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1.
Chin J Nat Med ; 19(9): 686-692, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34561080

RESUMO

Six new tirucallane-type triterpenoids (1-6), along with ten known triterpenoids, were isolated from methylene chloride extract of the resin of Boswellia carterii Birdw. By the application of the comprehensive spectroscopic data, the structures of the compounds were clarified. The experimental electronic circular dichroism spectra were compared with those calculated, which allowed to assign the absolute configurations. Compounds 5 and 6 possesed a 2, 3-seco tirucallane-type triterpenoid skeleton, which were first reported. Their inhibitory activity against NO formation in LPS-activated BV-2 cells were evaluated. Compound 9 showed appreciable inhibitory effect, with an IC50 value of 7.58 ± 0.87 µmol·L-1.


Assuntos
Boswellia , Triterpenos , Estrutura Molecular , Resinas Vegetais , Triterpenos/farmacologia
2.
J Egypt Natl Canc Inst ; 33(1): 20, 2021 Aug 09.
Artigo em Inglês | MEDLINE | ID: mdl-34368899

RESUMO

BACKGROUND: Globally, head and neck cancer is the sixth most common cancer. Despite the advancement in treatment, drug resistance remains a major cause for setback. In an earlier work, the authors reported that Boswellia dalzielii (Hutch) stem bark exhibited dose-dependent cytotoxicity in head and neck cancer cells, AW8507. Therefore, the cell death induction effect of Boswellia dalzielii stem bark chloroform extract in head and neck cancer cell line, AW8507, and its derived constituent on cell cycle and apoptosis proteins was further investigated. METHODS: The cell death induction activity of the Boswellia dalzielii stem bark chloroform fraction (CLBD) in AW8507 was determined using Annexin V-FITC/PI staining in flow cytometry. High-performance liquid chromatography-mass spectrometry was employed for compounds analysis of the CLBD, and reverse virtual screening was used to identify the mechanism of action of the compound, acetyl-11-keto-beta-boswellic acid, that was elucidated in the Boswellia dalzielii chloroform fraction. RESULTS: The data obtained showed that Boswellia dalzielii stem bark Chloroform extract increased the percentage of cells presenting for early apoptosis from 4.14 to 10.10% in AW8507 cells. High-performance liquid chromatography-mass spectrometry analysis of the chloroform fraction identified acetyl-11-keto-beta-boswellic acid. Reverse virtual screening on selected proteins showed that acetyl-11-keto-beta-boswellic acid is a multi-protein target compound. It binds preferably to phosphorylated-cyclin dependent kinase 1 (p-CDK1) (binding score = - 9.2 kcal/mol), blocking the activation of cyclin B-CDK1 needed for cell cycle progression at G2/M phase of the cell cycle. Acetyl-11-keto-beta-boswellic acid also binds more tightly with αß tubulin (binding score = 8.9 kcal/mol) than with the standard drug, docetaxel (binding score = 8.3 kcal/mol). CONCLUSIONS: The results obtained confirmed the culpability of Boswellia dalzielii-derived acetyl-11-keto-beta-boswellic acid in the obstruction of the cell cycle progression in head and neck cancer cell line, AW8507; and the induction of apoptosis earlier reported for Boswellia dalzielii (Hutch) stem bark. Additional in vitro and/or in vivo studies would be required to validate in silico observations.


Assuntos
Boswellia , Apoptose , Ciclo Celular , Divisão Celular , Clorofórmio , Humanos , Casca de Planta , Extratos Vegetais/farmacologia , Triterpenos
3.
Phytochemistry ; 191: 112897, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-34412004

RESUMO

Frankincense of Boswellia species has long been used in traditional medicines, mainly for its interesting anti-inflammatory and anti-depressant properties of its di- and triterpenes. Boswellic acids (triterpenes) and cembranoids (diterpenes) are the major constituents of frankincense from all reported species which are responsible for the overall biological activity of frankincense. Boswellic acids have been thoroughly investigated for decades but cembranoids have attracted considerable attention only recently, and a good number of publications have highlighted the important role of these 14-membered rings in contributing to the superior anti-inflammatory activity of the sacred resin. Partial and total syntheses of some cembranoids from frankincense have been reported. Their therapeutic potential is not limited to the well proven anti-inflammatory activity but also to their recently reported anti-depressant properties. There is a considerable number of publications in the field of cembranoids of Boswellia species where we feel a review in this topic will be of interest to the readership of Phytochemistry. In this article we have discussed the chemistry (isolation and chemical structures as well as synthetic studies), biogenesis and bioactivity of the reported cembranoids of Boswellia species. The structural discrepancies due to wrongly assigned structures of some cembranoids have been highlighted and corrected. We have covered the related literature up to the end of 2020.


