybenzoic acid and normal saline as positive and negative control respectively. The method employed the inhibition of sodium metabisulphite induced sickling of HbSS red blood cells, collected from confirmed sickle cell patients. Results obtained showed that; 50 mg/ml aqueous extract of Musa acuminata showed the lowest sickling inhibition (80.3%) at 60 minutes while 1 mg/ml gave the highest inhibition of 97.3% at 90 minutes. For Citrus paradisi, lowest (83.3%) and highest (98%) sickling inhibitions were obtained with 25 mg/ml and 50 mg/ml fruit extracts at 30 minutes and 60 minutes respectively. Malus domestica had the highest antisickling activities of 99% and 99.33% respectively at 30 and 60 minutes. In all, the sickling inhibition was least with Musa acuminata but highest with Malus domestica. Also, highest inhibitions were observed at 60 minutes (optimum time) and 10 mg/ml (optimum concentration). This study has demonstrated that; Malus domestica, Citrus paradisi and Musa acuminata possess antisickling potentials useful in the management or therapy of sickle cell diseases.

Antisickling potential of compounds derived from Detarium microcarpum (Fabaceae): in vitro and in silico studies

Detarium microcarpum is a legume tree of tropical Africa, widely known for its ethno-medicinal potentials. Previous studies have reported its rich contents of phytochemicals which could be linked to the bioactive principle of the plant. The in vitro antisickling properties of D. microcarpum stem bark was evaluated using blood samples obtained from thirty-five confirmed sickle cell disease patients using standard microscopic techniques. The research outcome showed that D. microcarpum extract inhibited sickling of red blood cells with a laudable mean difference compared to p-hydrozybenzoic acid (reference antisickling drug) which is a pure compound. To further expounds it’s mechanism of action, six compounds previously isolated from D. microcarpum stem bark and fruits was docked into the active sites of deoxy-hemoglobin (PDB ID: IGZX) and 2, 3-bisphosphoglycerate mutase (PDB ID: 1T8P) using Autodock Vina algorithm. Results from the in silico studies showed that oxokolavenic acid, 5α, 8α -2-oxokalavenic acid and Copalic acid exhibited the most favorable ligand–protein molecular interaction with deoxy-hemoglobin and 2,3-bisphosphoglycerate mutase when compared with the reference antisickling drug, hydroxyurea. The interaction of these compounds with deoxy-hemoglobin could alter hemoglobin conformation, favoring the relaxed state, thereby delaying/inhibiting hemoglobin polymerization and sickling. Their interactions with 2, 3-bisphosphoglycerate mutase could inhibit 2, 3-bisphosphoglycerate synthesis, thus delaying enhanced delivery of oxygen to tissues which is twice the case seen in sickle cell anemia. This clearly shows the possible mechanism of action of D. microcarpum and further substantiates the antisickling potential of these compounds derived from D. microcarpum leaves and fruits.

Bioactivity-directed isolation of antisickling compounds from Cnidoscolus acontifolius (Mill.) I.M. Johnst leaf extract

Context: There is continuous search for therapeutic agents from indigenous plants that can be employed in the treatment of sickle cell anemia. Aims: To evaluate the antisickling potential of Cnidoscolus aconitifolius leaf extract, determine the most active fraction, and isolate the putative compounds. Methods: Oven dried leaves of C. aconitifolius (CA) were extracted by maceration in ethanol for 72 h. The extract was fractionated into n-hexane, dichloromethane, ethyl acetate and methanol using vacuum liquid chromatography (VLC). The crude CA extract and fractions were subjected to inhibitory and reversal antisickling assays at 0.25-4.00 mg/mL concentration range. Bioactivity-directed fractionation of the most active fraction was done on repeated silica gel column chromatography, followed by preparative thin-layer chromatography, and their analyses on thin-layer chromatography. The isolated compounds were characterized using spectroscopic methods of 1H- and 13C- Nuclear Magnetic Resonance, COSY, HMBC, HSQC, and LC-MS. Results: The results showed that CA had 80.4 ± 0.15% inhibitory and 56.0 ± 2.90% reversal effects at 4 mg/mL. The ethyl acetate fraction gave significantly higher (p<0.05) inhibitory (68.0 ± 4.32%) and reversal (61.4 ± 6.2%) activities at 4 mg/mL than the other VLC fractions. The positive control Ciklavit® had 59.8 ± 0.3% inhibitory and 56.6 ± 0.2% reversal properties. Two compounds, T1 and T2 were isolated from the ethyl acetate fraction and identified as tetramethyl bicosahydropicen-3-ol and 5β-pregnane, respectively. Compound T1 demonstrated an inhibitory effect of 83.6 ± 0.11%. Conclusions: The study concluded that the ethyl acetate fraction of the ethanol extract of C. aconitifolius has the highest antisickling property and identified tetramethylbicosahydropicen-3-ol as a potential antisickling agent.

