Tag Archives: anti-inflammatory

Pharmacological studies of A. leiocarpa leaves

J. Pharm. Pharmacogn. Res., vol. 10, no. 3, pp. 459-468, May-June 2022.

Original Article

Pharmacological studies of anti-inflammatory, anti-nociceptive and anti-pyretic compounds found in chromatographic fractions of Anogeissus leiocarpa (DC). Guill. & Perr. leaves

[Estudios farmacológicos de compuestos antiinflamatorios, antinociceptivos y antipiréticos encontrados en fracciones cromatográficas de hojas de Anogeissus leiocarpa (DC). Guill. & Perr.]

Precious A. Idakwoji1*, Francis O. Atanu1, Paul C. Nweje-Anyalowu2,9, Theophilus B. Momoh3, Wisdom O. Oniwon1, Sara T. Elazab4, Souty M.Z. Sharkawi5,10, Rania M. Waheed6, Amal Youssef7, Gaber El-Saber Batiha8

1Department of Biochemistry, Faculty of Natural Science, Kogi State University, P.M.B. 1008, Anyigba, Kogi State, Nigeria.

2Biochemistry Programme, Department of Chemical Sciences, Faculty of Science, Clifford University, Owerrinta, Abia State, Nigeria.

3Department of Plant Science and Biotechnology, Faculty of Natural Science, Kogi State University, P.M.B. 1008, Anyigba, Kogi State, Nigeria.

4Department of Pharmacology, Faculty of Veterinary Medicine, Mansoura University, Mansoura 35516, Egypt.

5Department of Pharmacology and Toxicology, Faculty of Pharmacy, Nahda University, Egypt.

6Department of Forensic Medicine and Toxicology, Faculty of Veterinary Medicine, Benha University, Toukh 13736, Egypt.

7Medical Pharmacology Department, Faculty of Medicine, Cairo University, Egypt.

8Department of Pharmacology and Therapeutics, Faculty of Veterinary Medicine, Damanhour University, Damanhour 22511, Albeheira, Egypt.

9Department of Biochemistry, Faculty of Biological Sciences, University of Nigeria, Nsukka, Enugu State, Nigeria.

10Department of Pharmacology and Toxicology, Faculty of Pharmacy, Beni-Suef University, Egypt.

*E-mail: precious.ia@ksu.edu.ng

Abstract

Context: The anti-nociceptive and anti-pyretic properties of the crude aqueous extract of Anogeissus leiocarpa (DC). Guill. & Perr. leaves have been reported.

Aims: To investigate the anti-inflammatory, anti-nociceptive, and anti-pyretic properties of aqueous extract of A. leiocarpa leaves (AEAL) and its fractions to identify the bioactive compound(s).

Methods: AEAL was fractionated successively and eluted in gradients of solvent mixture (n-hexane, ethylacetate, and methanol). Eluates, which showed similar TLC profiles were pooled to afford 5 fractions (F1-F5). AEAL and the fractions were subjected to phytochemical analysis and investigated for anti-inflammatory, anti-nociceptive, and anti-pyretic effects using carrageenan-induced paw edema and Brewer’s yeast-induced pyrexia in rats, and acetic acid-induced writhing in mouse models, respectively.

Results: Phytochemical analysis indicated presence of terpenoids, saponins, steroids, glycosides, flavonoids, tannins and alkaloids. At 200 mg/kg b.w, AEAL and F1-F5 recorded significant (p<0.05) improvements in paw edema, abdominal constrictions and pyrexia, which is comparable to the standard (ketoprofen or Aspirin), relative to the control groups, with F4 observed to be the most potent fraction. GC-MS analysis of F4 reveal the presence of hexadecenoic acid, 15-methyl-, methylester, 9-oxabicyclo (6.1.0) nonane, cis-, cholest-4-en-3-one, cholesterol and 3-diazo-1-methyl-1, 3-dihydro-indol-2-one.

Conclusions: The results indicate that identified compounds, particularly 3-dihydro-indol-2-one, could be responsible for the anti-inflammatory, anti-nociceptive, and anti-pyretic properties of the extract.

