Madu gelam telah didapati mempunyai kesan anti-oksidatif, anti-kanser dan antiinflamasi
terhadap banyak jenis kanser. Tujuan kajian ini adalah untuk menentukan
kesan madu gelam terhadap aras tekanan oksidatif sel kanser peparu manusia.
IC50 madu gelam ditentukan dengan merawat sel A549 dengan dos madu yang
berbeza (50-200 mg/ml). Sel dibahagikan kepada 4 kumpulan dan diaruh tekanan
oksidatif dengan menggunakan hidrogen peroksida (H2
) mengikut kumpulan
tertentu: kawalan, H2
, madu gelam, H2
+ madu gelam. Selepas 24 jam
rawatan, biopetanda tekanan oksidatif seperti malondialdehid (MDA) dan protein
karbonil ditentukan. Aruhan tekanan oksidatif meningkatkan aras MDA (p
The present study was conducted to determine the effect of air (AD), oven (OD) and freeze drying (FD) on the free radical scavenging activity and total phenolic content (TPC) of Cosmos caudatus and the effect of storage time by the comparison with a fresh sample (FS). Among the three drying methods that were used, AD resulted in the highest free radical scavenging activity against 1,1-diphenyl-2-picrylhydrazyl (DPPH) (IC50 = 0.0223 mg/mL) and total phenolic content (27.4 g GAE/100 g), whereas OD produced the lowest scavenging activity and TPC value. After three months of storage, the dried samples showed a high and consistent free radical scavenging activity when compared to stored fresh material. The drying methods could preserve the quality of C. caudatus during storage and the stability of its bioactive components can be maintained.
6-Chloro-2-Aryl-1H-imidazo[4,5-b]pyridine derivatives 1-26 were synthesized and characterized by various spectroscopic techniques. All these derivatives were evaluated for their antiglycation, antioxidant and β-glucuronidase potential followed their docking studies. In antiglycation assay, compound 2 (IC50=240.10±2.50μM) and 4 (IC50=240.30±2.90μM) was found to be most active compound of this series, while compounds 3 (IC50=260.10±2.50μM), 6 (IC50=290.60±3.60μM), 13 (IC50=288.20±3.00μM) and 26 (IC50=292.10±3.20μM) also showed better activities than the standard rutin (IC50=294.50±1.50μM). In antioxidant assay, compound 1 (IC50=69.45±0.25μM), 2 (IC50=58.10±2.50μM), 3 (IC50=74.25±1.10μM), and 4 (IC50=72.50±3.30μM) showed good activities. In β-glucuronidase activity, compounds 3 (IC50=29.25±0.50μM), compound 1 (IC50=30.10±0.60μM) and compound 4 (IC50=46.10±1.10μM) showed a significant activity as compared to than standard D-Saccharic acid 1,4-lactonec (IC50=48.50±1.25μM) and their interaction with the enzyme was confirm by docking studies.
Alpinia conchigera (lengkuas kecil) merupakan sejenis tumbuhan herba yang sering digunakan sebagai rawatan alternatif
dalam bidang perubatan tradisional. Kajian ini dijalankan untuk menilai kesan sitotoksik, genotoksik serta mod kematian
sel yang disebabkan oleh ekstrak heksana A. conchigera ke atas sel hepar Chang. Asai MTT selama 24 jam telah dijalankan
untuk mengenal pasti peratus viabiliti sel hepar Chang setelah dirawat dengan ekstrak heksana A. conchigera. Keputusan
menunjukkan terdapat penurunan viabiliti sel secara signifi kan (p < 0.05) dengan nilai IC50 (8.6 μg/ml) berbanding kawalan
negatif. Berdasarkan nilai IC50 ini, pewarnaan AO/PI dilakukan untuk menentukan mod kematian sel hepar Chang iaitu sama
ada secara apoptosis atau nekrosis. Didapati bahawa terdapat perbezaan secara signifi kan (p < 0.05) bagi mod kematian
sel hepar Chang secara apoptosis berbanding kawalan negatif. Dalam kajian ini, penentuan tahap kerosakan DNA sel
hepar Chang turut dilakukan dengan menggunakan asai komet beralkali dengan nilai IC10 dan IC25 yang diperoleh daripada
asai MTT (4 μg/ml dan 6 μg/ml) masing-masing. Setelah sel hepar Chang dirawat dengan ekstrak heksana A. conchigera
selama 2 jam, didapati terdapat perbezaan secara signifi kan (p < 0.05) bagi peratus kerosakan DNA bagi kumpulan rawatan
berbanding kawalan negatif. Kesimpulannya, ekstrak heksana A. conchigera memberi kesan sitotoksik dan genotoksik
terhadap sel hepar Chang serta menyebabkan kematian sel secara apoptosis.