In-vitro anti-sickling and membrane stability potentials of Mishenland polyherbal extract on sickle red blood cells

Background Sickle cell disease is a genetic disorder that causes stiff, rod-like sickle-shaped hemoglobin in red blood cells (RBCs) and consequently poses serious health complications. Aim We investigated an in-vitro anti-sickling potential of a novel Mishenland polyherbal formula (MPF) for possible ameliorative effects. Materials and methods Sickling of RBCs induced with 2% sodium metabisulfite was followed by treatment with MPF mixtures in different saline concentrations (7, 9, 14, and 28 mg/ml). The red cell morphology was examined microscopically. Percentage sickling was assessed at 30 min intervals at 37°C for 2 h. The effect of the MPF on membrane stability of RBCs was analyzed using osmotic fragility testing. Results Qualitative phytochemical screening demonstrated the presence of some secondary metabolites namely alkaloids, glycosides, phenols, saponin, tannin, and terpenoids. Sickling of RBCs induced with metabisulfite was inhibited by MPF. This anti-sickling effect was directly proportional to the concentration of the MPF, dose dependently. There was a significant difference (P Conclusion MPF demonstrated significant anti-sickling and erythrocyte membrane stability properties. These effects under hypoxia signified a promising effect of the bioactive components as probable drug candidates against sickling of red cells.

Stabilizing Ability and Anti-sickling Potentials of Ganoderma Lucidum Decoction Extract on Human HbS Erythrocytes Membrane

Stabilizing Ability and Anti-sickling Potentials of Ganoderma Lucidum Decoction Extract on Human HbS Erythrocytes Membrane

Hydroxyurea in the management of sickle cell disease: pharmacogenomics and enzymatic metabolism.

Hydroxyurea (HU) was approved to be used in the treatment of sickle cell disease (SCD) because of its anti-sickling potential. However, there is variability in HU response among SCD patients and this can be due to physiological, socioeconomic, environmental, metabolic and/or genetic factors. The present review focuses on the latter two. Three quantitative trait loci, HBG2, BCL11A and HMIP, have been suggested as important markers for HU response. Other genes (ASS1, KLF10, HAO2, MAP3K5, PDE7B, TOX, NOS1, NOS2A, FLT1, ARG1, ARG2, UGT1A1, OR51B5/6, SIN3A, SALL2, SAR1A, UTB, OCTN1, CYP2C9, AQP9, MPO, CYP2E1, and GSTT1) have also been considered. Studies implicate catalase, urease, horseradish peroxidase and enzymes of CYP450 family in HU metabolism. However, little is known about these enzymes. Therefore, further studies are needed to elucidate the metabolic pathway of HU, which will facilitate pharmacogenomic studies and help in identification of candidate genes for predicting HU response.

