Antimycobacterial and Nitric Oxide Production Inhibitory Activities ofOcotea notatafrom Brazilian Restinga

The genusOcotea(Lauraceae) is distributed mainly in tropical and subtropical regions. Some species of this genus asO. puberulaandO. quixoshave been described in the literature, showing antibacterial activity. AndOcotea macrophyllashowed anti-inflammatory activity with inhibition of COX-1, COX-2, and LOX-5. The purpose of this study was the phytochemical investigation of the plant speciesOcotea notatafrom Restinga Jurubatiba National Park, Macaé, RJ, Brazil, and the search for antimycobacterial fractions and compounds. The crude extract was evaluated for antimycobacterial activity and presented95.75±2.53% of growth inhibition at 100 µg/mL. Then, it was subjected to a liquid-liquid partition and subsequently was chemically investigated by HPLC, revealing the major presence of flavonoids. In this process the partition fractions hexane, ethyl acetate, and butanol are shown to be promising in the antimycobacterial assay. In addition, ethyl acetate fraction was chromatographed and afforded two flavonoids identified by MS and NMR as afzelin and isoquercitrin. The isolated flavonoids afzelin and isoquercitrin were evaluated for their antimycobacterial activity and for their ability to inhibit NO production by macrophages stimulated by LPS; both flavonoids isoquercitrin (Acet22) and afzelin (Acet32) were able to inhibit the production of NO by macrophages. The calculated IC50of Acet22 and Acet32 was 1.03 and 0.85 µg/mL, respectively.

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Ergosterol of Cordyceps militaris Attenuates LPS Induced Inflammation in BV2 Microglia Cells

Natural Product Communications ◽

10.1177/1934578x1501000623 ◽

2015 ◽

Vol 10 (6) ◽

pp. 1934578X1501000 ◽

Cited By ~ 4

Author(s):

Neeranjini Nallathamby ◽

Lee Guan-Serm ◽

Sharmili Vidyadaran ◽

Sri Nurestri Abd Malek ◽

Jegadeesh Raman ◽

...

Keyword(s):

Nitric Oxide ◽

Cell Viability ◽

Ethyl Acetate ◽

Ethyl Acetate Fraction ◽

Cordyceps Militaris ◽

No Production ◽

Nitric Oxide Production ◽

Cytotoxic Effects ◽

Bv2 Cells ◽

Bv2 Microglia

Different solvent extracts of Cordyceps militaris stroma powder were tested for cell viability and inhibition of nitric oxide (NO) production in lipopolysaccharide (LPS) triggered BV2 microglia cells. Chemical investigation of the ethyl acetate fraction resulted in an enriched ergosterol sub-fraction CE3. The BV2 cells showed no cytotoxic effects when treated with the ethyl acetate fraction and sub-fraction CE3 at concentrations of 0.1 μg/mL – 100 μg/mL compared with the control. At 10 μg/mL, the ethyl acetate fraction and sub-fraction CE3 had the highest reduction of 48.0% and 44.7% of nitric oxide production, respectively. The major compound in sub-fraction CE3 was ergosterol, identified by GCMS, and the purity was checked by HPLC. Further, the reduction of nitric oxide in LPS triggered BV2 cells was about three fold higher when compared with the control commercial ergosterol.

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Antimycobacterial and Nitric Oxide Production Inhibitory Activities of Triterpenes and Alkaloids from Psychotria nuda (Cham. & Schltdl.) Wawra

Molecules ◽

10.3390/molecules24061026 ◽

2019 ◽

Vol 24 (6) ◽

pp. 1026 ◽

Cited By ~ 1

Author(s):

Almir de Carvalho Junior ◽

Rafaela Oliveira Ferreira ◽

Michel de Souza Passos ◽

Samyra da Silva Boeno ◽

Lorena Glória das Virgens ◽

...