2-Indolcarbohydrazones 1-28 were synthesized and evaluated for their α-glucosidase inhibitory potential. A varying degree of inhibitory potential with IC50 values in the range of 2.3±0.11-226.4±6.8μM was observed while comparing these outcomes with the standard acarbose (IC50=906.0±6.3μM). The stereochemistry of ten (10) randomly selected compounds (1, 3, 6, 8, 12, 18, 19, 23, 25 and 28) was predicted by Density Functional Theory (DFT). The stability of E isomer was deduced by comparing the calculated and experimental vibration modes of νCO, νNC and νCH (CH in NCH-R). It was observed that except compound 18, all other compounds were deduced to have E configuration while molecular modeling studies revealed the key interactions between enzyme and synthesized compounds.
Kesan sitotoksik sebatian organostanum (IV) terhadap pelbagai sel kanser telah dikaji oleh para saintis di seluruh dunia.Dalam kajian ini,dua sebatian baru organostanum (IV) iaitu difenilstanum (IV) etilfenilditiokarbamat (DFEF) dan difenilstanum (IV) butilfenilditiokarbamat (DFBF) telah diuji kesan sitotoksiknya terhadap sel eritroleukemia, K562. Sel eritroleukemia, K562 merupakan sel sasaran manakala, sel hepar Chang dan sel fibroblas V79 pula digunakan untuk menilai kesan kedua-dua sebatian ini terhadap sel bukan kanser. Kesan sitotoksik sebatian DFEF dan DFBF diuji menggunakan ujian asai 3-(4,5-dimetiltiazol-2-il)-2, 5-difeniltetrazolium bromida (MTT) dengan masa pendedahan 24 jam, 48 jam dan 72 jam pada kepekatan sebatian yang berbeza. Pemerhatian terhadap perubahan morfologi juga dilakukan menggunakan nilai IC50 yang diperolehi pada masa pendedahan seperti ujian asai MTT. Ujian sitotoksisiti telah menunjukkan sebatian DFEF dan DFBF adalah sangat toksik terhadap sel K562 dengan nilai IC50 kurang daripada 10 μM untuk ketiga-tiga masa pendedahan.Indeks pemilihan juga membuktikan bahawa kedua-dua sebatian memberikan kesan sitotoksik secara memilih terhadap sel K562 pada masa 48 jam dan 72 jam, tetapi pada masa 24 jam, sebatian ini bertindak secara tidak memilih terhadap sel K562 dan sel bukan kanser. Perubahan morfologi yang diperhatikan adalah menyerupai ciri-ciri apoptosis seperti pengecutan sel dan pembentukan jasad apoptotik dan juga nekrosis seperti sel lisis. Kesimpulannya, sebatian difenilstanum (IV) alkilfenilditiokarbamat berpotensi untuk dibangunkan sebagai agen antileukemia tetapi mekanisma khusus tindakan sebatian ini terhadap sel K562 perlu dikaji pada masa akan datang untuk menjelaskan potensi sebatian ini sebagai dadah antikanser yang baru.
A series of hydrazinecarboxamide derivatives were synthesized and examined against urease for their inhibitory activity. Among the series, the 1-(3-fluorobenzylidene)semicarbazide (4a) (IC50 = 0.52 ± 0.45 µM), 4u (IC50 = 1.23 ± 0.32 µM) and 4h (IC50 = 2.22 ± 0.32 µM) were found most potent. Furthermore, the molecular docking study was also performed to demonstrate the binding mode of the active hydrazinecarboxamide with the enzyme, urease. In order to estimate drug likeness of compounds, in silico ADME evaluation was carried out. All compounds exhibited favorable ADME profiles with good predicted oral bioavailability.
