HIV latency-reversing activity of latex from (Pax) Bruyns and three diterpenes isolated from this species.

Two unusual phorbol esters, namely 20-deoxyphorbol-3,4,12-triacetate-13-phenylacetate () and phorbol-3,4,12,13-tetraacetate-20-phenylacetate () plus ingol-3,8,12-triacetate-7-phenylacetate () were isolated from the latex of and identified by HRESIMS and 2D NMR. Compound is herein described for the first time. Assignment of the phenylacetyl group at C-7 in compound was suggested by the HMBC and NOESY spectra obtained in pyridine-.

In vitro toxicity of latex, its terpenoidal fractions and isolated phorbol esters from Euphorbia umbellata (Pax) Bruyns on monocytic and melanoma cells.

In Brazil, latex from Euphorbia umbellata (African milk tree) has been increasingly used in folk medicine to treat several types of cancer, including melanoma. The effect of lyophilized latex (LL), its hydroethanolic extract (E80), triterpene (F-TRI)- and diterpene (F-DIT)-enriched fractions, along with six isolated phorbol esters from LL and phorbol 12-myristate 13-acetate (PMA) on J774A.1, THP-1, SK-MEL-28, and B16-F10 cell line viability were evaluated by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) method.

Antiviral and Virucidal Activities of (Cat's Claw) against the Chikungunya Virus.

(UT) is a medicinal plant popularly known as cat's claw belonging to the Rubiaceae family that has been reported to display antiviral and anti-inflammatory activities. The chikungunya virus (CHIKV) outbreaks constitute a Brazilian public health concern. CHIKV infection develops an abrupt onset of fever, usually accompanied by a skin rash, besides incapacitating polyarthralgia.

Production of perillic acid from orange essential oil by Yarrowia lipolytica using a top-aerated bioreactor.

R-(+)-Perillic acid, a promising anticancer and immunomodulatory agent, is the major product from the biotransformation of R-(+)-limonene-rich orange essential oil by the yeast Yarrowia lipolytica. Due to the abundance and low cost of orange essential oil, which is a byproduct of the citrus industry, we attempted to improve the biotransformation process by optimizing yeast cell mass production. Then, the whole process was transposed and adapted to a 2-L instrumented bioreactor.

Miconia albicans (Melastomataceae) to treat Chikungunya viral infection: An effectual symptom-driven ethnomedicinal repurposing of an anti-inflammatory species?

Ethnopharmacological Relevance: Miconia albicans (MA) is consumed all over the Brazilian territory as a remedy to treat rheumatoid arthritis and has been increasingly used to alleviate the deleterious symptoms caused by Chikungunya virus (CHIKV).

Aim Of The Study: To investigate the effect of MA leaf and stem hydroethanolic extracts (LE and SE, respectively), their fractions enriched in triterpene acids or polyphenols as well isolated constituents, on CHIKV hosted in Vero cells.

Materials And Methods: Polyphenol profiles of LE and SE were dereplicated by HPLC-DAD-ESI-MS/MS, aided by standards.

Phorbol Esters from the Latex of : Bioguided Isolation of Highly Potent HIV-1 Latency Interrupters in Virus Reservoir Cells.

Three known compounds, 20-deoxyphorbol-5-hydroxy-12-tiglate-13-isobutyrate (), 20-deoxyphorbol-5-hydroxy-12-tiglate-13-phenylacetate (), and 4-deoxy-4-phorbol-12-tiglate-13-phenylacetate (), were reisolated from the latex of through a bioguided fractionation process to target HIV-1 latency reactivation. The in vitro bioassay using infected T-cell lymphoblasts (J-Lat 10.6), complemented with surface CD4 receptor downregulation assessment, led to isolation of the compounds as a highly active ternary mixture.

In vitro leishmanicidal activity of monoterpenes present in two species of Protium (Burseraceae) on Leishmania amazonensis.

Ethnopharmacological Relevance: Leishmaniasis is a neglected disease that affects millions of people around the world. Parasite resistance and the toxicity to the current treatments lead to the search for new effective molecules. Plants are widely used in traditional and indigenous medicine to treat different diseases.

Reactivation of latent HIV-1 in vitro using an ethanolic extract from Euphorbia umbellata (Euphorbiaceae) latex.

Euphorbia umbellata (E. umbellata) belongs to Euphorbiaceae family, popularly known as Janauba, and its latex contains a combination of phorbol esters with biological activities described to different cellular protein kinase C (PKC) isoforms. Here, we identified deoxi-phorbol esters present in E.

The in vitro antileishmanial activity of essential oil from Aloysia gratissima and guaiol, its major sesquiterpene against Leishmania amazonensis.