Assuntos
Boswellia , Franquincenso , Triterpenos , Anti-Inflamatórios/farmacologia , Fatores Imunológicos , Resinas Vegetais , Triterpenos/farmacologia
4.
Fitoterapia ; 154: 105017, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34418492

RESUMO

One undescribed tetracyclic triterpene (boswellicarin A), four undescribed pentacyclic triterpenes (boswellicarterins A-C) and one undescribed prenylaromadendrane-type diterpene (boscarterin A) were isolated from the gum resin of Boswellia carterii Birdw. (Burseraceae). Their structures were elucidated from NMR and HRESIMS spectroscopic data and ECD spectra. Boswellicarterins A-C and boscarterin A displayed weak and selective cytotoxicity against three human cancer cells (HepG2, A549 and MCF-7) by MTT assay.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Boswellia/química , Terpenos/farmacologia , Células A549 , Antineoplásicos Fitogênicos/isolamento & purificação , Células Hep G2 , Humanos , Células MCF-7 , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Resinas Vegetais/química , Terpenos/isolamento & purificação
5.
Arch Pharm (Weinheim) ; 354(11): e2100160, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-34427335

RESUMO

Boswellic acids (BAs) have been shown to possess antiviral activity. Using bioinformatic methods, it was tested whether or not acetyl-11-keto-ß-boswellic acid (AKBA), 11-keto-ß-boswellic acid (KBA), ß-boswellic acid (BBA), and the phosphorylated active metabolite of Remdesivir® (RGS-P3) bind to functional proteins of SARS-CoV-2, that is, the replicase polyprotein P0DTD1, the spike glycoprotein P0DTC2, and the nucleoprotein P0DTC9. Using P0DTD1, AKBA and KBA showed micromolar binding affinity to the RNA-dependent RNA polymerase (RdRp) and to the main proteinase complex Mpro . Phosphorylated BAs even bond in the nanomolar range. Due to their positive and negative charges, BAs and RGS-P3 bond to corresponding negative and positive areas of the protein. BAs and RGS-P3 docked in the tunnel-like cavity of RdRp. BAs also docked into the elongated surface rim of viral Mpro . In both cases, binding occurred with active site amino acids in the lower micromolecular to upper nanomolar range. KBA, BBA, and RGS-P3 also bond to P0DTC2 and P0DTC9. The binding energies for BAs were in the range of -5.8 to -6.3 kcal/mol. RGS-P3 and BAs occluded the centrally located pore of the donut-like protein structure of P0DTC9 and, in the case of P0DTC2, RGS-P3 and BAs impacted the double-wing-like protein structure. The data of this bioinformatics study clearly show that BAs bind to three functional proteins of the SARS-CoV-2 virus responsible for adhesion and replication, as does RGS-P3, a drug on the market to treat this disease. The binding effectiveness of BAs can be increased through phosphate esterification. Whether or not BAs are druggable against the SARS-CoV-2 disease remains to be established.


Assuntos
Monofosfato de Adenosina/análogos & derivados , Alanina/análogos & derivados , COVID-19 , SARS-CoV-2 , Glicoproteína da Espícula de Coronavírus/fisiologia , Triterpenos/farmacologia , Proteínas Virais/fisiologia , Monofosfato de Adenosina/farmacologia , Alanina/farmacologia , Anti-Inflamatórios não Esteroides/farmacologia , Antivirais/farmacologia , Sítios de Ligação/fisiologia , Boswellia , COVID-19/tratamento farmacológico , COVID-19/virologia , Biologia Computacional/métodos , Humanos , Simulação de Acoplamento Molecular , Nucleoproteínas/metabolismo , Poliproteínas/metabolismo , Pró-Fármacos/farmacologia , Ligação Proteica/fisiologia , SARS-CoV-2/efeitos dos fármacos , SARS-CoV-2/fisiologia , Relação Estrutura-Atividade
6.
Environ Monit Assess ; 193(8): 497, 2021 Jul 20.
Artigo em Inglês | MEDLINE | ID: mdl-34286386

RESUMO

In the present work, leaf extract of Boswellia sacra was used as reductant for synthesis of silver nanoparticles (AgNPs). The variables such as volume of Boswellia sacra leaf extract (1%), volume of silver nitrate (1 mM), and temperature were optimized by response surface methodology via Box-Behnken design for the synthesis of AgNPs. Design-Expert software generated the optimum conditions for the highest yield of silver nanoparticles as 8 mL of 1 mM AgNO3, 8 mL of 1% Boswellia sacra leaf extract, and temperature = 55 °C. The formed AgNPs were isolated and purified by centrifugation process using ethanol/ distilled water. AgNPs were characterized using FTIR, SEM, TEM, EDX, and XRD. AgNPs showed surface plasmon resonance absorption band at 422 nm. XRD pattern indicated the crystalline nature of the particles (diameter 11.17 to 37.50 nm) with face-centered cubic structure. SEM and TEM images highlighted the formation of spherical AgNPs. The energy dispersive spectroscopic spectrum confirmed the presence of elemental silver. The microbial activity of AgNPs was evaluated against bacteria and fungi. Synthesized AgNPs were very effective against Gram-positive E. coli bacterial strains and fungal strains (Penicillium chrysogenum).


