Traditional herbal drugs against liver diseases – Experimented in vitro using HepG2 cells for induced steatosis

Salvia fruticosa leaves, Malva sylvestris flowers, Taraxacum officinale aerial parts, Plantago ovata seeds, Tanacetum parthenium aerial parts, and Allium sativum bulbs are documented for traditional use against hepatic disorders and different liver diseases. To evaluate herbal drug material for potential use against liver diseases, at molecular level for the efficacy linked to ethnobotanical documented data.Different herbal extracts were prepared and standardized by HPLC, according to European Pharmacopoeia. Initially 0.25 mg/mL each standardized extract was applied to oleic+palmitic acid induced fatty liver using a HepG2 cell culture model. ALT, AST, GSH, and MDA levels were comparatively analyzed, in addition to cell Nil Red staining. The highest activity for MDA reduction was observed for the A. sativum extract at 48.2% level, followed by 36.4% for M. sylvestris, and S. fruticosa extracts with 27.3% reduction, respectively. Glutathione levels increased to 59.1% when A. sativum extract was applied. M. sylvestris extract increased the glutathione levels in the medium by 49.7%; S. fruticosa extract decreased ALT levels by 53.5% and M. sylvestris extract by 38.5%, whereas the standard resveratrol reduced ALT level by 30.9%, respectively. The AST levels for M. sylvestris extract was 46.5%, compared to resveratrol by 93%. A. sativum, M. sylvestris, and S. fruticosa standard extracts showed relatively good correlation and activity where further in vivo studies should be performed

Phlomis Pungens’in fitokimya ve in vitro farmakolojik etkilerinin değerlendirilmesi

Objective: This study aimed to investigate the in vitro wound healing, anti-inflammatory, antimicrobial and antioxidant activity of Phlomis pungens Willd. extract derived from the aerial parts. Material and Method: The phytochemical analysis was performed using GC-MS in order to identify the volatile components of the bioactive Hex extract. The wound healing activity of P. pungens extract was evaluated based on in vitro antimicrobial, antioxidant, anti-inflammatory, and, scratch activity was studied. In addition, the in vitro cytotoxicity of the extract was also evaluated. Result and Discussion: P. pungens methanol extract depicted a 5-LOX inhibitory activity at 78.2µg/mL (IC50), while the antioxidant activity by DPPH radical provided an IC50=2.41mg/mL, and the ABTS radical showed IC50=3.32mg/mL, respectively. The extract showed dose-dependently anti-inflammatory activity while L-NAME and P. pungens methanol extract significantly decreased LPS stimulated PGE2 production. According to the scratch assay results, all treatments led to an increase in cell migration rate with a dose-dependent effect. Our findings suggested that P. pungens methanol extract may have a role in wound healing according to the scratch test, and it is thought that its antioxidant and anti-inflammatory activity also contributed. Further evaluations are ongoing to confirm the in vitro activity under in vivo conditions.Amaç: Bu çalışmada, Phlomis pungens Willd. topraküstü kısımlarından elde edilen ekstrelerin in vitro yara iyileşmesi, antiinflamatuar, antimikrobiyal ve antioksidan aktivitesinin araştırılması amaçlanmıştır. Gereç ve Yöntem: Biyoaktif hekzan ekstresinin uçucu bileşenlerini belirlemek için fitokimyasal analiz GC-MS kullanılarak yapılmıştır. P. pungens ekstresinin yara iyileştirme aktivitesi, in vitro antimikrobiyal, antioksidan, antiinflamatuar etkinlikleri değerlendirilmiş ve ek olarak ekstrenin in vitro sitotoksisitesi de değerlendirilmiştir. Sonuç ve Tartışma: P. pungens metanol ekstresi, 78,2 µg/mL'de (IC50) 5-LOX inhibe edici aktivite gösterirken, DPPH yöntemi ile antioksidan aktivitesi IC50=2.41mg/mL ve ABTS IC50=3.32 mg/mL olarak bulunmuştur. Ekstre, doza bağlı olarak anti-inflamatuar aktivite gösterirken, L-NAME ve P. pungens metanol ekstresi, LPS ile uyarılan PGE2 üretimini önemli ölçüde azaltmıştır. Strach metodu sonuçlarına göre doza bağlı etki ile hücre göç hızında bir artış gözlemlenmiştir. Bulgularımız, starch testine göre P. pungens metanol ekstresinin yara iyileşmesinde rol oynayabileceğini ve antioksidan ve antiinflamatuar aktivitesinin de katkıda bulunduğu düşündürmüştür. İn vivo koşullar altında in vitro aktiviteyi doğrulamak için başka değerlendirmeler devam etmektedir

Antimicrobial, cytotoxic, antiviral wffects, and apectroscopic characterization of metabolites produced by fusarium oxysporum YP9B