Keywords: Anogeissus leiocarpa; anti-inflammatory; antinociception; antipyretic; inflammation; NSAID; pyrexia.

Resumen

Contexto: Se han reportado las propiedades anti-nociceptivas y antipiréticas del extracto acuoso crudo de hojas de Anogeissus leiocarpa (DC). Guill. & Perr.

Objetivos: Investigar las propiedades antiinflamatorias, anti-nociceptivas y antipiréticas del extracto acuoso de hojas de A. leiocarpa (AEAL) y sus fracciones para identificar los compuestos bioactivos.

Métodos: AEAL se fraccionó sucesivamente y se eluyó en gradientes de mezcla de solventes (n-hexano, acetato de etilo y metanol). Los eluatos que mostraron perfiles de TLC similares se agruparon para proporcionar 5 fracciones (F1-F5). AEAL y las fracciones se sometieron a análisis fitoquímicos y se investigaron los efectos antiinflamatorios, anti-nociceptivos y antipiréticos utilizando edema de la pata inducido por carragenina y pirexia inducida por levadura de Brewer en ratas, y retorcimiento inducido por ácido acético en modelos de ratón, respectivamente.

Resultados: El análisis fitoquímico indicó presencia de terpenoides, saponinas, esteroides, glucósidos, flavonoides, taninos y alcaloides. A 200 mg/kg p.c., AEAL y F1-F5 registraron mejoras significativas (p<0,05) en el edema de la pata, constricciones abdominales y pirexia que es comparable al estándar (ketoprofeno o Aspirina), en relación con los grupos de control, y se observó que F4 era la fracción más potente. El análisis GC-MS de F4 revela la presencia de ácido hexadecenoico, 15-metil-, éster metílico, 9-oxabiciclo (6.1.0) nonano, cis-, colest-4-en-3-ona, colesterol y 3-diazo-1 -metil-1,3-dihidro-indol-2-ona.

Conclusiones: Los resultados indican que los compuestos identificados, particularmente la 3-dihidro-indol-2-ona, podrían ser responsables de las propiedades anti-inflamatorias, anti-nociceptivas y anti-piréticas del extracto.

Palabras Clave: AINE; Anogeissus leiocarpa; anti-inflamatorio; anti-nocicepción; antipirético; inflamación; pirexia.

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Citation Format: Idakwoji PA, Atanu FO, Nweje-Anyalowu PC, Momoh TB, Oniwon WO, Elazab ST, Sharkawi SMZ, Waheed RM, Youssef A, Batiha GE-S (2022) Pharmacological studies of anti-inflammatory, anti-nociceptive and anti-pyretic compounds found in chromatographic fractions of Anogeissus leiocarpa (DC). Guill. & Perr. leaves. J Pharm Pharmacogn Res 10(3): 459–468.
References

Adigun JO, Amupitan JO, Kelly DR (2000) Isolation and investigation of antimicrobial effect of 3,4,3-tri-O-methylflavellagic acid and its glucoside from Anogeissus leiocarpa. Bull Chem Soc Ethiop 14: 169–174.

Adzu B, Haruna AK, Salawu OA, Sule A (2007) Bioassay-guided evaluation of the antidiarrhoeal potentials of Zizyphusspina-christi root bark in rats. Int J Biol Chem 1: 15–20.

Akuodor GC, Anyalewechi AN, Udoh FV, Okoro NC, Akpan JL, Gwotmut MD, Iwuanyanwu TC, Osunkwo UA (2011) Pharmacological evaluation of Verbena hastata leaf extract in the relief of pain and fever. AdvPharmacol Toxicol 12: 1–8.

Almgeer UM, Muhammad NM, Hafeez UK, Safirah M, Muhammad NHM, Taseer A (2015) Evaluation of anti-inflammatory, analgesic and anti-pyretic activities of Thymus serphyllum Linn. in mice. Acta Pol Pharm 72: 113–118.

Amir M, Kumar S (2005) Anti-inflammatory and gastro- sparing activity of some new indomethacin derivatives. Arch Pharm 338: 24–31.