Assuntos
Boswellia , Nanopartículas Metálicas , Antibacterianos , Monitoramento Ambiental , Escherichia coli , Testes de Sensibilidade Microbiana , Extratos Vegetais , Prata
7.
Inflammopharmacology ; 29(4): 1033-1048, 2021 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-34224069

RESUMO

The most severe cases of COVID-19, and the highest rates of death, are among the elderly. There is an urgent need to search for an agent to treat the disease and control its progression. Boswellia serrata is traditionally used to treat chronic inflammatory diseases of the lung. This review aims to highlight currently published research that has shown evidence of potential therapeutic effects of boswellic acids (BA) and B. serrata extract against COVID-19 and associated conditions. We reviewed the published information up to March 2021. Studies were collected through a search of online electronic databases (academic libraries such as PubMed, Scopus, Web of Science, and Egyptian Knowledge Bank). Several recent studies reported that BAs and B. serrata extract are safe agents and have multiple beneficial activities in treating similar symptoms experienced by patients with COVID-19. Because of the low oral bioavailability and improvement of buccal/oral cavity hygiene, traditional use by chewing B. serrata gum may be more beneficial than oral use. It is the cheapest option for a lot of poorer people. The promising effect of B. serrata and BA can be attributed to its antioxidant, anti-inflammatory, immunomodulatory, cardioprotective, anti-platelet aggregation, antibacterial, antifungal, and broad antiviral activity. B. serrata and BA act by multiple mechanisms. The most common mechanism may be through direct interaction with IκB kinases and inhibiting nuclear factor-κB-regulated gene expression. However, the most recent mechanism proposed that BA not only inhibited the formation of classical 5-lipoxygenase products but also produced anti-inflammatory LOX-isoform-selective modulators. In conclusion a small to moderate dose B. serrata extract may be useful in the enhancing adaptive immune response in mild to moderate symptoms of COVID-19. However, large doses of BA may be beneficial in suppressing uncontrolled activation of the innate immune response. More clinical results are required to determine with certainty whether there is sufficient evidence of the benefits against COVID-19.


Assuntos
Anti-Inflamatórios não Esteroides/uso terapêutico , Boswellia , COVID-19/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Triterpenos/uso terapêutico , Idoso , Anti-Inflamatórios não Esteroides/isolamento & purificação , COVID-19/imunologia , COVID-19/fisiopatologia , Humanos , Extratos Vegetais/isolamento & purificação , Triterpenos/isolamento & purificação
8.
Molecules ; 26(9)2021 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-34062884

RESUMO

Osteoporosis is a systemic metabolic bone disorder that is caused by an imbalance in the functions of osteoclasts and osteoblasts and is characterized by excessive bone resorption by osteoclasts. Targeting osteoclast differentiation and bone resorption is considered a good fundamental solution for overcoming bone diseases. ß-boswellic acid (ßBA) is a natural compound found in Boswellia serrata, which is an active ingredient with anti-inflammatory, anti-rheumatic, and anti-cancer effects. Here, we explored the anti-resorptive effect of ßBA on osteoclastogenesis. ßBA significantly inhibited the formation of tartrate-resistant acid phosphatase-positive osteoclasts induced by receptor activator of nuclear factor-B ligand (RANKL) and suppressed bone resorption without any cytotoxicity. Interestingly, ßBA significantly inhibited the phosphorylation of IκB, Btk, and PLCγ2 and the degradation of IκB. Additionally, ßBA strongly inhibited the mRNA and protein expression of c-Fos and NFATc1 induced by RANKL and subsequently attenuated the expression of osteoclast marker genes, such as OC-STAMP, DC-STAMP, ß3-integrin, MMP9, ATP6v0d2, and CtsK. These results suggest that ßBA is a potential therapeutic candidate for the treatment of excessive osteoclast-induced bone diseases such as osteoporosis.