A new class of triazinoindole-bearing thiosemicarbazides (1-25) was synthesized and evaluated for α-glucosidase inhibitory potential. All synthesized analogs exhibited excellent inhibitory potential, with IC50 values ranging from 1.30 ± 0.01 to 35.80 ± 0.80 µM when compared to standard acarbose (an IC50 value of 38.60 ± 0.20 µM). Among the series, analogs 1 and 23 were found to be the most potent, with IC50 values of 1.30 ± 0.05 and 1.30 ± 0.01 µM, respectively. The structure-activity relationship (SAR) was mainly based upon bringing about different substituents on the phenyl rings. To confirm the binding interactions, a molecular docking study was performed.
4-Thiazolidinone analogs 1-20 were synthesized, characterized by (1)H NMR and EI-MS and investigated for urease inhibitory activity. All twenty (20) analogs exhibited varied degree of urease inhibitory potential with IC50 values 1.73-69.65μM, if compared with standard thiourea having IC50 value of 21.25±0.15μM. Among the series, eight derivatives 3, 6, 8, 10, 15, 17, 19, and 20 showed outstanding urease inhibitory potential with IC50 values of 9.34±0.02, 14.62±0.03, 8.43±0.01, 7.3±0.04, 2.31±0.002, 5.75±0.003, 8.81±0.005, and 1.73±0.001μM, respectively, which is better than the standard thiourea. The remaining analogs showed good to excellent urease inhibition. The binding interactions of these compounds were confirmed through molecular docking studies.
Thiadiazole derivatives 1-24 were synthesized via a single step reaction and screened for in vitro β-glucuronidase inhibitory activity. All the synthetic compounds displayed good inhibitory activity in the range of IC50=2.16±0.01-58.06±1.60μM as compare to standard d-saccharic acid 1,4-lactone (IC50=48.4±1.25μM). Molecular docking study was conducted in order to establish the structure-activity relationship (SAR) which demonstrated that thiadiazole as well as both aryl moieties (aryl and N-aryl) involved to exhibit the inhibitory potential. All the synthetic compounds were characterized by spectroscopic techniques (1)H, (13)C NMR, and EIMS.
Benzimidazole analogs 1-27 were synthesized, characterized by EI-MS and (1)HNMR and their α-glucosidase inhibitory activities were found out experimentally. Compound 25, 19, 10 and 20 have best inhibitory activities with IC50 values 5.30±0.10, 16.10±0.10, 25.36±0.14 and 29.75±0.19 respectively against α-glucosidase. Compound 6 and 12 has no inhibitory activity against α-glucosidase enzyme among the series. Further studies showed that the compounds are not showing any cytotoxicity effect. The docking studies of the compounds as well as the experimental activities of the compounds correlated well. From the molecular docking studies, it was observed that the top ranked conformation of all the compounds fit well in the active site of the homology model of α-glucosidase.
Introduction: Benzimidazole analogues are bicyclic compounds that had been synthesized comprising the fusion of benzene and imidazole. It gains interest in research as it poses numerous therapeutic potential such as anti-ulcer, anti-malarial, anti-helminthic, anti-fungal, anti-inflammatory, and anti-cancer. Hence, this work aims to screen novel benzimidazole analogues using MTT assay for potential anti-proliferation activities on gastric cancer, which is the second cause of cancer-related death. Methods: MTT assay was conducted following standard protocol on HGT-1 gastric cancer cells. Cells were seeded and allowed to attach overnight before being introduced with various con-centration of benzimidazole analogues up to 72 hours and the optical density of the MTT was recorded using 560 nm wavelength. Two-Way ANOVA was used to analyse all data, followed by post-hoc Tukey test and the structure analysis relationship was analysed using MTT result. Results: From five analogues, only compound 4 showed an-ti-proliferation activity with IC50 8.212 ± 0.813 μM at 72 hours. Compound 4 had hydroxyl group at ortho- and para- position and remarkably, compound 2 which contained the hydroxyl group at ortho- and meta- position together with compound 5 which contained the combination of meta- and para- induced proliferation on gastric cancer. Conclusion: Different position of hydroxyl group on the benzene ring gives different activities on gastric cancer and from the experiment, only compound 4 had the anti-proliferative activity.
The present study was conducted to evaluate the antioxidant activity of Vernonia cinerea, Peperomia
pellucida and combination of Vernonia cinerea and Peperomia pellucida. These two herbs are pants that
often grow at random in different environments but are not commercialized due to the fact that no
comprehensive study of the importance of their use. The extract was prepared with methanol respectively.