Arai KF, Lee A, Miyajima S, Miyatake NA, Yokota T (1990) Cytokines: Coordinators of immune and inflammatory responses. Annu Rev Biochem 59: 783–836.

Atawodi SE, Adekunle OO, Bala I (2011) Antioxidant, organ protective and ameliorative properties of methanol extract of Anogeissus leiocarpa leaf against carbon tetrachloride-induced liver injury. Int J Pharm Sci Res 2: 1443–1448.

Batawila K (2005) Antifungal activities of five Combretaceae used in Togolese traditional medicine. Fitoterapia 76: 264–268.

Bhat MA, Al-Omar MA (2011) Synthesis, characterization and in vivo anticonvulsant screening of Schiff bases of phthalimide. Acta Pol Pharm Drug Res 68: 375–380.

Bhat MA, Al-Omar MA, Ansari MA, Zoheir KMA, Imam F, Attia SM, Bakheet SA, Nadeem A, Korashy HM, Voronkov A (2015) Design and synthesis of N-aryl-phthalimides as inhibitors of glucocorticoid-induced TNF receptor-related protein, pro-inflammatory mediators and cytokines in carrageenan-induced lung inflammation. J Med Chem 58: 8850–8867.

Burkill HM (1985) The Useful Plants of Tropical Africa. Vol. 1, 2nd ed. Kew: Royal Botanical Garden.

Deghrigue M, Festa C, Ghribi L, D’Auria MV, Marino SD, Jannet HB, Bouraoui A (2015) Anti-inflammatory and analgesic with gastroprotective effect of semi-purified fractions and isolation of pure compounds from Mediterranean gorgonian Eunicella singularis. Asian Pac J Trop Med 8: 606–611.

Essien AD, Akuodor GC, Essien EA, Asika EC, Chilaka KC, Nwadum SK (2015) Evaluation of anti-pyretic potential of the ethanolic leaf extract of Salacia lehmbachii Loes. Asian J Med Sci 7: 22–25.

Etuk EU, Mohammed BJ (2009) Informant consensus selection method: A reliability assessment on medicinal plants used in north western Nigeria for the treatment of diabetes mellitus. Afr J Pharm Pharmacol 3(10): 496–500.

Gaber A, Alsnie WF, Kumar DN, Refat MS, Saied EM (2020) Novel papaverine metal complexes with potential anti-cancer activities. Molecules 25: 5447.

Hijazi MA, El-Mallah A, Ellakany A (2017) Evaluation of analgesic activity of Papaver libanoticum extract in mice: involvement of opioids receptors. Evid-Based Complement Altern Med 17: 8935085.

Idakwoji PA, Agatemor UM, Akuba BO, Oniemola JM, Momoh TB (2019) Effect of aqueous leaf extract of Anogeissus leiocarpa against experimental models of pain and pyrexia. Int J Adv Res Biol Sci 6: 181–188.

Idakwoji PA, Ekpo DE, Joshua PE, Njoku OU, Nwodo OFC (2021b) Ethanol extract of Tephrosia bracteolata leaves and its fractions ameliorates alloxan-induced diabetes and its associated complications in Wistar rat model. Int J Diabetes Dev Ctries 41: 456–468.

Idakwoji PA, Joshua PE, Asamodu RO, Njoku OU, Nwodo OFC (2021a) Antidiabetic activity, phytochemical and proximate compositions of different extracts of Tephrosia bracteolata leaves. Asian J Plant Sci 20: 291–299.

Kamau JK, Nthiga PM, Safari VC, Njagi SM, Mwonjoria JK, Ngugi P (2016) Anti-pyretic properties of methanolic stem bark extract of Acacia hockii De Wild and Kigelia Africana (Lam) Benth in Wistar rats. J Pharmacogn Nat Prod 2: 3.

Kumar SA, VenkatarathanammaV, Saibabu NV, Ram SK (2015) Anti-pyretic activity of Annona plant leaves on brewer’s yeast induced febrile rats. Asian J Pharm Clin Res 8: 210–212.

Lahlou M (2013) The success of natural products in drug discovery. Pharmacol Pharm 4: 17–31.