Leishmaniases is a tropical disease caused by protozoa of the genus Leishmania for which the current treatment is expensive, besides increasing reports of parasite resistance. This study investigated the anti-Leishmania amazonensis activity of the essential oil from Aloysia gratissima (AgEO) and guaiol, the major sesquiterpene constituent in the oil. Our results showed that AgEO killed promastigotes and intracellular amastigotes at an IC50 of 25 and 0·16 µg mL-1, respectively, while guaiol killed amastigotes at an IC50 of 0·01 µg mL-1.

Decrease in Dengue virus-2 infection and reduction of cytokine/chemokine production by Uncaria guianensis in human hepatocyte cell line Huh-7.

Background: Dengue fever may present hemorrhages and cavitary effusions as result of exacerbated immune responses. We investigated hydro-alcoholic extracts from leaves (UGL) and bark (UGB) of the medicinal species Uncaria guinanensis with respect to antiviral effects in Dengue virus (DENV) infection and in immunological parameters associated with in vivo physiopathological features.

Methods: Chemical profiles from UGB or UGL were compared in thin layer chromatography and 1H nuclear magnetic resonance using flavonoid compounds and a pentacyclic oxindole alkaloid-enriched fraction as references.

Selective and cost-effective protocol to separate bioactive triterpene acids from plant matrices using alkalinized ethanol: Application to leaves of Myrtaceae species.

Background: Triterpenes as betulinic (BA), oleanolic (OA) and ursolic acids (UA) have increasingly gained therapeutic relevance due to their wide scope of pharmacological activities. To fit large-scale demands, exploitable sources of these compounds have to be found and simple, cost-effective methods to extract them developed. Leaf material represents the best plant sustainable raw material.

Production of antiretroviral drugs in middle- and low-income countries.

This review outlines the main issues concerning the production of antiretroviral (ARV) drugs in middle- and low-income countries and the relevant political, legal and technical requirements for supporting such production. The requirements for efficient local production, including the manufacture of generic and branded products and public demand, have been considered from economic, market and socio-political perspectives. A steady and consistent government policy is crucial to success.

Efficiency and selectivity of triterpene acid extraction from decoctions and tinctures prepared from apple peels.

Background: This study assessed the extraction efficiency of ursolic (UA) and oleanolic acids (OA), as well as the total phenols in aqueous and hydroethanolic extracts of dry apple peels at room temperature.

Materials And Methods: AFTER RUNNING PRELIMINARY ASSAYS ON DECOCTIONS AND TINCTURES (ETHANOL: water 7:3 v/v), the extracts from dried apple (cv. Fuji) peels were obtained by static maceration over varied intervals (2 to 180 days).

Anti-inflammatory effects of methyl ursolate obtained from a chemically derived crude extract of apple peels: potential use in rheumatoid arthritis.

Ursolic acid (UA), a pentacyclic triterpene acid found in apple peels (Malus domestica, Borkh, Rosaceae), has a large spectrum of pharmacological effects. However, the vegetal matrix usually produces highly viscous and poorly soluble extracts that hamper the isolation of this compound. To overcome this problem, the crude EtOH-AcOEt extract of commercial apple peels was exhaustively treated with diazomethane, after which methyl ursolate (MU) was purified by column chromatography and characterized spectrometrically.

Bioconversion of R-(+)-limonene to perillic acid by the yeast Yarrowia lipolytica.

Perillyl derivatives are increasingly important due to their flavouring and antimicrobial properties as well as their potential as anticancer agents. These terpenoid species, which are present in limited amounts in plants, may be obtained via bioconversion of selected monoterpene hydrocarbons. In this study, seventeen yeast strains were screened for their ability to oxidize the exocyclic methyl group in the p-menthene moiety of limonene into perillic acid.

Uncaria tomentosa alkaloidal fraction reduces paracellular permeability, IL-8 and NS1 production on human microvascular endothelial cells infected with dengue virus.

Dengue is the major Arbovirus in the world, annually causing morbidity and death. Severe dengue is associated with changes in the endothelial barrier function due to the production of inflammatory mediators by immune cells and by the endothelium. Dengue virus (DENV) replicates efficiently in human endothelial cells in vitro and elicits immune responses resulting in endothelial permeability.

Trans- β -Caryophyllene: An Effective Antileishmanial Compound Found in Commercial Copaiba Oil (Copaifera spp.).

This study investigated the leishmanicidal activity against Leishmania amazonensis of four commercial oils from Copaifera spp. named as C1, C2, C3, and C4, the sesquiterpene and diterpene pools obtained from distilling C4, and isolated β -caryophyllene (CAR). Copaiba oils chemical compositions were analyzed by gas chromatography and correlated with biological activities.