Keyword(s):

Nitric Oxide ◽

Indole Alkaloids ◽

Antimycobacterial Activity ◽

No Production ◽

Nitric Oxide Production ◽

In Vitro Activity ◽

Phytochemical Study ◽

Pomolic Acid ◽

Inhibitory Activities

A phytochemical study of leaves and twigs of Psychotria nuda resulted in 19 compounds, including five indole alkaloids, N,N,N-trimethyltryptamine, lyaloside, strictosamide, strictosidine, and 5α-carboxystrictosidine; two flavonolignans, cinchonain Ia and cinchonain Ib; an iridoid, roseoside; a sugar, lawsofructose; a coumarin, scopoletin; a diterpene, phytol; three triterpenes, pomolic acid, spinosic acid, and rotungenic acid; and five steroids, sitosterol, stigmasterol, campesterol, β-sitosterol-3-O-β-d-glucoside, and β-stigmasterol-3-O-β-d-glucoside. Some compounds were evaluated for their in vitro activity against Mycobacterium tuberculosis and their ability to inhibit NO production by macrophages stimulated by lipopolysaccharide (LPS). The compounds pomolic acid, spinosic acid, strictosidine, and 5α-carboxystrictosidine displayed antimycobacterial activity with minimum inhibitory concentrations ranging from 7.1 to 19.2 µg/mL. These compounds showed promising inhibitory activity against NO production (IC50 3.22 to 25.5 μg/mL). 5α-carboxystrictosidine did not show cytotoxicity against macrophages RAW264.7 up to a concentration of 100 µg/mL. With the exception of strictosamide, this is the first report of the occurrence of these substances in P. nuda.

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Wound healing activity of Conyza canadensis (L.) Cronquist

Science and Technology Development Journal - Natural Sciences ◽

10.32508/stdjns.v1it5.533 ◽

2018 ◽

Vol 1 (T5) ◽

pp. 35-40

Author(s):

To Dinh Le ◽

Nga Thi Hoang ◽

Nhan Thi Thanh Nguyen ◽

Thuoc Linh Tran ◽

Thao Thi Phuong Dang

Keyword(s):

Wound Healing ◽

Antibacterial Activity ◽

Ethyl Acetate ◽

National Park ◽

Ethanolic Extract ◽

Ethyl Acetate Fraction ◽

Conyza Canadensis ◽

Keratinocyte Proliferation ◽

Wound Healing Activity ◽

Stimulation Of

Conyza canadensis (L.) Cronquist (CCL) has been used by K’Ho minority in Bidoup Nui Ba national park, Lam Dong province, Vietnam as one of wound healing remedies. However, the scientific proof of treatment is still unclear. This study aimed to evaluate this wound healing potential of CCL. CCL power was extracted by ethanol and then partitioned consecutively with petroleum ether, ethyl acetate and water. Wound healing potential was evaluated by antibacterial activity, stimulation of fibroblast and keratinocyte proliferation. Agar-well diffusion was used in the antibacterial tests and the results showed that CCL had antibacterial activity against 02 dermatitis bacteria (Pseudomonas aeruginosa, Staphylococcus aureus) and 02 opportunistic infection bacteria (Escherichia coli, Enterococcus faecalis). Moreover, our results illustrated that CCL stimulated the fibroblast and keratinocyte proliferation compared to the control. Particularly, the fibroblast division increased 1.6 times at 31.25 µg/mL when treated by ethanolic extract, while ethyl acetate fraction showed 1.7 times increase at 10 µg/mL in keratinocyte proliferation compared to the control. Taken together, our study contributed scientific base of CCL in the wound healing.

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Novel benzofurane-pyrazole derivatives with anti-inflammatory, cyclooxygenase inhibitory and cytotoxicity evaluation

Zeitschrift für Naturforschung C ◽

10.1515/znc-2021-0217 ◽

2022 ◽

Vol 0 (0) ◽

Author(s):

Zafer Sahin ◽

Yağmur Özhan ◽

Hande Sipahi ◽

Sevde Nur Biltekin ◽

Leyla Yurttaş ◽

...

Keyword(s):

