scholarly journals In vivo anti-inflammatory, anti-nociceptive, and in vitro antioxidant efficacy, and acute oral toxicity effects of the aqueous and methanolic stem bark extracts of Lonchocarpus eriocalyx (Harms.)

Heliyon ◽  
2021 ◽  
Vol 7 (5) ◽  
pp. e07145
Author(s):  
Gervason Apiri Moriasi ◽  
Anthony Muriithi Ireri ◽  
Elias Mandela Nelson ◽  
Mathew Piero Ngugi
2021 ◽  
Vol 26 ◽  
pp. 2515690X2110645
Author(s):  
Evans Kapanat Akimat ◽  
George Isanda Omwenga ◽  
Gervason Apiri Moriasi ◽  
Mathew Piero Ngugi

The root and leaf extracts of Launaea cornuta have been locally used in traditional medicine for decades to manage inflammatory conditions and other oxidative-stress-related syndromes; however, their pharmacologic efficacy has not been scientifically investigated and validated. Accordingly, we investigated the in vitro antioxidant activity, anti-inflammatory ( in vitro, ex vivo, and in vivo) efficacy, acute oral toxicity, and qualitative phytochemical composition of the aqueous root extract of L. cornuta. The ferric-reducing antioxidant power (FRAP) and the 2,2-diphenyl-2-pycrylhydrazyl (DPPH) radical scavenging test methods were used to determine the studied plant extract’s antioxidant activity. Besides, the anti-inflammatory efficacy of the studied plant extract was investigated using in vitro (anti-proteinase and protein denaturation), ex vivo (membrane stabilization), and in vivo (carrageenan-induced paw oedema in Swiss albino mice) methods. The studied plant extract demonstrated significant in vitro antioxidant effects, which were evidenced by higher DPPH radical scavenging and FRAP activities, in a concentration-dependent manner ( p < 0.05). Generally, the studied plant extract exhibited significant in vitro, ex vivo, and in vivo anti-inflammatory efficacy, respectively, and in a concentration/dose-dependent manner compared with respective controls ( p < 0.05). Moreover, the studied plant extract did not cause any observable signs of acute oral toxicity, even at the cut-off dose of 2000 mg/Kg BW (LD50 > 2000 mg/Kg BW), and was thus considered safe. Additionally, qualitative phytochemistry revealed the presence of various antioxidant- and anti-inflammatory-associated phytochemicals, which were deemed responsible for the reported pharmacologic efficacy. Further studies to characterise bioactive molecules and their mode(s) of pharmacologic efficacy are encouraged.


Author(s):  
SUPRIYA RAJA H

Objective: Knema attenuata (Myristicaceae), popularly known as “wild nutmeg,” is an endemic tree species from Western Ghats, which has been used in folk medicine. Conventionally, the stem bark of K. attenuata is used for treating inflammatory conditions without any scientific information available for the same. The present study was undertaken to evaluate the anti-inflammatory activity of the ethanolic stem bark extract (ESBE) of K. attenuata using in vivo and in vitro screening models. Methods: The ethanolic extract of stem bark was prepared by soxhlation, and its cytotoxicity in RAW 264.7 cell line was assessed using MTT assay method. In vivo anti-inflammatory effect of extract was estimated in rats using carrageenan-induced paw edema model and cotton pellet-induced granuloma model. The in vitro anti-inflammatory activity of the extract was evaluated by cyclooxygenase and lipoxygenase inhibition assay, estimation of myeloperoxidase activity, and determination of cellular nitrite levels in lipopolysaccharide-stimulated RAW 264.7 macrophage cells. Results: Toxic symptoms were not observed for the ESBE. The extract demonstrated significant anti-inflammatory activity in both in vivo and in vitro models. The anti-inflammatory action exhibited by the extract was a result of the inhibition of leukocyte migration and nitric oxide pathway and partially by inhibition of mediators such as prostaglandins and leukotrienes. Conclusion: Findings from the study provide the evidence for the popular use of stem bark extract of K. attenuata as a potential anti-inflammatory agent.


