Objective Pneumonia remains a leading cause of morbidity and mortality worldwide. Pluchea pteropoda has shown in vitro anti-inflammatory and antibacterial activities, but its effects in pneumonia are unknown. This study assessed the preliminary oral tolerability of P. pteropoda extract (PP) and its protective effects in a predominantly prophylactic, cyclophosphamide-immunosuppressed mouse model of Streptococcus pneumoniae lung infection. Methods Acute (5 g/kg) and 28-day repeated-dose (290, 870 and 1450 mg/kg) oral toxicity were evaluated in Swiss albino mice of both sexes following Vietnamese Ministry of Health guidance (Decision No. 141/QĐ-K2ĐT), with reference to, but not full compliance with, OECD Test Guidelines 420 and 407. Cyclophosphamide-leukopenic mice received PP orally, alone or with ceftriaxone (CTX), from 14 days before to 3 days after intranasal S. pneumoniae challenge. The primary outcome was relative lung weight; white blood cell (WBC) count and lung histopathology were secondary. Results A dose of 5 g/kg caused no mortality or clinical signs over 14 days. Over 28 days, no mortality or liver and kidney histological changes occurred; lower WBC count and higher total and direct bilirubin occured at 870 mg/kg only, without a dose–response relationship. In infected mice, all PP-treated groups, with or without CTX, had lower relative lung weight than the untreated pneumonia group (p < 0.001). PP 1450 mg/kg, alone or with CTX, was associated with higher WBC counts (p = 0.0075 and 0.0039, respectively), and PP 870 and 1450 mg/kg (alone or with CTX) with lower lung edema scores. Conclusion PP was tolerated at the doses tested, and prophylactic administration was associated with reduced lung weight and edema in immunosuppressed mice infected with S. pneumoniae . These preliminary observations do not establish antibacterial or therapeutic efficacy and require confirmation using quantitative bacterial burden, a standardized extract and post-infection treatment.
Objectives Bacterial resistance to current antibiotics is escalating at an alarming rate, rendering many conventional drugs ineffective and creating an urgent global health crisis; therefore, there is a critical need for the discovery of new antibacterial hits from underexplored natural sources such as marine sponges. This study aimed to isolate and characterize secondary metabolites from the Red Sea sponge Callyspongia fistularis and evaluate their antimicrobial activity against several pathogens. Methods The organic extract of the sponge was subjected to bioassay-guided fractionation using VLC and Dep-Pak C18, Sephadex LH-20 C18, and C18 HPLC. Compound structures were elucidated by NMR and (+)-HRESIMS. Antimicrobial activity was evaluated at 200 μg/disk and broth microdilution MIC assays. Results Four compounds were isolated including ( E )-3-(4-chlorophenyl)acrylic acid ( 1 ), ( Z )-3-(4-chlorophenyl)acrylic acid ( 2 ), 1-methyl( E )-3-(4-chlorophenyl)acrylate ( 3 ), and N -(4-hydroxyphenethyl)acetamide ( 4 ). In the Disk Diffusion and MIC determinations, 2 showed weak activity against S. aureus (10.5 mm; MIC = 213.33 μg/mL) and was inactive against E. coli , C. albicans , and MRSA, with a profile nearly identical to 1 (10.83 mm against S. aureus , MIC = 213.33 μg/mL; inactive against the other pathogens). Compound 3 exhibited improved activity against S. aureus (16.5 mm and 85.33 μg/mL), E. coli (14.5 mm and 213.33 μg/mL), and C. albicans (14.8 mm and 213.33 μg/mL), but remained inactive against MRSA, while 4 was essentially inactive against all pathogens. All compounds were significantly less potent than imipenem and clotrimazole ( P < 0.001). Conclusion This study reports the first natural occurrence of compounds 2 and 3 from a natural source and compounds 1 and 2 from a marine source. Compound 3 was the most active compound in this series, though still weak compared to clinical standards. None of the compounds exhibited anti-MRSA activity. Further structural optimization, including ester chain elongation and aromatic substitution, is required to improve potency.
Objective Artocarpus lacucha Roxb. (Moraceae), locally known as Monkey jack (Dewa), is traditionally used in Bangladesh to treat diarrhea, inflammation and metabolic disorders. However, scientific validation of its pharmacological potential remains limited. This study aimed to investigate the hypoglycemic, analgesic and anti-inflammatory activities of the ethanolic extract of A. lacucha leaves (EAL) in a mouse model, identify its bioactive compounds using gas chromatography-mass spectrometry (GC-MS) and evaluate molecular interactions through in silico studies. Methods Leaves were extracted using cold maceration with 95% ethanol. Hypoglycemic activity was assessed using an oral glucose tolerance test (OGTT) in Swiss albino mice at doses of 250 mg/kg and 500 mg/kg body weight (BW). Anti-inflammatory and analgesic activities were evaluated using formalin-induced paw edema and biphasic paw-licking models. GC–MS analysis was performed to identify phytoconstituents. Molecular docking against selected antidiabetic and anti-inflammatory targets (5YW7, 3BAJ and 5KIR) and a complementary protein-binding and transport target (7JWN) and ADMET properties were predicted using pkCSM. Results EAL significantly reduced blood glucose levels ( p<0.05 ) in OGTT compared to control. In the paw edema model, EAL significantly inhibited formalin-induced inflammation in a time and dose-dependent manner ( p<0.001 ), with the 500 mg/kg BW dose showing pronounced edema reduction comparable to standard drugs. In the licking test, EAL significantly reduced nociceptive responses in both early (neurogenic) and late (inflammatory) phases ( p<0.001 ). GC-MS analysis revealed multiple bioactive compounds, including phenolics and terpenoids. Docking analysis demonstrated favorable binding affinities with target proteins, supporting potential antidiabetic and anti-inflammatory mechanisms, while interactions with HSA provided complementary information regarding potential protein-binding behavior. Conclusion The findings indicate that the ethanolic leaf extract of A. lacucha exhibits preliminary glucose-lowering, antinociceptive and anti-inflammatory activities. GC–MS, molecular docking, ADMET analyses provide tentative phytochemical and computational support. Further bioactivity-guided isolation, mechanistic, pharmacokinetic and toxicological studies are needed to confirm its therapeutic potential.