Hydroxy Ketone ◽

No Production ◽

Raw 264.7 ◽

Pyrazole Derivatives ◽

H Nmr ◽

Pyrazolone Derivatives ◽

Cox 2 ◽

Anti Inflammatory ◽

Cox 1 ◽

C Nmr

Abstract Novel benzofurane-pyrazolone hybrids have been synthesized for evaluating their anti-inflammatory and cytotoxic properties. 4-(2-chloroacetyl)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one were reacted with α-hydroxy aldehyde or α-hydroxy ketone derivatives to obtain nine novel pyrazolone derivatives. Structures were successfully elucidated by 1H NMR, 13C NMR, IR and HRMS. Enzyme inhibitory activity was measured on cyclooxygenases (COXs) as considered to address anti-inflammatory activity. Compound 2 showed the highest activity on both COX-1 and COX-2 subtypes with 12.0 μM and 8.0 μM IC50, respectively. This activity was found close to indomethacin COX-2 inhibition measured as 7.4 μM IC50. Rest of the compounds (1, 3–9) showed 10.4–28.1 μM IC50 on COX-2 and 17.0–35.6 μM IC50 on COX-1 (Compound 1 has no activity on COX-1). Tested compounds (1–9) showed activity on NO production. Only compound was the 4, which showed a low inhibition on IL-6 levels. Cell viability was up to 60% at 100 μM for all compounds (1–9) on RAW 264.7 and NIH3T3 cell lines, thus compounds were reported to be noncytotoxic.

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ANTI-INFLAMMATORY ACTIVITY OF BACTERIA ASSOCIATED WITH MARINE SPONGE (HALICLONA AMBOINENSIS) VIA REDUCTING NO PRODUCTION AND INHIBITING CYCLOOXYGENASE-1, CYCLOOXYGENASE-2, AND SECRETORY PHOSPHOLIPASE A2 ACTIVITIES

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2017.v10i11.20094 ◽

2017 ◽

Vol 10 (11) ◽

pp. 95 ◽

Cited By ~ 1

Author(s):

Yosie Andriani ◽

Leni Marlina ◽

Habsah Mohamad ◽

Hermansyah Amir ◽

Siti Aisha M Radzi ◽

...

Keyword(s):

Methanol Extract ◽

Inflammatory Activity ◽

No Production ◽

Secretory Phospholipase A2 ◽

Phytochemical Screening ◽

Spla2 Activity ◽

Cyclooxygenase 1 ◽

Cox 2 ◽

Anti Inflammatory ◽

Cox 1

Objective: This study aimed to investigate the anti-inflammatory activity of methanol extract and fractions of bacteria associated with sponge (Haliclona amboinensis) and to evaluate their effect in reducing NO production and inhibiting cyclooxygenase-1 (COX-1), cyclooxgenase-2 (COX-2) and secretory phospholipase A2 (sPLA2) activity.Methods: All bacterial isolates were cultured and supernatants were collected for the extraction of secondary metabolites using diaion HP-20 to obtain methanol extracts. Evaluation of cytotoxicity property was carried out on macrophage cell lines (RAW264.7) by 3-(4,5-dimethylthiazol- 2-yl) 2,5-diphenyl tetrazoliumbromide assay. Anti-inflammatory screening was done by inducible nitric oxide assay on RAW264.7 cell lines with lipopolysaccharide (LPS) stimulation. Dianion HP-20 was used to remove salt content. A selected methanol extract was subjected to further fractionations by C-18 reverse phase and their anti-inflammatory potential was evaluated by COX-1 and COX-2, and sPLA2 enzymatic assay.Results: Seven methanol extracts showed no cytotoxic property against RAW 264.7 cell line (inhibitory concentration 50% > 30 μg/ml) and selected for anti-inflammatory screening assay. Result showed methanol extract HM 1.2 reduced NO production >80% and it has been selected for phytochemical screening, further fractionations and assay. Phytochemical screening showed alkaloids and terpenoids present in the HM 1.2. The HM 1.2 and its fractions (F1, F2, F1C1, F1C2, F1C3, and F1C4) were proven to inhibit COX-1, COX-2, and sPLA2 activity in the range of 60.516-116.886%, 20.554- 116.457%, and 70.2667-114.8148%, respectively.Conclusions: This study revealed that bacteria associated with H. amboinensis have produced anti-inflammatory activity via reducing NO production and inhibiting COX-1, COX-2, and sPLA2 activity.

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Non-alkaloid Constituents from Mahonia bealei

Natural Product Communications ◽

10.1177/1934578x1701201024 ◽

2017 ◽

Vol 12 (10) ◽

pp. 1934578X1701201

Author(s):

Bui Van Thanh ◽

Nguyen Thi Van Anh ◽

Do Hoang Giang ◽

Nguyen Hai Dang ◽

Luu Dam Ngoc Anh ◽

...