2021 ◽  
Vol 12 (6) ◽  
pp. 8471-8491

Bioprospecting has contributed to the work of pharmaceutical chemists in the development and commercial disposal of new drugs. Currently, the pharmaceutical industry has emphasized drugs produced from bioactive compounds extracted from natural sources, based on popular medicine discussed in the literature, such as secondary metabolites isolated from the stem bark and seeds of the Amburana cearensis, rich in coumarin derivatives, flavonoids, and phenolic acids and is popularly used in the treatment of respiratory diseases and with anti-inflammatory and antioxidant bioactivity. This review is a study of the structure/activity and structure/property (SAR/SPA) relationship with the physicochemical properties calculated by the algorithms of the MarvinSketch software for the secondary metabolites of A. cearensis, as well as their correlation with in silico test values the SwissADME and admetSAR 2.0 servers and in vitro and in vivo models of the dataset from the PreADMET, GUSAR Online and PASS Online servers. The results showed that substances derived from coumarin, flavonoids, and phenolic acids have attributes of good permeability and low efflux, which favor their oral bioavailability, since phenolic heterosides, amburoside analogs, and biflavonoids are effective in local action as subcutaneous application, constituting promising antimicrobial, anti-inflammatory and antioxidant therapeutic actions in their proper administration routes.


2020 ◽  
Vol 10 (2) ◽  
pp. 65
Author(s):  
Mbiantcha Marius ◽  
Ateufack Gilbert ◽  
TsafackEric Gonzal ◽  
DjuichouNguemnang Stephanie Flore ◽  
AtsamoAlbert Donatien ◽  
...  

2020 ◽  
Vol 9 (10) ◽  
pp. e5059108817
Author(s):  
Dayse Lucia do Nascimento Brandão ◽  
Michel Tavares Martins ◽  
Adreanne Oliveira Silva ◽  
Amanda Dias Almeida ◽  
Renata Cristina de Paula ◽  
...  

The objective of this work was to evaluate the antiplasmodial activity and toxicity of the extract and fractions obtained from the bark of Aspidosperma nitidum. The ethanol extract obtained from the powdered bark of plants was acid-base partitioned and phytochemically analyzed. The antiplasmodial activity, in vivo antimalarial activity and in vitro cytotoxicity were acessed. The selectivity index (SI) was calculated. The acute oral toxicity and pathological effects, of the ethanol extract was evaluated in mice. The major constituent of the ethanol extract was suggestive of a β-carboline chromophore. The alkaloid and neutral fractions contained compounds with an aspidospermine core as the major constituent. The ethanol extract (IC50 = 3.60 µg/mL), neutral fraction (IC50 = 3.34 µg/mL) and alkaloid fraction (IC50= 2.32 µg/mL) showed high activity against P. falciparum (W2 strain). The ethanol extract and the alkaloid fraction reduced 80% of the parasitemia of P. berghei (ANKA)-infected mice (dose of 500 mg/kg) in the 5th day, which was not sustainable at the 8th day. A similar result was obtained for chloroquine. The ethanol extract (CC50 = 410.65 µg/mL; SI = 114.07), neutral fraction (CC50 = 452.53 µg/mL; SI = 135.49), and alkaloid fraction (CC50 =346.73 µg/mL; SI 149.45) demonstrated low cytotoxicity and high SI. The ethanol extract (5000 mg/kg; gavage) presented low acute oral toxicity, with no clinical or anatomopathological modifications being observed (in comparison to the control group). In vitro studies with a chloroquine-resistant clone of P. falciparum confirmed the antiplasmodial activity of the A. nitidum ethanol extract, and its fractions had low cytotoxicity for HepG2 cells. In vivo studies with P. berghei–infected mice and acute toxicity studies corroborated these results.


2022 ◽  
Vol 23 (1) ◽  
Author(s):  
Yuan Fan ◽  
Yunxing Fu ◽  
Yuhang Zhou ◽  
Yu Liu ◽  
Baocheng Hao ◽  
...  

Abstract Background Py-mulin is a new pleuromutilin derivative with potent antibacterial activities in vitro and in vivo, suggesting this compound may lead to a promising antibacterial drug after further development. The present study is aimed to evaluate the acute and subacute oral toxicity, and the genotoxicity with the standard Ames test according to standard protocols. Methods Acute oral toxicity of Py-mulin was determined using Kunming mice. The 28-day repeated dose oral toxicity study in SD rats was performed according to OECD guideline No. 407. The bacterial reverse mutation (Ames test) was carried out using four Salmonella typhimurium (S. typhimurium) strains TA97, TA98, TA100 and TA1535 with and without S9 metabolic activation. Results The LD50 values in acute oral toxicity were 2973 mg/kg (female mice) and 3891 mg/kg (male mice) calculated by the Bliss method. In subacute toxicity study, 50 mg/kg Py-mulin did not induce any abnormality in body weight, food consumption, clinical sign, hematology, clinical chemistry, organ weight, and histopathology in all of the treatment groups. However, high doses of Py-mulin (100 and 300 mg/kg) displayed slightly hepatotoxicity to female rats. Furthermore, Py-mulin did not significantly increase the number of revertant colonies of four standard S. typhimurium strains with the doses of 0.16–1000 μg/plate in the Ames study. Conclusions Based on our findings, our study provides some information for the safety profile of Py-mulin.


