Alternative Anti-inflammatory Agents Research Articles

Molecular Modeling of Brassicaceae Derivatives for Inhibiting Lipoxygenases: A Promising Therapeutic Strategy.

Inflammation plays a crucial role in the body's defense mechanisms, but uncontrolled inflammation can lead to chronic and pathological conditions. This study aimed to identify natural compounds as potential replacements for the synthetic drug Zileuton, known for its side effects. Utilizing the MOE and Molegro modeling methods, several molecules were evaluated, and three compounds, namely 1-Isothiocyanatopent-4-en-2-ol, 7-Isothiocyanatohept-1-ene, and 5- (Isothiocyanatomethyl)-1,2,3-trimethoxybenzene, exhibited superior inhibitory properties. These compounds consistently demonstrated low energy values, indicating high inhibition potency. Notably, 5-(Isothiocyanatomethyl)-1,2,3-trimethoxybenzene emerged as the most promising candidate among all tested compounds. These findings provide valuable insights for the development of alternative anti-inflammatory agents. Further research is required to assess the efficacy and safety profiles of these compounds in clinical settings. This study represents a significant advancement in the search for innovative therapeutic strategies to manage inflammation-related disorders.

Comparative effectiveness of nitro dihydrocapsaicin, new synthetic derivative capsaicinoid, and capsaicin in alleviating oxidative stress and inflammation on lipopolysaccharide-stimulated corneal epithelial cells

Loss of tear homeostasis, characterized by hyperosmolarity of the ocular surface, induces cell damage through inflammation and oxidation. Transient receptor potential vanilloid 1 (TRPV1), a sensor for osmotic changes, plays a crucial role as a calcium ion channel in the pathogenesis of hypertonic-related eye diseases. Capsaicin (CAP), a potent phytochemical, alleviates inflammation during oxidative stress events by activating TRPV1. However, the pharmacological use of CAP for eye treatment is limited by its pungency. Nitro dihydrocapsaicin (NDHC) was synthesized with aromatic ring modification of CAP structure to overcome the pungent effect. We compared the molecular features of NDHC and CAP, along with their biological activities in human corneal epithelial (HCE) cells, focusing on antioxidant and anti-inflammatory activities. The results demonstrated that NDHC maintained cell viability, cell shape, and exhibited lower cytotoxicity compared to CAP-treated cells. Moreover, NDHC prevented oxidative stress and inflammation in HCE cells following lipopolysaccharide (LPS) administration. These findings underscore the beneficial effect of NDHC in alleviating ocular surface inflammation, suggesting that NDHC may serve as an alternative anti-inflammatory agent targeting TRPV1 for improving hyperosmotic stress-induced ocular surface damage.

Anti-inflammatory activity of combination of ethanol extracts of ginger (Zingiber officinale) and bangle (Zingiber cassumunar) in carrageenan-induced rats

Background: Inflammation is an essential innate immune response aimed at antigen elimination and preventing their spread. Ginger (Zingiber officinale) and bangle (Zingiber cassumunar) rhizomes have been empirically utilized as medicinal components due to their anti-inflammatory potential. However, the combined efficacy of these rhizomes has not been previously explored. Objective: This study aimed to assess the anti-inflammatory activity of a combination of ginger and bangle rhizome extracts. Method: Ginger and bangle rhizomes were individually subjected to extraction through maceration with 96% ethanol, followed by purification with n-hexane. The anti-inflammatory activity was evaluated via motility tests on subjects administered orally with 1% CMC-Na (control), diclofenac sodium (4.5 mg/kg body weight), ginger ethanol extract (200 mg/kg body weight), bangle ethanol extract (400 mg/kg body weight), and a combination of both extracts (100:200 mg/kg body weight). Observations were made over 6 hours, with motility scores subsequently analyzed using ANOVA and the LSD test for statistical significance. Results: Treatments involving ginger extract, bangle extract, and their combination significantly improved motility scores compared to the negative control. Furthermore, these treatments displayed no significant difference in effectiveness compared to the diclofenac sodium group (p > 0.05). Conclusion: The combined ethanol extracts of ginger and bangle rhizomes demonstrate anti-inflammatory activity comparable to diclofenac sodium, as evidenced by motility score evaluations. This suggests their potential as alternative anti-inflammatory agents.