Keyword(s):

Ethyl Acetate ◽

Ethyl Acetate Fraction ◽

Spectroscopic Methods ◽

Phytochemical Investigation ◽

Mahonia Bealei ◽

New Compounds

A phytochemical investigation of an ethyl acetate fraction of Mahonia bealei trunks led to the isolation of three new and four known compounds. By means of NMR and MS spectroscopic methods, the structure of the new compounds was elucidated as bishexadecyl epiphyllate (1), 3-(4-hydroxy-3,5-dimethoxyphenyl)-3-ethoxy-2-sulfopropane-1-ol (2), and 6α-acetoxystigmastan-3β-ol (3).

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Flavonoids from Acacia pennata and their Cyclooxygenase (COX-1 and COX-2) Inhibitory Activities

Planta Medica ◽

10.1055/s-2007-981596 ◽

2007 ◽

Vol 73 (11) ◽

pp. 1202-1207 ◽

Cited By ~ 13

Author(s):

Alain Dongmo ◽

Tomofumi Miyamoto ◽

Kazuko Yoshikawa ◽

Shigenobu Arihara ◽

Marie-Aleth Lacaille-Dubois

Keyword(s):

Inhibitory Activities ◽

Cox 2 ◽

Cox 1

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Immunomodulatory Activity of Phyllanthus maderaspatensis in LPS-Stimulated Mouse Macrophage RAW 264.7 Cells

Separations ◽

10.3390/separations8090129 ◽

2021 ◽

Vol 8 (9) ◽

pp. 129

Author(s):

Uoorakkottil Ilyas ◽

Deepshikha P. Katare ◽

Punnoth Poonkuzhi Naseef ◽

Mohamed Saheer Kuruniyan ◽

Muhammed Elayadeth-Meethal ◽

...

Keyword(s):

Nitric Oxide ◽

Liquid Chromatography ◽

Ethyl Acetate ◽

Ethyl Acetate Fraction ◽

Raw 264.7 Cells ◽

Immunomodulatory Activity ◽

No Production ◽

Raw 264.7 ◽

Mouse Macrophage ◽

Significant Stimulatory Effect

Phyllanthus species (Family Euphorbiaceae) has been used in traditional medicine of several countries as a cure for numerous diseases, including jaundice and hepatitis. This study is an attempt to evaluate the immunomodulatory activity of various fractions, column eluents of ethyl acetate fraction, and their polyphenols. Phyllanthus maderaspatensis were standardized using high-performance liquid chromatography to identify and quantify polyphenols, and purification of polyphenols was carried out using vacuum liquid chromatography. Subsequently, we tested various fractions, column eluents of ethyl acetate fraction, and polyphenols in vitro to assess their impact on nitric oxide (NO) production in LPS-stimulated mouse macrophage RAW 264.7 cells. The ethyl acetate fraction (100 μg mL−1) had a more significant stimulatory effect on LPS-stimulated NO production by the RAW 264.7 cells. We found that the ethyl acetate fraction contains a high amount of catechin, quercetin, ellagic acid kaempferol, and rutin, which are responsible for immunomodulation. The ethyl acetate fraction at concentrations of 25 and 50 μg mL−1 had a significant inhibitory effect and 100 μg mL−1 had a more significant stimulatory effect when compared with the LPS control. The percentage of inhibition by LPS control ranged from zero percentage, kaempferol ranged from 45.4% at 50 μg mL−1 to 41.88% at 100 μg mL−1, catechin ranged from 50% at 50 μg mL−1 to 35.28% at 100 μg mL−1, rutin ranged from 36.2% at 50 μg mL−1 to 47.44% at 100 μg mL−1, gallic acid ranged from 28.4% at 50 μg mL−1 to 50.9% at 100 μg mL−1, ellagic acid ranged from 45.12% at 50 μg mL−1 to 38.64% at 100 μg mL−1, and purified quercetin ranged from 26.2% at 50 μg mL−1to 45.48% at 100 μg mL−1. As NO plays an important role in the immune function, polyphenols’ treatment could modulate several aspects of host defense mechanisms owing to the stimulation of the inducible nitric oxide synthase.

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Anti-Inflammatory Flavonolignans from Triticum aestivum Linn. Hull

Applied Sciences ◽

10.3390/app10238656 ◽

2020 ◽

Vol 10 (23) ◽

pp. 8656

Author(s):

Ah-Reum Han ◽

Yun-Seo Kil ◽

Min Jeong Hong ◽

Jisu Park ◽

Hyeon Hwa Park ◽

...