Evaluation of Some Salicylaldehyde-derived Baylis-Hillman Adducts and Coumarin Derivatives as Potential Antisickling Compounds

Abstract Some salicylaldehyde-derived Baylis-Hillman adducts and 3-(chloromethyl)coumarins have been synthesised and evaluated in vitro for their antisickling activities. The compounds were screened for inhibitory and reversal activity against mutated haemoglobin (HbSS) in red blood cells at four different concentrations (4 mg/mL, 2 mg/mL, 1 mg/mL and 0.5 mg/mL) as a measure of their antisickling potentials. Among the synthesized compounds, 6-chloro-3-(chloromethyl)coumarin 4d showed the highest inhibitory activity (83.75±1.90%), followed by 6-chlorocoumarin-3-methylsulfinic acid 5d (80.90 ±0.91%) and the least was tert-butyl-3-hydroxy- 3-(2-hydroxyphenyl)-2-methylenepropanoate 3a (33.33±1.86%). The results obtained from the reversal antisickling experiment showed that the percentage of sickle cells able to revert to the normal biconcave shape was dose dependent. Compound 5d had the highest reversal activity (66.49±1.39%) followed by 6-bromo-3- (chloromethyl)coumarin 4c (59.66±2.95) and 4d (55.50±1.95%) at 4 mg/mL. Compound 4c had higher reversal activity than the standard p-hydroxybenzoic acid at 2 mg/mL, 1 mg/mL and at 0.5 mg/mL. The 3-substituted coumarins 4a-d, and 5d had higher inhibitory antisickling activities than their Baylis-Hillman precursors 3a-d. Effect of 4a-d and 5d on the rate of polymerization of sickle cell heamoglobin was further studied spectrophotomerically using hemolysate of HbSS. The considerable inhibitory and reversal activities of these compounds make them good candidates for further antisickling studies.

Monodora myristica (African nutmeg) modulates redox homeostasis and alters functional chemistry in sickled erythrocytes.

The antioxidative effect of Monodora myristica seed acetone extract and its effect on chemical functional groups were investigated in sickled erythrocytes as well as molecular modeling of the antisickling potentials of its secondary metabolites. The extract was subjected to gas chromatography-mass spectrometry to identify the compounds present, which were then docked into the allosteric-binding site of deoxy-hemoglobin. The extract was incubated with sickled erythrocytes at 37°C for 6, 12, and 24 h and were subjected to antioxidative analysis for reduced glutathione (GSH), superoxide dismutase (SOD), catalase, and lipid peroxidation (LPO). Chemical functional group of the treated cells was analyzed via Fourier transform infrared spectroscopy (FTIR). The predominant compounds identified were 17-octadecynoic acid; oleic acid, androstan-3-one, 17-hydroxy-2-methyl- (2.beta.,5.beta.,17.beta.)-; estran-3-one, 17-(acetyloxy)-2-methyl-, (2.alpha., 5.alpha., 17.beta.), and (+)-3-carene, 10-(acetylmethyl)-. They all fitted well within the active site of Hb with good binding affinity, as evidenced by the negative CDocker interaction energies of their complexes ranging between -54.4 and -26.7 kcal/mol. Treatment with the extract exacerbated SOD and catalase activities as well as GSH level, while LPO was suppressed. This antioxidative activity was time and/or dose dependent, with 6 and 12 h incubation showing the optimum activity. FTIR analysis of the treated cells showed the presence of hydrophobic functional groups. The synergetic molecular interaction of the major compounds of the extract with the α-dimer of Hb depicts an antisickling effect of M. myristica acetone extract. This is accompanied by exacerbation of endogenous antioxidant enzymes activity and modification of the functional chemistry of the cells.

Ethnomedicinal survey of medicinal plants used in the management of sickle cell disorder in Southern Nigeria