The goal of the work is to determine the bioactive pharmaceutical metabolites produced by the Fusarium oxysporum YP9B isolate. Ten new natural compounds were isolated from the ethyl acetate extract of the F. oxysporum YP9B strain. Their structures were elucidated by spectroscopic methods using 1D and 2D NMR, UV, FT-IR, and mass spectra (LC-QTOF MS and GC-FID/MS). Identified compounds were named as; (1-benzyl-2-methoxy-2-oxoethyl)-2-hydroxy-3-methylbutanoate (1), 2-oxo-8-azatricyclo[9.3.1.1(3,7)]-hexadeca-1(15),3(16),4,6,11,13-hexaen-10-one (2), 2,3-dihydroxypropanoic, hexadecanoic anhydride (3a), 2,3-dihydroxypropanoic (9Z)-octadecenoic anhydride (3b), 2,3-dihydroxy-propanoic (9Z,12Z)-octadecadienoic anhydride (3c), 2,3-dihydroxypropanoic (11Z)-octadecenoic anhydride (4a), 2,3-dihydroxypropanoic, (9E,12E)-octadecadienoic anhydride (4b), 3-hydroxy-1,2,6,10-tetramethylundecyl hexzadecanoate (5a), 3-hydroxy-1,2,6,10-tetramethylundecyl (9E)-octadecaenoate (5b), and 3-hydroxy-1,2,6,10-tetramethylundecyl octadecanoate (5c). Antimicrobial activities of the isolates obtained from the YP9B strain were determined. Cytotoxic and antiviral activities were tested for the isolates against VERO, MCF-7, PC-3, and A549. Compounds 5a-c, 1, and 3a-c showed bacteriostatic activity at low concentrations, and 4a-b and 2 were found to be bactericides. MIC and MBC values against Mycobacterium smegmatis for the compounds 5a-c and 1 were determined to be <0.5 mu g/mL and 0.46 mu g/mL, respectively. The experimental result showed that compounds 2, 5a-c and 1 have strong cytotoxic (7.51 +/- 1.38 and 19.13 +/- 0.68 (mu M) IC50) activity. The antiviral activity against HSV type-1 was determined to be 1.25 mu M for compounds 4a-c and 0.312 mu M for compound 1

Discovery of Novel Thiophene/Hydrazones: In Vitro and In Silico Studies against Pancreatic Cancer

Cancer is the disease with the highest mortality. Drug studies contribute to promising treatments; however there is an urgent need for selective drug candidates. Pancreatic cancer is difficult to treat and the cancer progresses rapidly. Unfortunately, current treatments are ineffective. In this study, ten new diarylthiophene-2-carbohydrazide derivatives were synthesized and evaluated for their pharmacological activity. The 2D and 3D anticancer activity studies suggested the compounds 7a, 7d, and 7f were promising. Among these, 7f (4.86 µM) showed the best 2D inhibitory activity against PaCa-2 cells. Compounds 7a, 7d and 7f were also tested for their cytotoxic effects on healthy cell line but only compound 7d showed selectivity. Compounds 7a, 7d, and 7f showed the best 3D cell line inhibitory effect according to spheroid diameters. The compounds were screened for their COX-2 and 5-LOX inhibitory activity. For COX-2, the best IC50 value was observed for 7c (10.13 µM) and all compounds showed significantly lower inhibition compared to standard. In the 5-LOX inhibition study, compounds 7a (3.78 µM), 7c (2.60 µM), 7e (3.3 µM), and 7f (2.94 µM) demonstrated influential activity compared to standard. Regarding molecular docking studies, binding mode of compounds 7c, 7e, and 7f to the 5-LOX enzyme were non-redox or redox types, but not the iron-binding type. As dual inhibitors of 5-LOX and pancreatic cancer cell line, 7a and 7f were identified as the most promising compounds

Antimutagenic and anticlastogenic effects of Turkish Black Tea on TA98 and TA100 strains of Salmonella typhimurium (in vitro) and mice (in vivo)

Context: Black tea has been reported to have significant antimutagenic and anticarcinogenic properties associated with its polyphenols theaflavins (TF) and thearubigins (TR). Similarly, Turkish black tea (TBT) also contains a considerable amount of TF and TR. Objective: This study investigated the mutagenic, antimutagenic and anticlastogenic properties of TBT. Materials and methods: The mutagenic and antimutagenic effects of TBT (10 to 40000 μg/plate) were investigated in vitro on Salmonella strains TA98 and TA100 with and without S9 fraction. Anticlastogenic effect was studied at concentrations of 300–1200 mg/kg TBT extract by chromosomal aberrations (CA) assay from bone marrow of mice. Results: The results of this study did not reveal any mutagenic properties of TBT. On the contrary, TBT extract exhibited antimutagenic activity at >1000 μg/plate concentrations in TA98 strain with and without S9 activation (40% inhibition with S9 and 27% without S9). In TA100 strain, the antimutagenic activity was observed at >20,000 μg/plate TBT extracts without S9 activation (28% inhibition) and at >1000 μg/plate with S9 activation (59% inhibition). A significant decrease in the percentage of aberrant cells (12.33% ± 1.27) was observed in dimethylbenz(a)anthracene (DMBA) plus highest concentration (1200 mg/kg) of TBT extract-treated group when compared to only DMBA-treated group (17.00% ± 2.28). Discussion and conclusion: Results indicated that TBT can be considered as genotoxically safe, because it did not exert any mutagenic and clastogenic effects. As a result, TBT exhibited antimutagenic effects more apparently after metabolic activation in bacterial test system and had an anticlastogenic effect in mice