Objective This study evaluated the influence of geographical origin and climatic conditions in Algeria on the phytochemical profile, mineral composition, and biological activities of hydro-ethanolic leaf extracts from Lippia citriodora . Methods Samples (LC1–LC4) were collected from four distinct regions. Total phenolic and flavonoid contents were measured, and biological potential was assessed via antioxidant (DPPH, FRAP), photoprotective (SPF), anti-inflammatory, antimicrobial, larvicidal, enzymatic inhibition assays (AChE, BChE, α-amylase, tyrosinase, and urease). Statistical significance was determined using ANOVA and t-tests. Results Environmental stress in the arid region (Ghardaia, LC4) stimulated the highest antioxidant capacity (DPPH IC 50 = 38.87 µg/mL). All extracts exhibited excellent photoprotective properties with SPF values exceeding 39. The most significant variations were observed in enzymatic assays: the extract from the sub-coastal region (Tipaza, LC3) was identified as the most potent tyrosinase inhibitor (67.35% inhibition at 3.125 µg/mL; p < 0.01 vs. LC4) and the only sample active against α-amylase. Urease inhibition remained high across all regions (IC 50 < 20 µg/mL). Extract (Jijel, LC 1) being the only sample to exhibit significant antibacterial activity. Extracts (Djelfa, LC2) and LC4 displayed lower toxicity, both presenting higher LD 50 values (269.15 µg/mL). Conclusions : The multidisciplinary screening of L . citriodora leaves extracts proves that environmental stress factors across Algerian regions (arid, semi-arid, and humid) create distinct ‘chemical signatures’. The arid region (Ghardaia) optimizes protective metabolites, while the humid coastal regions (Jijel, Tipaza) trigger the synthesis of aggressive defense molecules (antibacterial and larvicidal). This regional differentiation allows for the strategic selection of raw materials tailored to specific industrial needs. The selection of the cultivation site is crucial for achieving specific therapeutic outcomes, with sub-coastal regions favoring enzymatic inhibition and arid regions maximizing antioxidant potential.
Objective Artocarpus lacucha Roxb. (Moraceae), locally known as Monkey jack (Dewa), is traditionally used in Bangladesh to treat diarrhea, inflammation and metabolic disorders. However, scientific validation of its pharmacological potential remains limited. This study aimed to investigate the hypoglycemic, analgesic and anti-inflammatory activities of the ethanolic extract of A. lacucha leaves (EAL) in a mouse model, identify its bioactive compounds using gas chromatography-mass spectrometry (GC-MS) and evaluate molecular interactions through in silico studies. Methods Leaves were extracted using cold maceration with 95% ethanol. Hypoglycemic activity was assessed using an oral glucose tolerance test (OGTT) in Swiss albino mice at doses of 250 mg/kg and 500 mg/kg body weight (BW). Anti-inflammatory and analgesic activities were evaluated using formalin-induced paw edema and biphasic paw-licking models. GC–MS analysis was performed to identify phytoconstituents. Molecular docking against selected antidiabetic and anti-inflammatory targets (5YW7, 3BAJ and 5KIR) and a complementary protein-binding and transport target (7JWN) and ADMET properties were predicted using pkCSM. Results EAL significantly reduced blood glucose levels ( p<0.05 ) in OGTT compared to control. In the paw edema model, EAL significantly inhibited formalin-induced inflammation in a time and dose-dependent manner ( p<0.001 ), with the 500 mg/kg BW dose showing pronounced edema reduction comparable to standard drugs. In the licking test, EAL significantly reduced nociceptive responses in both early (neurogenic) and late (inflammatory) phases ( p<0.001 ). GC-MS analysis revealed multiple bioactive compounds, including phenolics and terpenoids. Docking analysis demonstrated favorable binding affinities with target proteins, supporting potential antidiabetic and anti-inflammatory mechanisms, while interactions with HSA provided complementary information regarding potential protein-binding behavior. Conclusion The findings indicate that the ethanolic leaf extract of A. lacucha exhibits preliminary glucose-lowering, antinociceptive and anti-inflammatory activities. GC–MS, molecular docking, ADMET analyses provide tentative phytochemical and computational support. Further bioactivity-guided isolation, mechanistic, pharmacokinetic and toxicological studies are needed to confirm its therapeutic potential.