Lamie PF, Ali WAM, Bazgier V, Rárová L (2016) Novel N-substituted indole Schiff bases as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase enzymes: synthesis, biological activities in vitro and docking study. Eur J Med Chem 123: 803–813.

Mukherjee K, Sahaand BP, Mukherjee PK (2002) Evaluation of anti-pyretic potential of Leucas lavandulaefolia (Labiatae) aerial part extract. Phytother Res 16: 686–688.

National Research Council (1996) Institute for Laboratory Animal Research. Guide for the Care and Use of Laboratory Animals. Washington (DC): National Academies Press (US).

Othman AR, Abdullah N, Ahmad S, Ismail IS, Zakaria MP (2015) Elucidation of in-vitro anti- 35 inflammatory bioactive compounds isolated from Jatropha curcas L. plant root. BMC Complement Altern Med 15: 11.

Rajeswari G, Murugan M, Mohan VR (2012) GC-MS analysis of bioactive components of Hugonia mystax L. (Linaceae). Res J Pharm Biol Chem Sci 3: 301.

Rani P, Srivastava VK, Kumar A (2004) Synthesis and anti-inflammatory activity of heterocyclic indole derivatives. Eur J Med Chem 39: 449–452.

Samriti F, Sharma S, Sati B, Pathak AK (2016) Comparative analysis of analgesic and anti-inflammatory activity of bark and leaves of Acacia ferruginea DC. Beni-Suef Univ J Basic Appl Sci 5: 70–78.

Sharar M, Saied EM, Rodriguez MC, Arenz C, Montes-Bayon M, Linscheid MW (2017) Elemental labeling and mass spectrometry for the specific detection of sulfenic acid groups in model peptides: a proof of concept. Anal Bioanal Chem 409: 2015–2027.

Sofowora AO (1993) Medicinal plants and traditional medicine in Africa. 2nd ed. Ibadan, Nigeria: Spectrum Books Limited.

Vasudevan A, Kalarickal VD, Pradeep KM, Madathilkovilakathu H (2012) Anti-inflammatory property of n-hexadecanoic acid: structural evidence and kinetic assessment. Chem Biol Drug Des 80: 434–439.

Winter CA, Risley EA, Nuss GW (1962) Carrageenan-induced oedema in the hind limb paw of the rat as an assay for anti-inflammatory Drugs Proc Soc Expt Biol Med 111: 544–547.

© 2022 Journal of Pharmacy & Pharmacognosy Research (JPPRes)

Liquid smoke as an oral ulcer remedy



J Pharm Pharmacogn Res 9(6): 905-920, 2021.

Original article

The potential of liquid smoke as an oral ulcer remedies: A proposed mechanism based on systematic review

[El potencial del humo líquido como remedio para las úlceras orales: Un mecanismo propuesto basado en una revisión sistemática]

Meircurius D.C. Surboyo1*, Diah S. Ernawati1, Ira Arundina2, Dieni Mansur3, Benni Iskandar4,5, Arvind B.R. Santosh6,Kelvin A.N. Anggrarista7, Pamela H. Cecilia7, Ayu A.B. Nagoro7

1Department of Oral Medicine, Faculty of Dental Medicine, Universitas Airlangga. Surabaya, Indonesia.

2Department of Oral Biology, Faculty of Dental Medicine, Universitas Airlangga. Surabaya, Indonesia.

3Research Centre for Chemistry, Indonesian Institute of Sciences, Kawasan PUSPIPTEK – Serpong, Tangerang Selatan, Banten, Indonesia.

4School of Pharmacy. College of Pharmacy, Taipei Medical University. Taipei, Taiwan

5Sekolah Tinggi Ilmu Farmasi Riau, Pekanbaru, Riau, Indonesia.

6School of Dentistry. Faculty of Medical Sciences. University of The West Indies, Jamaica.

7Bachelor of Dental Surgery, Faculty of Dental Medicine, Universitas Airlangga. Surabaya, Indonesia.

