HPLC ANALYSIS AND ANTI-INFLAMMATORY PROPERTIES STUDIES OF TRUNK BARKS OF ACACIA NILOTICA VAR ADANSONII (GUILL AND PERR) O KTZE (MIMOSACEAE)

Objective: The objective of this study was to evaluate the in vitro and in vivo anti-inflammatory properties of the aqueous extract and fractions of the trunk bark of Acacia nilotica. Methods: A maceration of the powder of the trunks barks of the plant was realized. Then the aqueous macerate obtained was fractionated with dichloromethane, butanol and ethyl acetate successively. The phenolic compounds of the aqueous extract, butanol and ethyl acetate fractions were identified by HPLC/DAD. Lipoxygenase and phospholipase inhibition tests with the aqueous extract and the butanol and ethyl acetate fractions were carried out. The anti-inflammatory potential of the aqueous extract was assessed in vivo by the anti-edema test with carrageenan and the analgesic test with acetic acid at different doses (200 mg/ml; 400 mg/ml; 600 mg/ml). Aspirin (200 mg/ml) and paracetamol (200 mg/ml) were used as a reference. Results: The HPLC/DAD analysis of the extracts revealed that gallic acid is the most abundant phenol acid in the extracts. The aqueous extract inhibited lipoxygenase (IC50 = 18.32±1.18 μg/ml), phospholipase (11.44±0.32% per 100 μg/ml) and cyclooxygenase (56.48±0.29% for 100 μg/ml) as well as its tested fractions. It also reduced edema and pain in the mice by more than 50% from the 400 mg/ml dose. Conclusion: Aqueous extract of Acacia nilotica has anti-inflammatory properties. Hence its use in traditional medicine in the treatment of inflammation

Quality control and standardization of FACA® syrup

Sickle cell disease is a major public health problem. It is the first genetic disease in the world. FACA syrup offers an alternative treatment. It is a dry powder preparation of two components, the roots barks of Zanthoxylum zanthoxyloides Lam. (Rutaceae) Zepernick, Timler and Calotropis procera. Ait. R.B.r. (Asclepiadaceae). The product was developed at Institute for Research in Health Sciences (IRSS) from a traditional recipe used in Burkina Faso for treatment of sickle cell crises. This study aimed to establish physical-chemical, pharmaco technical and microbiological control parameters essential for the standardization of the phytomedicine. This valuation concerned specifications of moisture content, pH, the fingerprint by thin layer chromatography, pesticide residues, heavy metal content, microbial quality, and total ash. These charcteristics were determined by the methods prescribed by the World Health Organization (1998) and the European Pharmacopoeia 6th edition. The results have shown that dry syrups and reconstituted syrups were sweet, slightly spicy with a bitter after taste, a white room color and a faint odor. The density at the preparation was 0.985 and the pH was 5.93. After 2 months of storage in the laboratory, the organoleptic parameters of the reconstituted syrups have not changed. They were mold free, the density remained around 1 and the pH between 5 and 4. These parameters have shown that the quality of plants powders and these medicine comply with the recommendations of the European pharmacopoeia. Faca syrup may contribute to the better management of sickle cell disease in children

Production de matières premières et fabrication des médicaments à base de plantes médicinales