Assuntos
Tirosina Quinase da Agamaglobulinemia/metabolismo , Reabsorção Óssea , Regulação da Expressão Gênica , Osteoclastos/metabolismo , Fosfolipase C gama/metabolismo , Ligante RANK , Triterpenos/farmacologia , Animais , Boswellia , Diferenciação Celular , Técnicas de Cocultura , Masculino , Camundongos , Camundongos Endogâmicos ICR , NF-kappa B/metabolismo , Osteoblastos/metabolismo , Osteogênese/efeitos dos fármacos , Osteoporose/metabolismo , Fosforilação , Transdução de Sinais
9.
Sci Total Environ ; 785: 147384, 2021 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-33933775

RESUMO

Boswellic acid (BA) is a pentacyclic terpenoid derived from the gum-resin of Boswellia serrate. It is known for its strong antioxidant, anti-inflammatory, and anticancer properties. It has improved spatial learning and provides neuroprotection against trimethyltin-induced memory impairment. The aim of this study is to evaluate the possible neuroprotective activity of B. serrata extract (BSE) containing BA against fipronil (FPN)-induced neurobehavioral toxicity in Wister male albino rats. Sixty male rats were allocated equally into six groups. The first group served as control; the second and third groups received BSE at two different oral doses (250 or 500 mg/kg body weight [BW], respectively). The fourth group was orally intoxicated with FPN (20 mg/kg BW), whereas the fifth and sixth groups served as preventive groups and co-treated with FPN (20 mg/kg BW) and BSE (250 or 500 mg/kg BW, respectively). The experiment was conducted over 8 weeks period. Results revealed that co-treatment with BSE led to significant (p > 0.05) dose-dependent reduction in malondialdehyde (MDA), nitric oxide (NO), interleukin-6 (IL6), tumor necrosis factors-alpha (TNF-α), nuclear factor Kappa-B (NF-κB), Cyclooxegenase-2 (COX-2), prostaglandin E2 (PGE2), serotonin, and acetylcholine (ACh). Conversely, significant (p > 0.05) up regulation of catalase (CAT), glutathione peroxidase (GSH-Px), gamma-aminobutyric acid (GABA), and acetylcholine esterase (AChE) has reported in BSE-co-treated groups. In addition, significant (p > 0.05) promotion in neurobehaviours, histopathologic imaging of the cerebral, cerebellar, and hippocampal regions, and immunohistochemical expression of caspase-3 and glial fibrillary acidic protein (GFAP) were also reported in the BSE-treated groups in a dose-dependent manner. In conclusion, BSE (500 mg/kg BW) is a natural, promising neuroprotective agent that can mitigate FPN-induced neurobehavioral toxicity via the suppression of oxidative, inflammatory, and apoptotic pathways and relieve neuronal necrosis and astrogliosis.


Assuntos
Boswellia , Animais , Antioxidantes , Masculino , Necrose , Estresse Oxidativo , Extratos Vegetais/toxicidade , Pirazóis , Ratos
10.
Zhongguo Zhong Yao Za Zhi ; 46(9): 2215-2219, 2021 May.
Artigo em Chinês | MEDLINE | ID: mdl-34047123

RESUMO

This study aims to study the chemical components from the gum resin of Boswellia carterii. Five cembranoid diterpenes were isolated from the gum resin of B. carterii by various of column chromatographies including silica gel, Sephadex LH-20, and semi-preparative HPLC. Their structures were identified on the basis of physicochemical properties, mass spectrometry(MS), nuclear magnetic resonance(NMR), Ultraviolet(UV) and infrared(IR) spectroscopic data. These compounds were identified as(1S,2E,4R,5S,7E,11E)-4-methoxy-5-hydroxycembrane(1),(1R~*,4R~*,5E,8E,12E,15E)-4-hydroxycembra-5,8,12,15-tetraene(2), cembrene A(3),(3S,4S,7R)-4-hydroxycembrane(4), and pavidolide D(5). Compound 1 was a new compound. Compounds 2, 4, and 5 were obtained from the gum resin of B. carterii for the first time. Compound 2 showed weak inhibition on the human liver cancer cell line HepG2.


Assuntos
Boswellia , Diterpenos , Linhagem Celular , Humanos , Estrutura Molecular , Resinas Vegetais
11.
J Pharm Biomed Anal ; 201: 114106, 2021 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-33962180

RESUMO

Boswellic acids, a class of triterpenes, are the bioactive constituents in Indian frankincense, an herbal drug with pronounced anti-inflammatory activity. In this study their separation and quantification in B. serrata extracts is reported for the first time by using Supercritical Fluid Chromatography. Under optimized conditions, i.e. a Viridis HSS C18 SB column and carbon dioxide, methanol, acetonitrile and ammonium hydroxide as mobile phase, six boswellic acids could be separated in under 6 min. The assay fulfilled all validation criteria with coefficients of determination higher than 0.999, a wide linear range (30-1000 µg/mL), recovery rates from 97.1-103.0 %, excellent precision, and detection limits typical for SFC with UV-detection (≤ 5.5 µg/mL). The method could easily be hyphenated to mass spectrometry, which was helpful to tentatively assign further compounds (mainly derivatives of tirucallic acid) and to increase the assay's sensitivity. Its practical applicability was confirmed by analyzing several commercial products, which mainly contained ß-boswellic acid as dominant triterpene, yet in extremely variable amounts ranging from 0.9 to 16.9 %.