Finding the research gap of the potential anti-inflammatory activity of cocoa (Theobroma cacao L.) through systematic literature review

The use of conventional drugs in treating inflammation has various side effects, and thus it is necessary to have an alternative anti-inflammatory agent that is effective and safe. Cocoa (Theobroma cacao L.) is one of the agricultural products with a high content of polyphenols, especially flavan-3-ols potentially used as an anti-inflammatory agent. The purpose of this research is to investigate the research gap of the potential antiinflammatory activity of cocoa based on the published literatures. The systematic method of synthesizing the review follows the guidelines of the PRISMA Statement 2020 using the PICOS literature search strategy. The results of this study showed that the positive effect of cocoa on inflammation indicated by 44 out of 72 biomarkers (61.11%). Flavan-3- ols can effectively reduce inflammation by reducing the activation of transcripts that regulate pro-inflammatory cytokines (NF-kB), prostaglandins, and NO. The antiinflammatory effect was effectively found in different groups, i.e., subjects without health issue (healthy subject), subjects with some health problems record and subjects with obesity. Nevertheless, it was found in the previous researches that the manifest of cocoaderived products as well as the biomarkers for determining the anti-inflammatory effect of cocoa still vary. Also, there is no study investigating the anti-inflammatory effect of cocoa on different age group. Therefore, further researches are required in this area to complete the puzzle of information regarding the potential anti-inflammatory activity of cocoa.

Exploring the Anti-Inflammatory Potential of Cyperus pangorei Rhizome Extracts An In Vitro and In Vivo Study

Background and aim: Inflammation is a pivotal process implicated in various physiological and pathological conditions, necessitating the exploration of alternative anti-inflammatory agents with minimal side effects. This study aimed to investigate the anti-inflammatory potential of the standardized ethyl acetate (EtAc) fraction derived from Cyperus pangorei rhizomes. Methods: The rhizomes of C. pangorei were collected, processed, and subjected to extraction and fractionation to obtain the EtAc fraction. RP-HPLC analysis was employed to standardized the EtAc fraction against standard quercetin, luteolin, and apigenin. In vitro studies utilized peritoneal macrophages isolated from male Swiss albino rats to assess NO production and cytokine levels (IL-1β, IL-6, TNF-α) upon treatment with the EtAc fraction. In vivo evaluation was conducted using a carrageenan-induced rat paw edema model. Results: RP-HPLC analysis revealed the presence of quercetin, luteolin, and apigenin in the EtAc fraction. In vitro studies demonstrated dose-dependent inhibition of LPS-induced NO production and suppression of inflammatory cytokines (IL-1β, IL-6, TNF-α) by the EtAc fraction. Furthermore, in the carrageenan-induced rat paw edema model, the EtAc fraction exhibited dose-dependent inhibition of paw edema. Conclusion: The findings of this study highlight the significant anti-inflammatory potential of C. pangorei rhizome extracts, particularly the EtAc fraction. The identified compounds, quercetin, luteolin, and apigenin, contribute to its anti-inflammatory activity by modulating key inflammatory mediators. These results support the potential therapeutic use of C. pangorei in managing inflammation-related disorders. Further research is warranted to elucidate the underlying mechanisms and evaluate the long-term efficacy and safety of C. pangorei extracts as anti-inflammatory agents.

Germinated Rice Seeds Improved Resveratrol Production to Suppress Adipogenic and Inflammatory Molecules in 3T3-L1 Adipocytes.

Obesity is a major risk factor for a variety of diseases and contributes to chronic inflammation. Resveratrol is a naturally occurring antioxidant that can reduce adipogenesis. In this study, the antiadipogenic and anti-inflammatory activities of resveratrol-enriched rice were investigated in 3T3-L1 adipocyte cells. Cotreatment of dexamethasone and isobutylmethylxanthin upregulated adipogenic transcription factors and signaling pathways. Subsequent treatment of adipocytes with rice seed extracts suppressed the differentiation of 3T3-L1 by downregulating adipogenic transcription factors (peroxisome proliferator-activated receptor γ and CCAAT/enhancer-binding protein α) and signaling pathways (extracellular signal-regulated kinase 1/2 and protein kinase B Akt), this was especially observed in cells treated with germinated resveratrol-enriched rice seed extract (DJ526_5). DJ526_5 treatment also markedly reduced lipid accumulation in the cells and expression of adipogenic genes. Lipopolysaccharide (LPS)-induced inflammatory cytokines (prostaglandin-endoperoxide synthase 2 (COX-2), tumor necrosis factor (TNF)-α, interleukin (IL)-1β, and IL-6) decreased in cells treated with DJ526_5. Collectively, DJ526_5 exerts antiadipogenic effects by suppressing the expression of adipogenesis transcription factors. Moreover, DJ526_5 ameliorates anti-inflammatory effects in 3T3-L1 adipocytes by inhibiting the activation of phosphorylation NF-κB p65 and ERK ½ (MAPK). These results highlight the potential of resveratrol-enriched rice as an alternative obesity-reducing and anti-inflammatory agent.