Les plantes constituent un réservoir pour les pharmacopées du monde. Plusieurs médicaments importants sont fabriqués à partir des substances actives d’origine végétales. En outre de nombreux médicaments modernes ont été fabriqués à partir de ces matières premières. Les plantes médicinales sont utilisées directement sous forme fraîche, sèche ou transformée, stabilisée, ou extrait ou formulée avec d’autres plantes ou excipients de synthèse. Dans tous les cas, la matière végétale utilisée pour fabriquer la forme posologique doit faire preuve de son efficacité, son innocuité et être de qualité conforme aux exigences de la Pharmacopée Européenne pour les phytomédicaments, garantissant ainsi sa sécurité d’emploi. Pour ce faire, l’Organisation Mondiale de la Santé (OMS) a mis à la disposition des états membres des guides et standards permettant d’harmoniser et de sécuriser leur utilisation. Ainsi de nombreux pays africains ont adopté ces outils après des modifications appropriées pour faire progresser la recherche et le développement (R&D) de médicaments à base de plante. Le but de ce travail était de faire une synthèse des différentes étapes de production, de contrôle qualité et de  standardisation des matières premières issues des plantes médicinales et des médicaments à base de plantes médicinales.Mots clés : Pharmacopée, médicaments, médecine traditionnelle, sécurité d’emploi, phytomédicaments. English title: Production of raw materials and manufacturing of drugs from medicinal plants Plants are a reservoir for the world's pharmacopoeias. Several important medicines are made from active substances of plant origin. In addition, many modern medicines have been made from these raw materials. Medicinal plants are used directly in fresh, dry or processed, stabilized, or extracted form or formulated with other plants or synthetic excipients. In all cases, the herbal material used to manufacture the dosage form must demonstrate its efficacy, safety and be of a quality that meets the requirements of the European Pharmacopoeia for phytomedicines, thus ensuring its safe use. To this end, the World Health Organization (WHO) has made available to Member States guides and standards to harmonize and secure their use. Thus, many African countries have adopted these tools after appropriate modifications to advance research and development (R&D) of plant-based drugs. The aim of this work was to make a synthesis of the different stages of production, quality control and standardization of raw materials from medicinal plants and herbal medicines.Keywords: Pharmacopoeia, drugs, traditional medicine, safe use, phytomedicines

ENDOTHELIUM-INDEPENDENT AND ENDOTHELIUM-DEPENDENT VASORELAXATION BY A DICHLOROMETHANE FRACTION FROM ANOGEISSUS LEIOCARPUS (DC) GUILL. ET PERR. (COMBRETACEAE): POSSIBLE INVOLVEMENT OF CYCLIC NUCLEOTIDE PHOSPHODIESTERASE INHIBITION.

Many traditional medicinal herbs from Burkina Faso are used to treat arterial hypertension (HTA). Among them, Anogeissus leiocarpus (A. Leiocarpus) which is well known and widely used in Burkina traditional medicine. Herein we assess the effects of dichloromethane fraction from A. leiocarpus stem bark (ALF), selected as the most active on cyclic nucleotide phosphodiesterases (PDEs) and characterized its specificity towards purified vascular PDE1 to PDE5 isoenzymes and study its effects on a vascular model. ALF potently and preferentially inhibits (IC50=1.6 ± 0.6 µg/mL) the calmodulin-dependent phosphodiesterase PDE1, being mainly present in vascular smooth muscle and preferentially hydrolyses cGMP. In the same range (IC50 =2.8 ±0.2 µg/ml) ALF inhibits PDE2, a cGMP-activated enzyme that is only present in endothelial cells and hydrolyses both cAMP and cGMP. PDE5, which specifically hydrolyses cGMP and which mainly contributes to cGMP hydrolysis is also potently inhibited by ALF (IC50=7.6±3.5 µg/ml). The potencies of ALF on cAMP hydrolyzing isoenzymes was lesser, being more effective on PDE4 (IC50= 17.6±3.5 µg/ml) than on PDE3 (60.9 ± 1.8 µg/ml). Since the major effect of ALF were against cGMP hydrolysis and since cGMP is implicated in endothelium-dependent relaxation, the endothelium-dependent vasorelaxation was studied on isolated porcine coronary arteries rings pre-contracted with U46619. The endothelium-dependent vasorelaxation is significantly inhibited by Nω-nitro-L-arginine (LNA 300 µmol/L, an inhibitor of endothelial NO synthase), but not affected by charybdotoxin (CTX, 100nM) plus apamin (APA, 100nM) (two inhibitors of EDHF-mediated responses). The combination of 4-aminopyridine (4-AP, 1 mmol/L, inhibitor of voltage-dependent potassium channels, Kv) plus baryum (Ba2+, 30 µmol/L, inhibitor of the potassium channels with entering correction, Kir) plus ouabain (3 µmol/L, inhibitor of ATPase Na+/K+ channels) partially inhibits endothelium-independent vasorelaxant effect. This endothelium-independent relaxant effect was also sensitive to combination of 1H-[1,2,4]-oxadiazole-[4,3-α]-quinoxalin-1-one (ODQ, 10 µM, soluble guanylyl cyclase inhibitor) and N-[2-(p-Bromocinnamylamino)ethyl]-5-isoquinoline sulfonamide dihydrochloride (H89, 100 nM, Protein Kinase A inhibitor). Taken together, these results indicate that ALF is a powerful vasodilator modulated by the formation of NO from endothelium, but also act by directly relaxing the vascular smooth muscle cells, by inhibiting cGMP hydrolyzing PDEs (PDE1, PDE2 and PDE5) and to a lesser extend on cAMP degradation (PDE3 and PDE4), cAMP and cGMP being second messengers involved in vascular relaxation