Assuntos
Boswellia , Cromatografia com Fluido Supercrítico , Franquincenso , Triterpenos , Suplementos Nutricionais , Extratos Vegetais , Triterpenos/análise
12.
PLoS One ; 16(5): e0252279, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34048452

RESUMO

INTRODUCTION: Osteoarthritis is a progressive degenerative joint disease which is high prevalent in dogs. In the late stage of the disease, it determines chronic neuropathic pain which leads to reduced quality-of-life in affected patients. To date it has not yet been identified a specific treatment, but it has been proved that nutraceutical and dietary supplements may play an important role in controlling inflammation and pain. The aim of this study was to evaluate, by the use of force plate gait analysis, the clinical efficacy of Boswellia and Curcuvet® combined with conventional nutraceutical therapy compared with conventional nutraceutical alone in dogs affected by osteoarthritis. MATERIALS AND METHODS: Twenty client-owned dogs, over 12 months old and 20 kg of body-weight, with a confirmed diagnosis of Osteoarthritis, were included in this randomized, double-blinded study. The dogs were randomly divided into two groups: the first group (A) received a conventional nutraceutical (consisted in a preparation of glucosamine, chondroitin sulfate, fish-oil containing 80% of omega 3-fatty acid, vitamin C and E, saccharomyces Cerevisiae) with a combination of acid boswellic and Curcuvet®, while the second group (B) received a conventional nutraceutical. All the enrolled dogs underwent a washout period before starting the treatment with nutraceuticals products which were the only admitted treatment over the study period. A full orthopaedic and neurologic examination, and force plate gait analysis were performed before starting the treatment, at 45, 90, and 60 days post-treatment. Ground reaction forces were recorded and analyzed. RESULTS: Twenty dogs were enrolled in the study. In both groups there was an increasing values of ground reaction forces. These results might indicate that both nutraceutical products determined a better condition in terms of pain feeling but that effect is much more visible after 60 days from the end of the administration in treated group. DISCUSSION: In conclusion Curcuvet in combination with Boswellic acid could be considered a valid aid in a multimodal treatment for canine osteoarthritis.


Assuntos
Osteoartrite/tratamento farmacológico , Triterpenos/uso terapêutico , Animais , Ácido Ascórbico/sangue , Peso Corporal/fisiologia , Boswellia/química , Sulfatos de Condroitina/uso terapêutico , Cães , Ácidos Graxos Ômega-6/sangue , Feminino , Glucosamina/uso terapêutico , Masculino , Osteoartrite/sangue , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Vitamina E/sangue
13.
J Food Biochem ; 45(6): e13730, 2021 06.
Artigo em Inglês | MEDLINE | ID: mdl-33880765

RESUMO

The development of plant-based nano-materials is considered an eco-friendly technology because it does not involve hazardous chemicals. In this study, bimetallic ZnFe2 O4 and CrFe2 O4 nanoparticles were synthesized using an aqueous extract of Boswellia carteri resin. Synthesized ZnFe2 O4 and CrFe2 O4 nanoparticles were characterized by UV-Vis spectroscopy, FTIR, XRD, and HR-TEM. The anti-inflammatory activity was investigated in LPS-stimulated RAW 264.7 macrophages, whereas antioxidant activity was examined using a Hydrogen Peroxide Scavenging Activity Assay, Nitric Oxide Scavenging Activity Assay, and ABTS Radical Scavenging Assay. ZnFe2 O4 and CrFe2 O4 nanoparticles demonstrated a moderate scavenger of H2 O2 with IC50 values; 87.528 ± 8 µg/ml and 146.4468 ± 12 µg/ml, respectively. While they exhibited a strong scavenger of NO with IC50 values; 4.01 ± 0.7 µg/ml and 4.01 ± 0.7µg/ml, respectively. Interestingly, ZnFe2 O4 and CrFe2 O4 nanoparticles revealed an excellent anti-inflammatory activity by dose-dependently suppressing mRNA expressions of IL-1b, IL-6, and TNF-α. Also, ZnFe2 O4 and CrFe2 O4 nanoparticles suppress the protein expression of TNF-α. Together, our results proved that phyto-mediated ZnFe2 O4 and CrFe2 O4 nanoparticles using Boswellia carteri resin have great potential in biomedical applications such as anti-inflammatory and antioxidant. PRACTICAL APPLICATIONS: Our phyto-synthesized chromium iron oxide bimetallic nanoparticles (NPs) have shown a novel and potent anti-inflammatory activity, with remarkable biosafety toward tested macrophages. Zinc iron oxide bimetallic NPs exhibited anti-inflammatory effect with a lesser extent compared to the former, with moderate cytotoxicity against tested macrophages. Both zinc and chromium iron oxide NPs exhibited an equivalent antioxidant activity. Our resin-capped chromium iron oxide NPs are suggested to be a competing nonsteroidal anti-inflammatory agent; it is further recommended to establish advanced animal studies to confirm their biosafety, stability, and anti-inflammatory activity accompanied with the antioxidant activity.