ROLE OF LOW-DOSE AZITHROMYCIN IN THE MANAGEMENT OF CYSTIC BRONCHIECTASIS: A CASE SERIES

Bronchiectasis is an abnormal chronic and persistent dilatation of the bronchi that is accompanied by destruction of the bronchial walls due to congenital or acquired disorders such as chronic respiratory tract infections. Recurrent respiratory tract infections are characteristic of bronchiectasis. Radiological examination plays a role in diagnosis, a thin section CT to confirm a diagnosis of bronchiectasis when clinically suspected, and provides clearer information on lung morphology. The goals of treating bronchiectasis are to prevent exacerbations, reduce complaints, improve the patient's quality of life, and stop the disease from worsening. Therapy is expected to address the proven underlying cause, cutting off the vicious cycle of bronchiectasis Long-term antibiotics are considered in patients with bronchiectasis with frequent exacerbations three or more times per year to relieve symptoms and reduce the frequency of exacerbations. Macrolides are a plausible alternative antibiotic and anti-inflammatory agent with a lower burden of treatment for bronchiectasis patients. We present three cases of Bronchiectasis that were admitted to Mataram University Hospital. The three cases were given Long-term antibiotics with low-dose Azithromycin for 2 and 3 months. This report demonstrates clinical improvement in a reduction of exacerbation frequency, improvement in quality of life, decreased sputum production, and increased ability to carry out activities in patients treated with low-dose azithromycin. The most common side effect that appears in three cases is gastrointestinal disturbances.

In vitro assessment of antimicrobial, anti-inflammatory, and schistolarvicidal activity of macroalgae-based gold nanoparticles

There is a growing need to improve facile, eco-friendly, and cheap approaches for nanoparticle (NP) synthesis. Green protocols have been investigated for the fabrication of NPs using several natural sources as plants, algae, fungi, and bacteria. Thus, the present study proposed a rapid, convenient, and efficient biosynthesis of gold NPs (Au-NPs) using the ethanolic extracts of three macroalgae, i.e., Cystoseira myrica, C. trinodis, and Caulerpa prolifera. The reduction of Au ions and the fabrication of Au-NPs were validated using ultraviolet-visible (UV–Vis) spectroscopy, X-ray diffraction, Fourier transform infrared spectroscopy (FT-IR), transmission electron microscopy (TEM), and zeta potential analysis. The produced Au-NPs were tested for their antibacterial, antifungal, anti-inflammatory, and schistolarvicidal activity. Results revealed the formation of Au-NPs with an average size of 12.6–15.5 nm and different shapes that are mainly spherical with pure crystalline nature. The strong antibacterial activities of C. trinodis– and C. myrica–based Au-NPs against E. coli (inhibition zones of 22 and 19 mm) and against Staphylococcus aureus (inhibition zones of 18 and 20.5 and mm) were recorded, respectively. On the other hand, the high antifungal activity of C. trinodis Au-NPs against Aspergillus niger and Alternaria alternate showed the inhibition zones of 18 and 17 mm, respectively. The high antifungal activity of C. trinodis Au-NPs against Candida albicans (inhibition zone 16 mm) was also recorded. Regarding anti-inflammatory and schistolarvicidal activity, Au-NPs fabricated using C. myrica showed 64.2% of the inhibitory effect on protein denaturation and recorded the highest schistolarvicidal activity against Schistosoma mansoni cercariae that sank and died after 7 min. Overall, these findings proved that macroalgal ethanolic extracts can be effectively used for the biosynthesis of Au-NPs. These Au-NPs offer a significant alternative antimicrobial, anti-inflammatory, and schistolarvicidal agents. for biomedical uses.