Pharmacological study of trunk bark of Acacia nilotica var adansonii (Guill et Perr).o Ktze (Mimosaceae): Assays, antioxidant and antispasmodic activities

Aim of this study was to evaluate in vitro polyphenols content, antioxidant and antispasmodic properties of the aqueous extract and fractions of the trunk bark of Acacia nilotica. According to a survey conducted in rural Burkina Faso, Acacia nilotica var. adansonii (Guill and Perr). Ktze reported to be widely used in the treatment of gastrointestinal diarrhoea and parasitosis. A maceration of the powder of the trunk bark of the plant was carried out. Then the aqueous macerate obtain, was fractionated with dichloromethane, butanol and ethyl acetate successively. The phenolic compounds of the aqueous extract, butanol and ethyl acetate fractions was determinated. The antioxidant activity of aqueous extract and fractions was evaluated by the DPPH, ABTS and FRAP tests. The contractility test on smooth muscle was realized according to Magnus method. Assay of the extracts revealed a high content of polyphenols, tannins and flavonoids. The aqueous extract, the butanol fraction and the ethyl acetate fraction demonstrated a high antioxidant capacity. Aqueous extract showed a better antispasmodic effect of acetylcholine contraction induction at 1 μM (IC50 = 13.02 μg / mL) and for BaCl2 at 160 μg / mL (IC50 = 117.2 μg / mL). The aqueous extract of Acacia nilotica and his fractions had antioxidant properties. Only aqueous extract proven better antispasmodic property. Hence its use in traditional medicine in the treatment of diarrhoea. Keywords: Acacia nilotica, Antioxidant, Antispasmodi

Antioxidant properties and subchronic toxicity of the standardized extract of LAMIC, a phytomedicine prototype based on aqueous extracts from trunk bark of Lannea microcarpa Engl and K. Krause

Aims: This study investigated the antioxidant activity and the 90 days subchronic toxicity of the standardized LAMIC phytomedicine prototype based on aqueous extracts from Lannea microcarpa trunk bark. Methods: Three spectrophotometric methods were used to evaluated the antioxidant activity of LAMIC which were 2,2-Diphenyl-1-picrylhydrazyl (DPPH) free radical, 2,2’-azinobis(3-ethylbenzolin-6-sulphonate) (ABTS) radical scavenging assays and ferric reducing antioxidant power (FRAP) assays. For the standardized LAMIC subchronic toxicity study, male and female Wistar rats were used by daily oral administration at doses of 500, 1000 and 1500 mg/kg bw consecutively for 90 days. Results: The LAMIC extract exhibit better inhibitory activity against DPPH radical than ABTS radical with respective IC50 values of 45.38±3.21 µg/mL and 66.45±18.76 µg/mL, while FRAP assay exhibit antioxidant activity of 211.34±15.92 mmol EAA/g. Subchronic oral administration of LAMIC was well-tolerated at all tested doses. No behavioral and physiological changes and mortality were observed. The LAMIC extract did not present any impact on general hematological parameters and biochemical parameters. Moreover, no significant changes were raised in organ and body weight of treated groups compared to the Control group. Conclusion: These results support that LAMIC prototype was a valuable source of natural antioxidants and no toxicity was associated to its long terms oral consumption in rats indicating a potential application as a cardiovascular protective formulation. Keywords: LAMIC–Lannea microcarpa–Standardization–Antioxidant–Subchronic toxicity. &nbsp

In Vivo Diuretic Activity and Anti-Hypertensive Potential of <i>Hibiscus sabdariffa</i> Extract by Inhibition of Angiotensin-Converting Enzyme and Hypertension Precursor Enzymes