*E-mail: meircurius-2015@fkg.unair.ac.id

Abstract

Context: The standard management of oral ulcer therapy is focused only on symptomatic therapy, such as reducing pain. To date, there is no topical drug that has the pharmacodynamics to intervene in oral ulcer pathogenicity. Liquid smoke is traditionally used as a safe natural preservative. The liquid smoke is highly phenolic and compound rich. It is presumed to have analgesic and anti-inflammatory effects with potentially promising therapeutic effects on oral ulcers.

Aims: To describe the possible pharmacodynamics or action mechanism of liquid smoke as a promising remedy for oral ulcer therapy.

Methods: A comprehensive literature review on PubMed, ScienceDirect, Scopus and Embase was performed using Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA). The keywords used included ‘liquid smoke’, ‘wood vinegar’, ‘liquid pyrolysis’ and ‘oral ulcer’. A screening process, including titles, abstracts and full texts, was performed. Eight related articles were selected to describe the possible pharmacodynamics or mechanism action of the liquid smoke originating from coconut shells and rice hulls for oral ulcer remedies.

Results: Liquid smoke from coconut shell and rice husk is highly contained phenol, guaiacol and 2-methoxy-5-methylphenol (2-EMP). These compounds are antioxidants that can bind reactive oxygen species and increase cellular responses, inhibiting nuclear factor-kappa B activation and pro-inflammatory cytokine production while increasing macrophage differentiation to M2. The increase of M2, with help from lymphocytes, can secrete various growth factors, which can accelerate the proliferation of fibroblasts and collagens needed in the healing process of oral ulcers.

Conclusions: Liquid smoke pharmacodynamics inhibit both inflammatory and proliferation pathway stimulation, which promises remedies for oral ulcers.

Keywords: analgesic; anti-inflammatory; coconut shell-liquid smoke; human health; oral ulcer.

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Resumen

Contexto: El humo líquido es altamente fenólico y rico en compuestos. Se presume que este tiene efectos analgésicos y antiinflamatorios con prometedores efectos terapéuticos potenciales sobre las úlceras orales.

Objetivos: Describir la posible farmacodinámica o mecanismo de acción del humo líquido como un remedio prometedor para la terapia de úlceras orales.

Métodos: Se realizó una revisión exhaustiva de la literatura sobre PubMed, ScienceDirect, Scopus y Embase utilizando elementos de informes preferidos para revisiones sistemáticas y metaanálisis (PRISMA). Las palabras clave utilizadas incluyeron “humo líquido”, “vinagre de madera”, “pirólisis líquida” y “úlcera oral”. Se realizó un proceso de selección, que incluyó títulos, resúmenes y textos completos. Se seleccionaron ocho artículos relacionados para describir la posible farmacodinámica o mecanismo de acción del humo líquido procedente de las cáscaras de coco y de arroz para remediar las úlceras orales.

Resultados: El humo líquido de la cáscara de coco y la cáscara de arroz tiene un alto contenido de fenol, guayacol y 2-metoxi-5-metilfenol (2-EMP). Estos compuestos son antioxidantes que pueden unirse a especies reactivas de oxígeno y aumentar las respuestas celulares, inhibiendo la activación del factor nuclear kappa B y la producción de citocinas proinflamatorias al tiempo que aumentan la diferenciación de macrófagos a M2. El aumento de M2, con la ayuda de los linfocitos, puede secretar varios factores de crecimiento, que pueden acelerar la proliferación de fibroblastos y colágenos necesarios en el proceso de curación de las úlceras orales.

Conclusiones: La farmacodinamia del humo líquido inhibe la estimulación de las vías de proliferación e inflamación, lo que promete remedios para las úlceras orales.

Palabras Clave: analgésico; antiinflamatorio; humo líquido de cáscara de coco; salud humana; úlcera oral.

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Citation Format: Surboyo MDC, Ernawati DS, Arundina I, Mansur D, Iskandar B, Santosh ABR, Anggrarista KNA, Cecilia PH, Nagoro AAB (2021) The potential of liquid smoke as an oral ulcer remedies: A proposed mechanism based on systematic review. J Pharm Pharmacogn Res 9(6): 905–920.

© 2021 Journal of Pharmacy & Pharmacognosy Research (JPPRes)

Pharmacological properties of Centaurea tougourensis



J Pharm Pharmacogn Res 9(6): 790-802, 2021.