β-caryophyllene and docosahexaenoic acid, isolated or associated, have potential antinociceptive and anti-inflammatory effects in vitro and in vivo

Inflammation is a complex biological response involving the immune, autonomic, vascular, and somatosensory systems that occurs through the synthesis of inflammatory mediators and pain induction by the activation of nociceptors. Staphylococcus aureus, the main cause of bacteremia, is one of the most common and potent causes of inflammation in public health, with worse clinical outcomes in hospitals. Antioxidant substances have been evaluated as alternative therapeutic analgesics, antioxidants, anti-inflammatory agents, antitumor agents, and bactericides. Among these, we highlight the essential oils of aromatic plants, such as β-caryophyllene (BCP), and polyunsaturated fatty acids, such as docosahexaenoic acid (DHA). The objective of this study was to evaluate the biological activities of BCP–DHA association in in vitro and in vivo experimental models of antinociception and inflammation. To determine the anti-inflammatory effects, monocytes isolated from the peripheral blood of adult male volunteers were infected with methicillin-resistant S. aureus and incubated with treatment for cytokine dosage and gene expression analysis. Antinociceptive effects were observed in the three models when comparing the control (saline) and the BCP-DHA treatment groups. For this purpose, the antinociceptive effects were evaluated in animal models using the following tests: acetic acid-induced abdominal writhing, paw edema induced by formalin intraplantar injection, and von Frey hypernociception. There was a significant reduction in the GM-CSF, TNFα, IL-1, IL-6, and IL-12 levels and an increase in IL-10 levels in the BCP-DHA treatment groups, in addition to negative regulation of the expression of the genes involved in the intracellular inflammatory signaling cascade (IL-2, IL-6, IRF7, NLRP3, and TYK2) in all groups receiving treatment, regardless of the presence of infection. Statistically significant results (p < 0.05) were obtained in the acetic acid-induced abdominal writhing test, evaluation of paw edema, evaluation of paw flinching and licking in the formalin intraplantar injection model, and the von Frey hypernociception test. Therefore, BCP and DHA, either administered individually or combined, demonstrate potent anti-inflammatory and antinociceptive effects.

Analgesic and anti-inflammatory potential of Lupeol isolated from Indian traditional medicinal plant Crateva adansonii screened through in vivo and in silico approaches

BackgroundLupeol, a triterpene bioactive compound isolated from Indian traditional plant Crateva adansonii acted as promising and alternative anti-inflammatory agent to treatments of diseases related to inflammation. The inflammatory process in the body serves an important function in the control and repair of injury. However, it is self-perpetuating in number of disease conditions, which must be prevented and treated. Worldwide most prescribing NASID drug shows severe side effects. Whereas drug from natural origin shows dual inhibition of inflammatory and analgesic target protein with more efficacy and less side effects than NSAID drugs. Our study aims to isolate and screen the analgesic and anti-inflammatory potential of lupeol, a pentacyclic triterpenoid isolated from leaf extract of Crateva adansonii belongs to Capparaceae family commonly used Indian traditional medicine for treating inflammatory diseases. ResultsMethanol and chloroform leaf extracts (ME and CE) and lupeol fraction (LF) of plant Crateva adansonii is investigated through employing in vivo male Wistar albino rat model. Acute toxicity study of C. adansonii ME and CE leaf extracts reveals that no mortality and no behavioral changes in experimental animals up to 2 g/kg. So no lethal dose we consider two optimal doses 200 and 400 mg of plant leaf extracts for in vivo inflammatory and analgesic study. In vivo acute and chronic anti-inflammatory activity was carried out through carrageenan-induced rat paw edema and cotton pellet-induced granuloma models. LF (100 mg/kg, oral route) of Crateva adansonii evoked highest percentage of inflammation inhibition (50 and 33.96% respectively) in both in vivo acute and chronic inflammation model among all tested samples (ME and CE 200 mg and 400 mg/kg, oral route) including reference standard (10 mg/kg, oral route) indomethacin. Carrageenan-challenged experimental animals were screened for one inflammatory marker enzyme myeloperoxidase (MPO), inflammatory products such as Prostaglandrin E2 (PGE2), and eight different cytokines markers (TNFα, IL-6, IFN γ, IL-1α, IL-1β, MCP-1, Rantes, and MIP) associated with inflammation reveals that LF (100 mg/kg, oral route) of Crateva adansonii shows prominent anti-inflammatory activity than reference standard indomethacin (10 mg/kg, oral route) over all these biological tested parameters. In vivo analgesic assays such as hot plate assay and acetic acid-induced writhing assay revealed that LF (100 mg/kg, oral route) possesses significant analgesic activity (11.60 s and 69.05%) when compared with standard drug pentazocine(10 mg/kg, oral route). Finally, we made an in silico screening of lupeol against analgesic (nAChR) and anti-inflammatory (COX-2) target proteins reveals that lupeol possess highest binding affinity with nAChR and COX-2 target proteins (− 8.5 and − 9.0 Kcal/mol) over the reference standard pentazocine and indomethacin (− 7.0 and − 8.4 Kcal/mol) respectively. ConclusionThe present study result provides a pharmacological evidences for analgesic and anti-inflammatory potential of lupeol isolated from Indian traditional plant Crateva adansonii act as a multi-target agent with immense anti-inflammatory potential targeting key molecules of inflammation such as MPO, PGE2, and eight pro-inflammatory cytokine markers. Outcome of present study is to find promising anti-inflammatory bioactive agents from the cheapest Indian traditional medicinal plant sources useful for pharmaceutical industries.