2020 ◽  
Vol 2020 ◽  
pp. 1-10
Author(s):  
Ben Olela ◽  
James Mbaria ◽  
Timothy Wachira ◽  
Gervason Moriasi

Inflammation and pain are devastating conditions characterizing many diseases. Their manifestation ranges from mild body discomfort, to a debilitating experience, which may culminate in organ failure or death. In conventional medicine, corticosteroids, nonsteroidal anti-inflammatory drugs, opioids, and adjuvants are utilized to manage symptoms related to pain and inflammation. Despite their reported successes, these agents are only palliative, debatably inaccessible, unaffordable, and cause many undesirable side effects. As a result, the search for alternative and complementary therapies is warranted. Medicinal plants have been intensively utilized by humans for a long time to treat various ailments. In spite of their reported efficacies, empirical scientific data supporting their healing claims is scanty. P. thonningii (Schumach.) has been used in African traditional medicine, especially by traditional herbalists in Nigeria and Kenya, to treat conditions associated with inflammation. Even though analgesic, anti-inflammatory, and toxicity studies have been performed on leaf extracts, and some of their isolated compounds in Nigeria, there is scanty data supporting the use of stem bark extracts, which are commonly utilized in Kenya for pain, and inflammation management. Moreover, scientific data regarding safety and toxicity of the stem bark extracts of P. thonningii utilized in Kenya by traditional herbalists are inadequate. Based on this background, acute oral toxicity evaluation of the aqueous and methanolic stem bark extracts of P. thonningii, in Swiss albino mice, was performed according to the OECD/OCDE (2008) guidelines. Anti-inflammatory activities were investigated using the xylene-induced ear oedema in mice, whereas analgesic activities were examined following the acetic acid-induced writhing technique. The acute oral toxicity data was analyzed, and interpreted according to the OECDE (2008) guidelines. Anti-inflammatory and analgesic activities data were tabulated on MS Excel, and exported to GraphPad Prism (v8.3). Descriptive statistics were computed, and expressed as mean ± SEM. Thereafter, One-Way ANOVA followed by Tukey’s test was performed. p<0.05 was considered statistically significant. All the studied plant extracts had LD50 values > 2000 mg/kg bw, and were hence deemed to be nontoxic according to OECD/OCDE document no. 425. The results showed that the acetic acid-induced writhing frequency in mice administered the aqueous stem bark extract of P. thonningii, at a dose of 500 mg/kg bw, was not significantly different from that recorded for mice which received the reference drug (acetylsalicylic acid 75 mg) (p>0.05). Additionally, at all the studied extract doses, significantly lower acetic acid-induced writhing frequencies were recorded in mice that received the aqueous stem bark extract of P. thonningii, compared with the writhing frequencies in mice that received the methanolic extract of the same plant (p<0.05). On the other hand, the aqueous stem bark extract of P. thonningii, at doses of 100 mg/kg bw and 500 mg/kg bw, and the methanolic stem bark extract of the same plant, at a dose level of 500 mg/kg bw, exhibited significantly higher percentage inhibitions of xylene-induced oedema than the percentage inhibitions shown by the reference drug (dexamethasone 1 mg/kg bw) (p<0.05). Generally, the aqueous stem bark extract of P. thonningii, at all the studied dose levels, caused significantly higher inhibitions of xylene-induced ear oedema in mice, compared with the percentage inhibitions shown by methanolic stem bark (p<0.05). Therefore, the aqueous, and methanolic stem bark extracts of P. thonningii, grown in Kenya, possess peripheral analgesic and anti-inflammatory activities in Swiss albino mice. Hence, they have a potential of offering safe analgesic, and anti-inflammatory compounds. Further studies aimed at isolating, elucidating, and characterizing bioactive components from the studied extracts are recommended. Moreover, specific mode(s) through which these extracts exert the reported bioactivities should be established. Further toxicological investigations involving the studied plant extracts are encouraged to fully establish their safety.


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