Original article

In vitro assessment of antioxidant, anti-inflammatory, neuroprotective and antimicrobial activities of Centaurea tougourensis Boiss. & Reut.

[Evaluación in vitro de las actividades antioxidantes, antiinflamatorias, neuroprotectoras y antimicrobianas de Centaurea tougourensis Boiss. & Reut.]

Mohamed Sabri Bensaad1,2, Saliha Dassamiour2*, Leila Hambaba2, Chawki Bensouici3, Hamada Haba4

1Laboratoire de Physio-Toxicologie, Pathologie Cellulaires et Moléculaires-Biomolécules (LPTPCMB), Département de Biologie des Organismes, Faculté des Sciences de la Nature et de la Vie, Université de Batna-2, Batna, Algeria.

2Laboratoire de Biotechnologie des Molécules Bioactives et de la Physiopathologie Cellulaire (LBMBPC), Département de Microbiologie et de Biochimie, Faculté des Sciences de la Nature et de la Vie, Université de Batna-2, Batna, Algeria.

3Centre de Recherche en Biotechnologie, Ali Mendjli nouvelle ville UV 03, Constantine, Algeria.

4Laboratoire de Chimie et Chimie de l’Environnement (LCCE), Département de Chimie, Faculté des Sciences de la Matière, Université de Batna-1, Batna, Algeria.

*E-mail: s.dassamiour@univ-batna2.dz

Abstract

Context: More than 500 Centaurea species compose the Asteraceae family, and most of the recent studies made on the species of this genus proved their pharmacological potential, especially to treat chronic illnesses.

Aims: To evaluate for the first time the antioxidant, anti-inflammatory, neuroprotective and anti-microbial properties of the n-butanol (n-BuOH) and ethyl acetate (EA) extracts of the aerial part of Centaurea tougourensis.

Methods: The antioxidant activity was determined by ABTS, galvinoxyl radical, phenanthroline, and reducing power assays, while the anti-inflammatory effects were assessed by heat-induced hemolysis and egg albumin denaturation assays. The neuroprotective activity was assessed against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) and the anti-microbial activity by the agar disk diffusion method.

Results: Both extracts possess a great antioxidant capacity, but it was considered higher in the n-BuOH extract with respective IC50 values of 8.04 ± 0.21 μg/mL in ABTS assay and 4.25 ± 0.6 μg/mL in GOR assay, while the A0.50 values were 4.46 ± 0.55 μg/mL in phenanthroline assay and 11.16 ± 0.64 μg/mL in reducing power assay. The n-BuOH extract also showed a remarkable anti-inflammatory activity with an EC50 of 120.81 ± 0.2 μg/mL in egg albumin denaturation assay and 154.15 ± 0.14 μg/mL in heat-induced hemolysis assay. The neuroprotective activity of the n-BuOH extract was very strong in both AChE and BChE inhibitory assays with respective IC50 values of 9.8 ± 0.62 μg/mL and 173.53 ± 0.04 μg/mL. EA extract was more active on microbial strains.

Conclusions: These encouraging results showed once again the pharmacological potential of Centaurea species.

Keywords: anti-inflammatory; antimicrobial; antioxidant; Centaurea tougourensis; neuroprotective.

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Resumen

Contexto: Más de 500 especies de Centaurea componen la familia Asteraceae y la mayoría de los estudios de las especies de este género demostraron su potencial farmacológico, especialmente para el tratamiento de enfermedades crónicas.

Objetivos: Evaluar por primera vez las propiedades antioxidantes, antiinflamatorias, neuroprotectoras y antimicrobianas de los extractos de n-butanol (n-BuOH) y acetato de etilo (EA) de la parte aérea de Centaurea tougourensis.

Métodos: La actividad antioxidante se determinó mediante ensayos de ABTS, radical galvinoxilo, fenantrolina y poder reductor, mientras que los efectos antiinflamatorios se evaluaron mediante ensayos de hemólisis inducida por calor y desnaturalización de albúmina de huevo. La actividad neuroprotectora se evaluó frente a acetilcolinesterasa (AChE) y butirilcolinesterasa (BChE) y la actividad antimicrobiana mediante el método de difusión en disco de agar.