Anti-inflammatory effects of functional beverage from a mixture of moringa leaves, pandanus leaves, and red ginger in mice induced with monosodium urate crystal

Production of uric acid that exceeds normal limits in the blood (hyperuricemia) can cause the formation of urate crystals and inflammatory reactions. In various studies, moringa leaves, pandanus leaves, and red ginger are known to contain phytochemical components (phenols and flavonoids) that are useful as antioxidants, anti-inflammatory, inhibiting xanthine oxidase enzyme activity, overcoming rheumatism, and antidiabetic. Functional drinks from the mixture of moringa leaves, pandanus leaves, and red ginger were optimised using the response surface method (RSM) in previous studies. The effect of this functional beverage product was tested for its effect as an anti-inflammatory in vivo. The testing process of the anti-inflammatory effect was using intradermally monosodium urate (MSU)-induced mice. Mice were measured for changes in edema, and after two days of treatment, the spleen was taken for flow cytometry testing of inflammatory cytokine expression of CD11b+ TNFα+, CD11b+ IL6+, CD11b+ IL10+, and blood was taken to test the expression of cytokine CD11b+ TNFα+. The results showed functional beverage products could potentially be used as an alternative anti-inflammatory agent in gout because it significantly inhibited edema, significantly inhibited the expression of proinflammatory cytokines CD11b+ TNFα+ and CD11b+ IL6+ and increased the expression of anti-inflammatory cytokines CD11b+ IL10+, where the anti-inflammatory effect was not significantly different from the control of indomethacin drugs.

Hydroxytyrosol ameliorates oxidative challenge and inflammatory response associated with lipopolysaccharide-mediated sepsis in mice.

Hydroxytyrosol (HT) is among the main bioactive ingredients isolated from olive tree with a variety of biological and pharmacological activities. In the current study, the antioxidative and anti-inflammatory activities of HT were distinguished in the splenic tissue following lipopolysaccharide (LPS)-mediated septic response. Thirty-five Swiss mice were divided into five groups (n = 7): control, HT (40 mg/kg), LPS (10 mg/kg), HT 20 mg+LPS and HT 40 mg+LPS. HT was administered for 10 days, while a single LPS dose was applied. The obtained findings demonstrate that HT administration enhanced the survival rate and decreased lactate dehydrogenase level in LPS-challenged mice. Treatment with HT inhibited the incidence of oxidative damage in splenic tissue through decreasing lipoperoxidation and increasing antioxidant molecules, namely glutathione, superoxide dismutase and catalase. HT also decreased total leukocytes count, C-reactive protein, monocyte chemoattractant protein-1, and myeloperoxidase levels. Additionally, HT suppressed the production levels of tumor necrosis factor-α, interleukin-1β, and interleukin-6. Moreover, mRNA expression of inducible nitric oxide synthase and nitric oxide production were increased after HT administration. Furthermore, HT supplementation resulted in a downregulation of p38 mitogen-activated protein kinase, inhibited the activation of the nuclear factor kappa-B from the nucleus to the cytoplasm, and attenuated infiltration of activated immune cells and tissue injury following LPS injection. Collectively, these findings demonstrate the antioxidative and anti-inflammatory properties of HT against LPS-mediated inflammation and sepsis. Therefore, HT could be applied as an alternative anti-inflammatory agent to minimize or prevent the development of systemic inflammatory response associated with septic shock.