Assuntos
Boswellia , Nanopartículas , Animais , Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Extratos Vegetais
14.
Artigo em Inglês | MEDLINE | ID: mdl-33802272

RESUMO

This report is part of a larger study designed to rapidly and efficiently screen potential treatments for Gulf War Illness (GWI) by testing nine different botanicals. In this placebo-controlled, pseudo-randomized, crossover clinical trial of 20 men with GWI, we tested three botanical agents with putative peripheral and central anti-inflammatory actions: curcumin (Curcuma longa), boswellia (Boswellia serrata), and French maritime pine bark extract (Pinus pinaster). Participants completed 30 +/- 3 days of baseline symptom reports, followed by 30 +/- 3 days of placebo, 30 +/- 3 days of lower-dose botanical, and 30 +/- 3 days of higher-dose botanical. Participants then repeated the process with a new botanical until completing up to three botanical cycles. Data were analyzed using linear mixed models. Curcumin reduced GWI symptom severity significantly more than placebo at both the lower (p < 0.0001) and higher (p = 0.0003) dosages. Boswellia was not more effective than placebo at reducing GWI symptoms at either the lower (p = 0.726) or higher (p = 0.869) dosages. Maritime pine was not more effective than placebo at the lower dosage (p = 0.954) but was more effective than placebo at the higher dosage (p = 0.006). This study provides preliminary evidence that curcumin and maritime pine may help alleviate symptoms of GWI. As a screening study, a final determination of the efficacy of these compounds for all individuals with GWI cannot be made, and further studies will need to be conducted to determine strength and durability of effects, as well as optimal dosage. These results suggest that GWI may, at least in part, involve systemic inflammatory processes. This trial was registered on ClinicalTrials.gov (NCT02909686) on 13 September 2016.


Assuntos
Boswellia , Curcumina , Síndrome do Golfo Pérsico , Pinus , Estudos Cross-Over , Curcuma , Curcumina/uso terapêutico , Guerra do Golfo , Humanos , Masculino , Síndrome do Golfo Pérsico/terapia , Casca de Planta , Extratos Vegetais/uso terapêutico
15.
ACS Chem Neurosci ; 12(10): 1791-1801, 2021 05 19.
Artigo em Inglês | MEDLINE | ID: mdl-33926190

RESUMO

The resin of the tree Boswellia sacra Flueck. (synonym: B. carterii; Burseraceae), also known as "frankincense", is a traditional remedy used for central nervous system disorders in East Africa. Here we report the evaluation of its antiseizure activity in zebrafish and mouse epilepsy models to identify novel antiseizure compounds. The resin was extracted by solvents of increasing polarity. The hexane extract demonstrated the strongest antiseizure activity and was therefore subjected to bioactivity-guided isolation, which leaded to the isolation of eight terpene derivatives. A new prenylbicyclogermacrene derivative (2) was isolated along with seven other compounds (1, 3-8). Among them, the triterpene ß-boswellic acid (5) showed the strongest activity and reduced 90% of pentylenetetrazole (PTZ)-induced seizures at 100 µg/mL. In parallel to B. sacra, a commercial extract of Boswellia serrata was also evaluated and showed moderate bioactivity (45% reduction at 30 µg/mL). The extract of B. serrata was subjected to targeted isolation of other boswellic acid derivatives (9-13), which were evaluated for antiseizure activity in comparison with 5. In the whole series, ß-boswellic acid (5) was the most active (60% reduction at 200 µM), and its potency was also confirmed with its purchased standard (S5). Pure nanoparticles of S5 and a commercially formulated extract of B. serrata were tested in a PTZ-kindling mouse seizure model. This notably revealed that the S5 administration reduced seizures by 50% in this mouse model, which was consistent with its detection and quantification in plasma and brain samples. This study and the preclinical evaluation performed indicate that ß-boswellic acid, common to various species of Boswellia, has some potential as an antiseizure agent.