Resultados: Ambos extractos poseen un gran efecto antioxidante, pero se consideró más alto en el extracto de n-BuOH con valores de IC50 respectivos de 8,04 ± 0,21 μg/mL en el ensayo ABTS y 4,25 ± 0,6 μg/mL en el ensayo GOR, mientras que los valores de A0,50 fueron 4,46 ± 0,55 μg/mL en el ensayo de fenantrolina y 11,16 ± 0,64 μg/mL en el ensayo de potencia reductora. El extracto de n-BuOH mostró también una notable actividad antiinflamatoria con una CE50 de 120,81 ± 0,2 μg/mL en el ensayo de desnaturalización de albúmina de huevo y 154,15 ± 0,14 μg/mL en el ensayo de hemólisis inducida por calor. La neuroprotección del extracto de n-BuOH se manifestó mediante la actividad inhibidora sobre AChE y BChE, con valores de IC50 respectivos de 9,8 ± 0,62 μg/mL y 173,53 ± 0,04 μg mL. El extracto de EA fue más activo contra las cepas microbianas.

Conclusiones: Estos alentadores resultados demostraron una vez más el potencial farmacológico de la especie Centaurea.

Palabras Clave: anti-inflamatorio; antimicrobiano; antioxidante; Centaurea tougourensis; neuroprotector.

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Citation Format: Bensaad MS, Dassamiour S, Hambaba L, Haba H (2021) In vitro assessment of antioxidant, anti-inflammatory, neuroprotective and antimicrobial activities of Centaurea tougourensis Boiss. & Reut. J Pharm Pharmacogn Res 9(6): 790–802.

© 2021 Journal of Pharmacy & Pharmacognosy Research (JPPRes)

Metabolic effects of M. charantia foliage extract


J Pharm Pharmacogn Res 9(4): 537-548, 2021.

Original article

Antidiabetic, hypolipidemic, antioxidant and anti-inflammatory effects of Momordica charantia L. foliage extract

[Efectos antidiabéticos, hipolipemiantes, antioxidantes y anti-inflamatorios del extracto foliar de Momordica charantia L.]

Alicia Lagarto Parra1, Roberto Menéndez Soto-del Valle2, Janet Piloto Ferrer1, Pham Thi Nguyet Hang3, Nguyen Thi Phuong3, Addis Bellma1, Orestes Darío López4, Dunia Casanave Guarnaluce1, Carlos Rodríguez Ferrada1, Alejandro S. Padrón Yaquis1, Nicte González Alfonso1, Gilberto L. Pardo-Andreu5*

1Center for Pharmaceuticals Research and Development. Av. 26 # 1605 b/ Av. Boyeros and Puentes Grandes, Havana, Cuba

2Cuban Center for Neurosciences (CNEURO), Ave 25 # 15202. Cubanacán, Playa. PO 11600. La Habana

3National Institute of Medicinal Material. 3B Quang Trung Str, Hoan Kiem Dist, Hanoi, Viet Nam.

4Facultad de Ciencia e Ingeniería en Alimentos, Universidad Técnica de Ambato, Ambato, Ecuador.

5Center for Research and Biological Evaluations, Institute of Pharmaceutical and Foods Sciences, University of Havana (UH), Av. 23 # 2317 b/ 214 and 222, La Coronela, La Lisa, PO 13600 Havana, Cuba.

*E-mail: gpardo@ifal.uh.cu

Abstract

Context: Momordica charantia (Cucurbitaceae) is extensively distributed in tropical areas, and it is traditionally used as antidiabetic. Nevertheless, few studies supporting the metabolic effects of its foliage extracts have been reported elsewhere.

Aims: To evaluate the effects of M. charantia foliage extract (MCh) on blood glucose and lipids levels in animal models of hyperglycemia. The anti-inflammatory and antioxidant properties together with the acute toxicity and genotoxic effects were also assessed.