POCl3 Mediated Syntheses, Pharmacological Evaluation and Molecular Docking Studies of Some Novel Benzofused Thiazole Derivatives as a Potential Antioxidant and Anti-inflammatory Agents

Background: The present research work is focused on the development of alternative antioxidant and anti-inflammatory agents. The review of the literature reveals that many benzofused thiazole analogues have been used as lead molecules for the design and development of therapeutic agent, including anticancer, anti-inflammatory, antioxidant and antiviral. The synthesized benzofused thiazole derivatives are evaluated for in vitro antioxidant, anti-inflammatory activities and molecular docking study. Thus, the present research work aims to synthesize benzofused thiazole derivatives and to test their antioxidant and antiinflammatory activities. Objective: To design and synthesize an alternative antioxidant and anti-inflammatory agents. Methods: The substituted benzofused thiazoles 3a-g were prepared by cyclocondensation reaction of appropriate carboxylic acid with 2-aminothiophenol in POCl3 and heated for about 2-3 h to offer benzofused thiazole derivatives 3a-g. All the newly synthesized compounds were in vitro screened for their anti-inflammatory and antioxidant activities by using a known literature method. Results: At the outset, the study of in vitro indicated that the compounds code 3c, 3d and 3e possessed distinct anti-inflammatory activity as compared to a standard reference. All the tested compounds show potential antioxidant activity against one or more reactive (H2O2, DPPH, SO and NO) radical scavenging species. Additionally, docking simulation is further performed to the position of compounds 3d &amp; 3e into the anti-inflammatory active site to determine the probable binding model. Conclusion: New anti-inflammatory and antioxidant agents were needed; it has been proved that benzofused thiazole derivatives were 3c, 3d and 3e constituted as an interesting template for the evaluation of new anti-inflammatory agents and an antioxidant’s work also may provide an interesting template for further development.

Characterization and antiinflammatory properties of fractionated pyroligneous acid from palm kernel shell.

Pyroligneous acid (PA) obtained from slow pyrolysis of palm kernel shell (PKS) has high total phenolic contents and exhibits various biological activities including antioxidant, antibacterial and antifungal. In this study, PA obtained using slow pyrolysis method and fractionated using column chromatography was characterized (chemical and antioxidative properties) and investigated for its cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) inhibition activities using the in vitro and in silico approaches. The F9 PA fraction exhibited highest total phenolic content of 181.75 ± 17.0μg/mL. Fraction F21-25 showed ferric reducing antioxidant power (FRAP) (331.80 ± 4.60mg TE/g) and IC50 of 18.56 ± 0.01μg/mL towards COX-2 and 5.25 ± 0.03μg/mL towards the 5-LOX enzymes, respectively. Molecular docking analysis suggested favourable binding energy for all chemical compounds present in fraction F21-25, notably 1-(2,4,6-trihydroxyphenyl)-2-pentanone, towards both COX-2 (- 6.9kcal/mol) and 5-LOX (- 6.4kcal/mol) enzymes. As a conclusion, PA from PKS has the potential to be used as an alternative antioxidant and antiinflammatory agents which is biodegradable and a more sustainable supply of raw materials.

Antioxidants, Toxicity, and Nitric Oxide Inhibition Properties of Pyroligneous Acid from Palm Kernel Shell Biomass

Huge volumes of lignocellulosic biomass residues generated from agricultural activities such as oil palm biomass pose great environmental threats if improperly treated. In this study, pyroligneous acid (PA) obtained from slow pyrolysis of palm kernel shell (PKS) were evaluated for its antioxidant activity via chemical assays, toxicity, and potential as anti-inflammatory agent based on nitric oxide (NO) inhibition activity. The PA was extracted using ethyl acetate (EA) and fractionated using column chromatography. Fractions 13–17 that contain highest total phenolic contents (866.84 ± 54.28 µg GAE/mg) were chosen for subsequent studies. Results obtained were as follows; DPPH—75.34 ± 3.40%, TEAC—1346.48 ± 5.29 μg Trolox/mg, FRAP—11.80 ± 0.41 mmol Fe(II)/mg, hydroxyl radical scavenging—IC50 270.34 ± 4.88 µg/mL, superoxide radical scavenging—IC50 472.32 ± 1.87 µg/mL, cytotoxicity after 24 h at less than 50 µg/mL—cell viability of ≥ 93.08% for RAW 264.7 macrophage cell and anti-inflammatory activity with NO production of 6.55% after 24 h at sample concentration of 25 µg/mL. From the GC–MS analysis, phenols and derivatives were identified as major compound (83.24%) followed by esters (11.23%), and ketones (5.53%). The present of phenolic compounds namely benzene-1,2-diol, catechol (35.01%), 1,3-dimethoxy-2-hydroxybenzene, syringol (23.81%), and other catechol derivatives can be attributed to the antioxidant and anti-inflammatory activities determined. This study has successfully demonstrated the potential use of PA obtained from PKS as alternative antioxidant and anti-inflammatory agent.