Anti-inflammatory activity of essential oils from Syzygium cumini and Psidium guajava.

Context: Despite the many biological activities reported for essential oils, their anti-inflammatory ability is relatively underexplored considering the wide variation in plant sources and in their volatile composition. Oils from Syzygium cumini Skells (SC) and Psidium guajava L. (PG) (Myrtaceae) have been described as having diverse pharmacological activities.

Flavonoids bearing an O-arabinofuranosyl-(1-->3)-rhamnoside moiety from Cladocolea micrantha: inhibitory effect on human melanoma cells.

Eleven known triterpenes (alpha-amyrin, beta-amyrin, lupeol, and their respective acetates, 3-O-acetyl derivatives of betulinic, oleanolic, and ursolic acids, cycloartenol, and tirucall-7,24-dienol), two new flavonols presenting an uncommon interglycosidic O-(1-->3) linkage (kaempferol 3-O-alpha-L-arabinofuranosyl(1-->3)-alpha-L-rhamnoside and quercetin 3-O-alpha-L-arabinofuranosyl-(1-->3)-alpha-L-rhamnoside), beta-sitosterol, stigmasterol, quercetin, and gallic acid were isolated from the Amazonian medicinal mistletoe, Cladocolea micrantha Kuijt (Loranthaceae). Their structures were established by spectral methods and eventual chromatographic comparisons. The quercetin derivative was not cytotoxic to MV3 human melanoma cells, but was able, when administered at 1 microg/mL, to promote a twofold inhibition of the migration of the cells through the transwell system when compared with paclitaxel at 5 microM.

Prevention of experimental diabetes by Uncaria tomentosa extract: Th2 polarization, regulatory T cell preservation or both?

Ethnopharmacological Relevance: Uncaria tomentosa (Willd.) DC (Rubiaceae) is a species native to the Amazon rainforest and surrounding tropical areas that is endowed with immunomodulatory properties and widely used around the world. In this study we investigated the immunomodulatory potential of Uncaria tomentosa (UT) aqueous-ethanol extract on the progression of immune-mediated diabetes.

Uncaria tomentosa aqueous-ethanol extract triggers an immunomodulation toward a Th2 cytokine profile.

Uncaria tomentosa (Willd.) DC (Rubiaceae) is a large woody vine that is native to the Amazon and Central American rainforests and is used widely in traditional medicine for its immunomodulatory and antiinflammatory activities. The present work used in vivo immunotoxic and in vitro immunomodulatory experiments to investigate the effects of a pentacyclic oxindole alkaloid extract from U.

[Chaulmoogra oil as scientific knowledge: the construction of a treatment for leprosy].

The article investigates how knowledge of medicinal plants and related treatment practices are assimilated and transformed. Taking as its focus the use of chaulmoogra oil to treat leprosy, it examines how information on this plant was incorporated and transformed into scientifically validated knowledge when 'Brazilian chaulmoogra' came onto the scene. Pointing to the addition of chaulmoogra byproducts to the Instituto Oswaldo Cruz's production agenda in the 1920s, the study establishes links between productive processes and relates these to the period's scientific context.

Development of an HPLC method for the determination of tetranortriterpenoids in Carapa guianensis seed oil by experimental design.

Carapa guianensis crabwood, popularly known in Brazil as "andiroba", is a tree that grows in South and Central America and is used by the local population mainly for its anti-inflammatory and insect anti-feeding activities. Scientific studies on this plant have led to the development of an insect-repellent candle and the investigations of the anti-inflammatory properties of its more important biomarkers-tetranortriterpenoids. These compounds, together with glycerides and fatty acids, are present in the seed oil, the most important commercial product from this plant.

Immunomodulating and antiviral activities of Uncaria tomentosa on human monocytes infected with Dengue Virus-2.

Uncaria tomentosa (Willd.) DC., a large woody vine native to the Amazon and Central American rainforests has been used medicinally by indigenous peoples since ancient times and has scientifically proven immunomodulating, anti-inflammatory, cytotoxic and antioxidant activities.

Inhibition of allergen-induced eosinophil recruitment by natural tetranortriterpenoids is mediated by the suppression of IL-5, CCL11/eotaxin and NFkappaB activation.

The present study reports the anti-allergic activity of a group of six different tetranortriterpenoids (TNTP) isolated from the seeds of Carapa guianensis Aublet: 6a-acetoxygedunin, 7-deacetoxy-7-oxogedunin, andirobin, methyl angolensate, 6a-acetoxyepoxyazadiradione and gedunin. Oral pretreatment with TNTP significantly inhibited total leukocyte and eosinophil accumulation in C57BL/10 mice pleural cavities 24 h after the intrathoracic (i.t.