Methods: An MCh powder was obtained by spray-drying techniques. The anti-hyperglycemic and hypolipidemic effects of MCh were evaluated in the glucose tolerance test and the alloxan-induced diabetes, respectively. The in vitro and ex vivo MCh antioxidant effects were assessed against the 2,2´-azinobis3-ethylbenzothiazoline-6-sulfonic acid (ABTS), peroxyl, and superoxide anion radicals. The MCh anti-inflammatory effects were also assessed together with its toxicological profile by means of the Acute Toxic Class Method, and the chromosome aberration assay.

Results: MCh administered orally diminished the glucose and lipids levels in normoglycemic healthy rats and alloxan-induced hyperglycemic mice. Strong in vitro free radical scavenging effects was demonstrated by MCh against ABTS, peroxyl, and superoxide anion radicals. The extract also improved the free radical scavenging ability of diabetic mice serum. Moreover, MCh reduced the weight of cotton-induced granulomas in mice, the exudate volume, and its leukocyte counts in carrageenan-induced pleurisy in rats. Very low MCh toxicity was also verified.

Conclusions: The hypoglycemic, hypolipidemic, anti-inflammatory, and antioxidant activities here observed make the spray-drayed powder from M. charantia foliage extract an interesting alternative for the correction of diabetes and its complications.

Keywords: antidiabetic; anti-inflammatory; antioxidant; foliage extract; toxicity; Momordica charantia.

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Resumen

Contexto: La Momordica charantia (Cucurbitaceae) se encuentra ampliamente distribuida en las áreas tropicales y se usa tradicionalmente como antidiabético. Sin embargo, pocos estudios sustentan los efectos metabólicos de sus extractos foliares.

Objetivos: Evaluar los efectos de un extracto foliar de M. charantia (MCh) sobre los niveles de glucosa y lípidos en modelos animales de hiperglicemia. También se evaluaron sus propiedades anti-inflamatorias y antioxidantes, así como su toxicidad aguda oral y efectos genotóxicos.

Métodos: Se obtuvo un polvo de MCh por técnicas de secado por aspersión. Sus efectos anti-hiperglicémicos e hipolipemiantes se evaluaron en modelos de tolerancia a la glucosa y de diabetes inducida por aloxano, respectivamente. Los efectos antioxidantes in vitro y ex vivo se evaluaron frente a los radicales 2,2´-azinobis3-ethylbenzotiazolina-6- ácido sulfónico, peroxilo, y el radical anión superóxido. Se evaluaron además los efectos anti-inflamatorios de MCh junto a su perfil toxicológico a través del Método de las Clases para la toxicidad aguda oral y el ensayo de aberración cromosómica.

Resultados: La administración oral de MCh disminuyó los niveles de glucosa y lípidos en ratas saludables normo-glicémicas y en ratones hiperglicémicos por acción del aloxano. Se demostró una potente actividad secuestradora de los radicales ABTS, peroxilo y superóxido, in vitro. El extracto también mejoró la actividad secuestradora de radicales libres del suero de ratones diabéticos. Además, el MCh redujo el peso de los granulomas inducidos por algodón en ratones, y en el modelo de pleuresía inducida por carragenina en ratas, redujo el volumen de exudado y su conteo de leucocitos. Se demostró una baja toxicidad para el MCh.

Conclusiones: Las actividades hipoglicémicas, hipolipemiantes, anti-inflamatorias y antioxidantes aquí observadas, hacen del extracto de M. charantia obtenido a partir de un secado por aspersión, una alternativa interesante para corregir la diabetes y sus complicaciones.

Palabras Clave: antidiabético; anti-inflamatorio; antioxidante; extracto foliar; toxicidad; Momordica charantia.

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Citation Format: Lagarto A, Menéndez R, Piloto J, Thi P, Thi N, Bellma A, Dario O, Casanave D, Rodríguez C, Padron AS, González N, Pardo-Andreu G (2021) Antidiabetic, hypolipidemic, antioxidant and anti-inflammatory effects of Momordica charantia L. foliage extract. J Pharm Pharmacogn Res 9(4): 537–548.

© 2021 Journal of Pharmacy & Pharmacognosy Research (JPPRes)