ANTI-INFLAMMATORY ACTIVITY OF BAWANG DAYAK (ELEUTHERINE BULBOSA (MILL. URB.))ETHANOL BULB EXTRACTS

Background: Inflammation is a normal process in response to injury, but causes problems for the patient, including the appearance of pain, swelling, or fever. Anti-inflammatory agents generally used for those conditions, have several side effects to patients. Purpose: The objective of this research was to find alternative anti-inflammatory agents, especially from natural sources. Eleutherine bulbosa (Mill.) Urb. knew as “Bawang Dayak” belong to family Iridaceae is one of the natural sources for anti-inflammatory agents. This plant is known as traditional medicine in East Kalimantan and used as material in this research. Method: The experimental method of anti-inflammatory measurement using membrane stabilization activity for E. Bulbosa ethanol bulbs extracts. Result: The results showed that significant differences of EC50(p &lt; 0.05) were achieved between indomethacin (26.39 ± 2.91) as the positive control with E. Bulbosa (52.87 ± 2.29). EC50 of E. bulbosa showed the potential anti-inflammatory activities with similar effectiveness to half indomethacin concentration. Conclusion: It could be concluded that E. bulbosa could be further developed as a new natural source of the anti-inflammatory agents.

Sinomenine Inhibits the Progression of Rheumatoid Arthritis by Regulating the Secretion of Inflammatory Cytokines and Monocyte/Macrophage Subsets.

Rheumatoid arthritis (RA) is a chronic autoimmune inflammatory arthropathy associated with articular damage and attendant comorbidities. Even although RA treatment has advanced remarkably over the last decade, a significant proportion of patients still do not achieve sustained remission. The cause of RA is not yet known despite the many potential mechanisms proposed. It has been confirmed that RA is associated with dysregulated immune system and persistent inflammation. Therefore, management of inflammation is always the target of therapy. Sinomenine (SIN) is the prescription drug approved by the Chinese government for RA treatment. A previous study found that SIN was a robust anti-inflammation drug. In this study, we screened the different secretory cytokines using inflammation antibody arrays and qRT-PCR in both LPS-induced and SIN-treated RAW264.7 cells followed by evaluation of the ability of SIN to modulate cytokine secretion in a cell model, collagen-induced arthritis (CIA) mouse model, and RA patients. Several clinical indexes affecting the 28-joint disease activity score (DAS28) were determined before and after SIN treatment. Clinical indexes, inflammatory cytokine secretion, and DAS28 were compared among RA patients treated with either SIN or methotrexate (MTX). To explore the mechanism of SIN anti-inflammatory function, RA-associated monocyte/macrophage subsets were determined using flow cytometry in CIA mouse model and RA patients, both treated with SIN. The results demonstrated that SIN regulated IL-6, GM-CSF, IL-12 p40, IL-1α, TNF-α, IL-1β, KC (CXCL1), Eotaxin-2, IL-10, M-CSF, RANTES, and MCP-1 secretion in vivo and in vitro and reduced RA activity and DAS28 in a clinical setting. Furthermore, SIN attenuated CD11b+F4/80+CD64+ resident macrophages in the synovial tissue, CD11b+Ly6C+CD43+ macrophages in the spleen and draining lymph nodes of CIA mice. The percentage of CD14+CD16+ peripheral blood mononuclear cells was reduced by SIN in RA patients. These data indicated that SIN regulates the secretion of multiple inflammatory cytokines and monocyte/macrophage subsets, thereby suppressing RA progression. Therefore, along with MTX, SIN could be an alternative cost-effective anti-inflammatory agent for treating RA.