Keyword(s):

Triticum Aestivum ◽

Crop Production ◽

Ethyl Acetate Fraction ◽

Inhibitory Effect ◽

Raw 264.7 Cells ◽

No Production ◽

Phytochemical Investigation ◽

Ic50 Values ◽

Anti Inflammatory ◽

Food Grain

Wheat (Triticum aestivum Linn.; Poaceae) is a very common and important food grain and ranks second in total cereal crop production. A large amount of wheat hull is produced after threshing that, as the non-food part of wheat, is agro-waste, accounting for 15~20% of the wheat. This study aimed at biologically and phytochemically investigating wheat hull for its valorization as a by-product. In our ongoing search for natural product-derived anti-inflammatory agents, T. aestivum hull was evaluated for its nitric oxide (NO) production inhibition in lipopolysaccharide (LPS)-activated RAW 264.7 cells, and the phytochemical investigation of the ethyl acetate fraction showing inhibitory effect led to the isolation of a flavone (1) and seven flavonolignans (2–8). Compounds 2–8 have not yet been isolated from Triticum species. All compounds were evaluated for their LPS-induced NO production inhibition, and 1, 2, 4, 6, and 8 exhibited inhibitory effects with IC50 values ranging from 24.14 to 58.95 μM. These results suggest the potential of using T. aestivum hull as a source for producing anti-inflammatory components, enhancing its valorization as a by-product.

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Ethyl Acetate Fraction of Lannea microcarpa Engl. and K. Krause (Anacardiaceae) Trunk Barks Corrects Angiotensin II-Induced Hypertension and Endothelial Dysfunction in Mice

Oxidative Medicine and Cellular Longevity ◽

10.1155/2019/9464608 ◽

2019 ◽

Vol 2019 ◽

pp. 1-13

Author(s):

Mathieu Nitiéma ◽

Raffaella Soleti ◽

Camille Koffi ◽

Lazare Belemnaba ◽

Patricia Mallegol ◽

...

Keyword(s):

Ethyl Acetate ◽

Vascular Function ◽

Ex Vivo ◽

Nicotinamide Adenine Dinucleotide Phosphate ◽

Ethyl Acetate Fraction ◽

Bark Extract ◽

Phytochemical Analysis ◽

Ang Ii ◽

Induced Hypertension ◽

Cox 2

Traditional remedies prepared from Lannea microcarpa leaves, barks, roots, and fruits are used to treat many diseases including hypertension. This study investigated whether oral administration of the ethyl acetate fraction of Lannea microcarpa trunk barks (LMAE) corrects angiotensin (Ang) II-induced hypertension in mice. Its effects on vascular function were specifically investigated. Experiments explored hemodynamic and echocardiographic parameters in vivo and vascular reactivity to acetylcholine (ACh) and CaCl2ex vivo on isolated aortas. Mice received LMAE for 3 weeks (50 mg/kg/day) by oral gavage. In the last two weeks of treatment, mice were implanted with osmotic minipumps delivering NaCl (0.9%) or Ang II (0.5 mg/kg/day). LMAE completely prevented the increase in systolic and diastolic blood pressure induced by Ang II. Echocardiographic and kidney parameters were not affected by the different conditions. LMAE abrogated Ang II-induced impairment of ACh-induced relaxation without affecting that of sodium nitroprusside. LMAE also completely prevented CaCl2-induced contraction in KCl-exposed aorta ex vivo. The extract alone did not modify superoxide (O2-) and nitric oxide (NO⋅) production in femoral arteries from control mice but significantly limited Ang II-induced O2- production. These effects were associated with reduced expression of inducible isoform of cyclooxygenase- (COX-) 2 and nicotinamide adenine dinucleotide phosphate (NADPH) oxidase isoform NOX-2 in aortas. Finally, phytochemical analysis showed that LMAE contains sterols, triterpenes, coumarins, and anthraquinone. These results showed that LMAE prevents Ang II-induced hypertension and vascular dysfunction through a reduction of oxidative stress linked to COX-2 and NOX-2 pathway and inhibition of calcium entry. This study provides pharmacological basis of the empirical use of Lannea microcarpa trunk bark extract against hypertension.

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