Aqueous extracts of calyx from Hibiscus sabdariffa (HS) (roselle) are highly appreciated for their nutritional and therapeutic effects, especially as anti-hypertensive substances. This study aimed to evaluate their anti-hypertensive potential through an in vitro inhibition assay of angiotensin-converting enzyme (ACE) and hypertension precursor enzymes and to assess the in vivo diuretic activity of HS. Results showed that HS extract inhibited enzymes belonging to several classes, such as α-amylase, trypsin, chymotrypsin, xanthine oxidase, lipoxygenase, and angiotensin-converting enzyme. In particular, enzymatic kinetics of ACE indicated a competitive inhibition fashion of HS extract. Furthermore, the extracts showed remarkable diuretic and natriuretic effects at doses of 50 mg/kg/bw, 100 mg/kg/b.w, and 200 mg/kg.b.w. These activities can be explained by the high content of phenolic compounds and essential amino acids. Roselle could be a potential source of nutraceuticals and anti-hypertensive bioactive compounds

Evaluation of acute, subacute toxicity and in vivo impact of aqueous decoction of Flemingia faginea Guill. & Perr. (Barker) leafy stems on NMRI mice and normotensive Wistar rats

Introduction: Flemingia faginea, a Fabaceae family medicinal plant, has been used for a long time in Burkina Faso for the treatment of hypertension and excess salt. However, the safety of the preparations derived from this plant has not yet been scientifically documented. This study aimed to evaluate the acute and subacute oral toxicity of the leafy stems aqueous decoction of F. faginea (FAD) in healthy normotensive mice and rats and the impact on their normal blood pressure. Material and Methods: The acute oral toxicity study was conducted according to the toxicity class method of the Economic Cooperation and Development Organization (OECD) guideline 423. Subacute toxicity was carried out according to the OECD Guideline 407 for repeated dose chemical toxicity for 28 days. Hematological and biochemical analyzes of blood were performed after autopsy. An evaluation of the impact of the extract on the blood pressure of rats was performed using the non-invasive method. Results: A single oral dose of 2000 mg/kg bw to mice did not cause mortality or clinical signs or symptoms of toxicity during the 14-day study. The FAD was classified in the fifth category of the Harmonized System of Classification of the United Nations and considered practically safe with an estimated 50% lethal dose of 5000 mg/kg bw. Daily gavage of male and female rats with doses of 100,500 and 1000 mg/kg did not result in mortality or significant adverse effects during the 28days of experimentation. There were no significant differences in body weight gain, food &amp;water consumption or relative vital organ weights in treated animals. Analysis of the hematological and biochemical parameters of blood serum did not show significant differences between treated and control animals in this study. Additionally, no aberrant changes were found in the systolic and diastolic blood pressures of the test animals during the 28 days of inclusion compared to those of the control group. Conclusion: The extract FAD could be considered safe within the doses tested for the results of the toxicological evaluation. However, microscopic, histopathological, and subchronic investigations will have to be carried out to confirm the safety of this extract use

An aqueous extract of the Anogeissus leiocarpus bark (AEAL) induces the endothelium-dependent relaxation of porcine coronary artery rings involving predominantly nitric oxide

International audienc

Capsule Formulation Essay of Herbal Extracts of Trunk Bark of Anogeissus leiocarpus (DC) Guill. Et Perr. (Combretaceae) for the Treatment of Hypertension

Introduction: The trunks barks of Anogeissus leiocarpus contains multiple antihypertensive components and are, therefore, widely used for the treatment of hypertension. Objective: This study aimed to formulate capsules containing a freeze-dried aqueous extract of the trunk’s barks. Methodology: Three (03) capsule formulations were prepared using wet granulation from lyophilised aqueous extract of Anogeissus leiocarpus trunk bark, with different proportions of excipients including Corn starch used as the diluent, Polyvinylpyrrolidone K25 (PVP) used as binding agent and Magnesium stearate used as gliding agents. The filling of capsules was done using a semi-automatic capsule filler with empty capsules of size 3. The flow properties of the granules and the quality control were performed according to the European Pharmacopoeia 10th ed. Results/Discussion: All granules had good flow properties, and the F1 and F3 formulations had the best pharmaceutics characteristics according to the recommendations of the European Pharmacopoeia 10th ed. The mean levels of phenolic tracers were 0.039±0.0097 mg gallic acid equivalent per capsule (GAE/capsule) for the F1 formulation and 0.059±0.0063 mg GAE/capsule for the F3 formulation. Conclusion: This study allowed the galenic formulation of capsules based on extracts of good characteristic quality for the treatment of hypertension. Keywords: Anogeissus leiocarpus, extract, excipients, formulations, capsul