Membrane stabilization activity as anti-inflammatory mechanisms of Vernonia amygdalina leaves extracts

Inflammation is a normal process in the human body as a response to injury from healing process. Meanwhile, chronic inflammation will cause new health problems to patients. Anti-inflammatory agents generally used for those conditions, have several side effects to patients. The aim of this research was to find alternative anti-inflammatory agents, especially from natural sources. Vernonia amygdalina knew locally as “daun afrika” belong to family Apiaceae is one of those potential natural sources for alternative anti-inflammatory agents. This plant is known astraditionalmedicine from East Kalimantanfor health problems caused by the muscle stiffness and used as material in this research. The experimental method of anti-inflammatory measurement using membrane stabilization activity for V. amygdalina leaves extracts. The results showed that significant differences of EC50(p<0.05)achieved between indomethacin as the positive control (26.39 ± 2.91 µg/mL) with V. amygdalina leaves extracts for concentration 1% (131.81 ± 2.95 µg/mL) and 10% (62.54 ± 2.05 µg/mL). EC50 of V.amygdalina leaves extracts showed the potential anti-inflammatory activities. It could be concluded that V. amygdalina leaves extracts to have anti-inflammatory activities, which could be further developed as a new natural source of the anti-inflammatory agents.

Aktivitas Anti-Inflamasi In Vitro Ekstrak Etanol Daun Vernonia amygdalina DELILE Dengan Pengujian Stabilisasi Membran

Inflammation is a normal process in the human body as a response to injury from the healing process. Meanwhile, chronic inflammation will cause new health problems to patients. Anti-inflammatory agents generally used for those conditions, have several side effects to patients. The objective of this research was to find alternative anti-inflammatory agents, especially from natural sources. Vernonia amygdalina Delile knew locally as “Daun Bismillah” belong to family Apiaceae is one of those potential natural sources for alternative anti-inflammatory agents. This plant is known as traditional medicine and used as material in this research. The experimental method of in vitro anti-inflammatory measurement using membrane stabilization activity for ethanol extracts of V. amygdalina leaves. The results showed that significant differences of EC50 (p&lt;0.05) were achieved between indomethacin as the positive control with V. amygdalina leaves extracts for concentration 1% and 10%. EC50 of leaves ethanol extract of V. amygdalina showed the potential anti-inflammatory activities. It could be concluded that V. amygdalina leaves ethanol extracts to have anti-inflammatory activities, which could be further developed as a new natural source of the anti-inflammatory agents. &#x0D; &#x0D;

Protective effects of GV1001 on myocardial ischemia‑reperfusion injury.

The potential cardioprotective effects of the novel vaccine peptide GV1001 were evaluated in myocardial ischemia-reperfusion injury induced rat models. GV1001 is a human telomerase reverse transcriptase derived peptide, which has been reported to possess both anti-tumor and anti-inflammatory effects. The normal saline (control group) and various concentrations (0.001–10 mg/kg) of GV1001 were administered directly to the right ventricle anterior wall before induction of ischemia. The was induced by Tightening the snare around the left anterior descending coronary artery for 40 min, before releasing the snare for 10 min induced the myocardial ischemia-reperfusion injury and was conducted in Sprague-Dawley rats. The area at risk, histology, apoptotic cells, neutrophils and inflammatory cytokines were analyzed from the excised heart tissue following myocardial ischemia-reperfusion injury. The area at risk was protected by concentrations of GV1001 equal to or higher than 0.01 mg/kg. At 0.1 mg/kg and higher concentrations of GV1001, the hemorrhage in the heart was attenuated, while severe congestion was reported in the control group. Apoptotic cells, myeloperoxidase activity and inflammatory cytokines [tumor necrosis factor (TNF)-α and interleukin (IL)-6] revealed decreased levels in a dose-dependent manner with respect to GV1001 concentration. The group treated with 10 mg/kg GV1001 demonstrated 59.73% apoptotic cells (P<0.001), 48.14% neutrophil contents (P<0.001), 55.63% TNF-α (P<0.01) and 42.35% IL-6 (P<0.01) levels, compared with the control group. The novel vaccine peptide GV1001 provided protective effects on myocardial ischemia-reperfusion injury and, therefore, it should be considered as an alternative potential anti-inflammatory agent for myocardial ischemia-reperfusion injury.