Assuntos
Boswellia , Epilepsia , Triterpenos , Animais , Anticonvulsivantes/farmacologia , Epilepsia/tratamento farmacológico , Camundongos , Extratos Vegetais/farmacologia , Resinas Vegetais , Triterpenos/farmacologia , Peixe-Zebra
16.
Phytochemistry ; 184: 112660, 2021 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-33524859

RESUMO

This review is not intended to describe the triterpenes isolated from the Boswellia genus, since this information has been covered elsewhere. Instead, the aim is to provide insights into the biosynthesis of triterpenes in Boswellia. This genus, which has 24 species, displays fascinating structural diversity and produces a number of medicinally important triterpenes, particularly boswellic acids. Over 300 volatile components have been reported in the essential oil of Boswellia, and more than 100 diterpenes and triterpenes have been isolated from this genus. Given that no triterpene biosynthetic enzymes have yet been isolated from any members of the Boswellia genus, this review will cover the likely biosynthetic pathways as inferred from structures in nature and the probable types of biosynthetic enzymes based on knowledge of triterpene biosynthesis in other plant species. It highlights the importance of frankincense and the factors and threats affecting its production. It covers triterpene biosynthesis in the genus Boswellia, including dammaranes, tirucallic acids, lupanes, oleananes, ursanes and boswellic acids. Strategies for elucidating triterpene biosynthetic pathways in Boswellia are considered. Furthermore, the possible mechanisms behind wound-induced resin synthesis by the tree and related gene expression profiling are covered. In addition, the influence of the environment and the genotype on the biosynthesis of resin and on variations in the compositions and types of resins will also be reviewed.


Assuntos
Boswellia , Triterpenos , Ciclização , Estrutura Molecular , Resinas Vegetais
17.
Integr Cancer Ther ; 20: 1534735421996824, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33615860

RESUMO

Co-therapy with herbal extracts along with current clinical drugs is being increasingly recognized as a useful complementary treatment for cancer. The anti-cancer property of the phyto-derivative acetyl-11 keto ß boswellic acid (AKBA) has been studied in many cancers, including prostate cancer. However, the whole extract of the gum resin Boswellia serrata (BS) and anti-androgen enzalutamide has not been explored in prostate cancer to date. We hypothesized that the BS extract containing 30% (AKBA) with enzalutamide acted synergistically in the early phase of cancer, especially in LNCaP cells, by inhibiting androgen receptor (AR) and by reducing cell proliferation, and further, that the extract would be superior to the action of the active ingredient AKBA when used alone or in combination with enzalutamide. To test our hypothesis, we treated LNCaP cells with BS extract or AKBA and enzalutamide both individually and in combination to analyze cell viability under different levels of dihydrotestosterone (DHT). The inhibition of androgen receptor (AR) followed by the expression of prostate-specific antigen (PSA) and the efflux mechanism of the cells were analyzed to determine the effect of the combination on the cellular mechanism. Cells derived from prostate cancer patients were also tested with the combination. Only 6 µM enzalutamide along with BS in the range of 4.1 µg/ml to 16.4 µg/ml gave the best synergistic results with nearly 50% cell killing even though standard enzalutamide doses were as high as 48 µM. Cell killing was most effective at intermediate DHT concentrations of approximately 1 nM, which corresponds to normal physiological serum levels of DHT. The Pgp expression level and the androgen receptor expression levels were reduced under the combination treatment; the former helping to minimize drug efflux and the latter by reducing the sensitivity to hormonal changes. Furthermore, the combination reduced the PSA level secreted by the cells. In contrast, AKBA could not achieve the needed synergism for adequate cell killing at equivalent concentrations. The combination of enzalutamide and BS extract containing 30% AKBA because of their synergistic interaction is an attractive therapeutic option for treating early stage (hormone-dependent) prostate cancer and is superior to the use of AKBA alone.


Assuntos
Benzamidas/farmacologia , Boswellia , Nitrilas/farmacologia , Feniltioidantoína/farmacologia , Extratos Vegetais , Neoplasias da Próstata/tratamento farmacológico , Testosterona , Triterpenos , Androgênios , Boswellia/química , Linhagem Celular Tumoral , Humanos , Masculino , Extratos Vegetais/farmacologia , Triterpenos/farmacologia
18.
Sci Total Environ ; 767: 144285, 2021 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-33429269

RESUMO

Pure nanocellulose was extracted from agricultural waste material namely jackfruit (Artocarpus heterophyllus) peel through acid hydrolysis. The extraction method utilizes soapnut solution as an eco-friendly bleaching agent in order to avoid environment polluting chlorinated chemicals. Various thin films were prepared by solvent casting nanocellulose and different plasticizers namely glycerol, polyethylene glycol, polyvinyl alcohol, triethyl citrate along with novel filler, Boswellia serrata commonly known as frankincense. Thin films were characterized by FT-IR, XRD and the surface modifications were investigated using FESEM. The physical, mechanical, thermal properties and biodegradability of the film were also reported. The surface morphology was improved by different plasticizers and a self-assembly was obtained due to more stable hydrogen bonding between the nanocellulose, plasticizers and filler during the film formation. Thermal investigations of plasticizers/Boswellia serrata incorporated thin films revealed an increase in glass transition temperature of nanocellulose. Results indicate that these films are biodegradable and compostable in nature and could be used as substitute for petroleum derived plastics.