Ethnopharmacological relevanceThe present study entails the medicinal plant species used to manage sickle cell disorder in Southern States of Nigeria. Materials and methodsThe ethnomedicinal information was gathered through multistage approach from three geopolitical zones of Southern Nigeria, which were purposively selected. Semi-structured questionnaires were administered on 500 respondents in 125 locations. The ethnomedicinal data collected were analyzed using quantitative value indices such as fidelity level (percentage) and use value. The information got was cross checked using literature search and other related materials. ResultFive hundred respondents comprising 53.12% females and 46.88% males were observed. It was noted that 26.70% were illiterate while 73.30% had formal education. Seventy-nine percent is traditional healers, 27% herb traders and the other 4% are those who have awareness of sickle cell disease . One hundred and seventy five plant species belonging to 70 families, of which Fabaceae made up 26.76% and Euphorbiaceae 16.90% forming the highest occurrence. It was observed that leaves were the most common plant part used (69.10%) followed by root (15%) and stem bark (14%) in the preparation for sickle cell management. Majority (48.57%) of these plants were harvested from wild with 38.86% being trees. Citrus aurantifolia and Newbouldia laevis had highest use values of 0.69 and 0.64 respectively. Plants with the least use value (0.001) include Abrus canescens, Acacia xanthophloea, Aerva lanata and Axonopus compressus. The result of fidelity level values of the plant species for the management of Sickle Cell Disorder (SCD) revealed that Citrus aurantifolia had the highest value of 70.2% while Angraecum distichum and Axonopus compressus had the lowest Fidelity Level value of 0.18%. ConclusionThe study revealed that people in the studied areas were well grounded in the medicinal plants used to manage sickle cell disease. This study reported for the first time 102 plant species having anti-sickling potentials with Fabaceae and Euphorbiaceae as the most dominant plant families. Many of the claimed plants were harvested from the wild showing threat thus providing needs for conservation of plants. The documented plants had high use value and fidelity level that provided quantitative and qualitative ethnomedicinal evaluation within and across the plant families. These give room for further scientific investigations in pharmacological profiles.

Moringa oleifera Lam. (Moringaceae) grown in Nigeria: In vitro antisickling activity on deoxygenated erythrocyte cells

Context:Traditional medicine, which is more available and affordable for the poor uses medicinal plants for the treatment and management of various ailments, including the sickle cell disease (SCD). About 24 million Nigerians are carriers of this sickled cell gene, while approximately 2.4 million are SCD patients. Moringa oleifera Lam. (Moringaceae) possesses high nutritional value and has been used in folklore medicine to treat various ailments related to pain and inflammation. Chemical, pharmacological and pharmacognostical applications of Moringa oleifera have been reported.Objective:This study investigated the antisickling potential of polar and non-polar extracts of the seed, flower and leaf of Moringa oleifera for the first time.Materials and Methods:Using crude methanol extract, aqueous extract, ethyl acetate and butanol, the in vitro antisickling activities of Moringa oleifera fractions, were evaluated using erythrocyte cells deoxygenated with 2% sodium metabisulphite. p-Hydroxybenzoic acid and normal saline were employed as positive and negative controls.Results:Phytochemical screening revealed the presence of saponins, free anthraquinones, and alkaloids. Extracts of the seed and flower demonstrated a higher (P<0.05) antisickling activity in comparison to the leaf extract. The leaf extract, as well as those of the seed and flower, equally demonstrated a (P<0.05) reversal of sickled erythrocytes.Discussions and Conclusions:These findings suggest that Moringa oleifera may play a role in the management of SCD, by incorporation of its fractions into recipes. More extensive biological evaluations and further studies will be necessary for the chemical characterization of the antisickling principles.

Anti sickling potential of Aloe vera extract IV: Effects of acidic, basic and neutral metabolites on the gelling and sickling of human HBSS erythrocytes

The effects of acidic, basic and neutral metabolites from A. vera extract on the sickling and gelling time of human HbSS erythrocytes were investigated. The study showed that the various metabolites inhibited sickling in vitro and increased gelling time of HbSS blood samples. Moreover, a significant increase in the number of unsickled erythrocytes was observed for the acidic metabolites. The abilities of the metabolites to revert already sickled erythrocytes to their normal morphology was highest for the acidic metabolites, but non–existent for the neutral metabolites, which appeared to be toxic to the HbSS blood cells. Therefore, it was concluded that the reversal of the sickling phenomenon could be achieved, almost quantitatively, by the consumption of acidic metabolites by sickle cell patients. Keywords: Sickle cell disease, fractionated A. vera extract, gelling time International Journal of Natural and Applied Sciences , 6(2): 155-160, 2010