Assuntos
Artocarpus , Plásticos Biodegradáveis , Boswellia , Celulose , Frutas , Plastificantes , Espectroscopia de Infravermelho com Transformada de Fourier , Resistência à Tração
19.
Molecules ; 26(2)2021 Jan 12.
Artigo em Inglês | MEDLINE | ID: mdl-33445710

RESUMO

Boswellic acids, and particularly 11-keto-boswellic acids, triterpenoids derived from the genus Boswellia (Burseraceae), are known for their anti-inflammatory and potential antitumor efficacy. Although boswellic acids generally occur as α-isomers (oleanane type) and ß-isomers (ursane type), 11-keto-boswellic acid (KBA) was found only as the ß-isomer, ß-KBA. Here, the existence and natural occurrence of the respective α-isomer, 11-keto-α-boswellic acid (α-KBA), is demonstrated for the first time. Initially, α-KBA was synthesized and characterized by high-resolution mass spectrometry (HR-MS) and nuclear magnetic resonance (NMR) spectroscopy, and a highly selective, sensitive, and accurate high-performance liquid chromatography coupled with tandem mass spectrometry (HPLC-MS/MS) method was developed by Design of Experiments (DoE) using a pentafluorophenyl stationary phase. This method allowed the selective quantification of individual 11-keto-boswellic acids and provided evidence for α-KBA in Boswellia spp. oleogum resins. The contents of α-KBA as well as further boswellic acids and the composition of essential oils were used to chemotaxonomically classify 41 Boswellia oleogum resins from 9 different species. Moreover, α-KBA exhibited cytotoxicity against three treatment-resistant triple-negative breast cancer (TNBC) cell lines in vitro and also induced apoptosis in MDA-MB-231 xenografts in vivo. The respective ß-isomer and the acetylated form demonstrate higher cytotoxic efficacies against TNBC cells. This provides further insights into the structure-activity relationship of boswellic acids and could support future developments of potential anti-inflammatory and antitumor drugs.


Assuntos
Antineoplásicos/farmacologia , Boswellia/química , Neoplasias de Mama Triplo Negativas/patologia , Triterpenos/farmacologia , Animais , Antineoplásicos/química , Morte Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Galinhas , Humanos , Isomerismo , Triterpenos/síntese química , Triterpenos/química , Triterpenos/isolamento & purificação
20.
Minerva Med ; 112(2): 255-260, 2021 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-32880419

RESUMO

BACKGROUND: Neck/shoulder, sudden pain, or muscular pain (not associated to structural or bone/joints components), due to fascial or muscular strain is common in active subjects, in non-professional athletes and sports performers. The aim of this supplement registry was the evaluation of a cream based on natural, active ingredients for topical application in supporting the improvement of pain and improving head/neck mobility, possibly minimizing the use of systemic drugs. METHODS: The cream includes standardized active ingredients of natural origin as an extract of Harpagophytum procumbes, an extract from Boswellia serrata, a CO2 extract of ginger and escin. Subjects were divided into three groups, all using the standard management (SM) in combination with the Sport Cream or in addition to Flector (diclofenac) patch. RESULTS: The groups were comparable and homogeneous at the baseline. No side effects or skin tolerability issues were observed with the Sport Cream nor with the SM or diclofenac patches. Subjects receiving sport cream + SM reported a significant improvement in pain, stiffness, altered mobility and altered working capacity, with a reduced need for rescue medication (diclofenac) compared to subjects in the other two groups. CONCLUSIONS: Finally, subjects receiving sport cream + SM reported a more remarkable decrease in skin temperature in the affected area associated to an improvement in clinical symptoms.


Assuntos
Boswellia/química , Escina/uso terapêutico , Gengibre/química , Cervicalgia/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Dor de Ombro/tratamento farmacológico , Administração Tópica , Adulto , Traumatismos em Atletas/tratamento farmacológico , Diclofenaco/administração & dosagem , Diclofenaco/uso terapêutico , Escina/administração & dosagem , Feminino , Harpagophytum/química , Humanos , Masculino , Pessoa de Meia-Idade , Tono Muscular , Mialgia/diagnóstico por imagem , Mialgia/tratamento farmacológico , Cervicalgia/diagnóstico , Cervicalgia/etiologia , Projetos Piloto , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Sistema de Registros , Terapia de Salvação , Dor de Ombro/diagnóstico , Dor de Ombro/etiologia , Creme para a Pele/administração & dosagem , Creme para a Pele/química , Creme para a Pele/uso terapêutico , Termografia
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