1,1-diphenyl-2-picrylhydrazyl (DPPH) assay were used to study their antioxidant activity. The extracts
were compared with commercial antioxidant, butylated hydroxytoluene (BHT). The highest scavenging
effect from peel extract was presented by Vernonia cinerea with the value of 76.3% scavenging activity
(IC50 = 2.909), followed by the combination of Vernonia cinerea and Peperomia pellucida (71.21%
scavenging activity; IC50 = 5.274) and Peperomia pellucida with value of 68.3% scavenging activity (IC50
= 5.572). BHT showed the lowest IC50 value 1.71 with the scavenging activity 90.0%. Low IC50 value will
indicates the strong ability of the extracts to act as DPPH scavenger.
The present study was conducted to evaluate the antioxidant activity of peel extract from three types of
melon, Cucumis melo var cantalupensis, Cucumis melo var inodorus and Citrullus lanatus in family
Curcurbitaceae. The extract was prepared with methanol respectively. 1,1-diphenyl-2-picrylhydrazyl
(DPPH) assay were used to study their antioxidant activity. The extracts were compared with commercial
antioxidant, butylated hydroxytoluene (BHT). The highest scavenging effect from peel extract was
presented by Cucumis melo var inodorus with the value of 52.7 ± 9.1µg/ml (IC50 = 4.61). BHT showed
the lowest IC50 value 1.71 with the scavenging activity 90.0 ± 1.7µg/ml. Low IC50 value will indicates the
strong ability of the extracts to act as DPPH scavenger.
In search of potent α-amylase inhibitor we have synthesized eighteen indole analogs (1-18), characterized by NMR and HR-EIMS and screened for α-amylase inhibitory activity. All analogs exhibited a variable degree of α-amylase inhibition with IC50 values ranging between 2.031 ± 0.11 and 2.633 ± 0.05 μM when compared with standard acarbose having IC50 values 1.927 ± 0.17 μM. All compounds showed good α-amylase inhibition. Compound 14 was found to be the most potent analog among the series. Structure-activity relationship has been established for all compounds mainly based on bringing about the difference of substituents on phenyl ring. To understand the binding interaction of the most active analogs molecular docking study was performed.
Desert truffles are seasonal and important edible fungi that grow wild in many countries around the world. Truffles are natural food sources that have significant compositions. In this work, the antioxidant, chemical composition, anticancer, and antiangiogenesis properties of the Terfezia claveryi truffle were investigated. Solvent extractions of the T. claveryi were evaluated for antioxidant activities using (DPPH, FRAP and ABTS methods). The extracts cytotoxicity on the cancer cell lines (HT29, MCF-7, PC3 and U-87 MG) was determined by MTT assay, while the anti-angiogenic efficacy was tested using ex-vivo assay. All extracts showed moderate anticancer activities against all cancer cells (p 50 μg/ml and significantly promoted cell apoptosis through the mitochondrial pathway and DNA fragmentation p
Previously, we synthesized triazoloquinazolines 1-14 and characterized their structure. In this study, we aimed to evaluate the in vitro activity of the targets 1-14 as α-glucosidase inhibitors using α-glucosidase enzyme from Saccharomyces cerevisiae type 1. Among the tested compounds, triazoloquinazolines 14, 8, 4, 5, and 3 showed the highest inhibitory activity (IC50 = 12.70 ± 1.87, 28.54 ± 1.22, 45.65 ± 4.28, 72.28 ± 4.67, and 83.87 ± 5.12 μM, respectively) in relation to that of acarbose (IC50 = 143.54 ± 2.08 μM) as a reference drug. Triazoloquinazolines were identified herein as a new class of potent α-glucosidase inhibitors. Molecular docking results envisaged the plausible binding interaction between the target triazoloquinazolines and α-glucosidase enzyme and indicated considerable interaction with the active site residues.
A phytochemical investigation of the stem bark of Calophyllum canum resulted in the isolation of a new xanthone dimer identified as biscaloxanthone (1), together with four compounds; trapezifoliaxanthone (2), trapezifolixanthone A (3), taraxerone (4) and taraxerol (5). The structures of these compounds were determined via spectroscopic methods of IR, UV, MS and NMR (1D and 2D). The cytotoxicity of compounds 1-3 were screened against A549, MCF-7, C33A and 3T3L1 cell lines, wherein weak cytotoxic activities were observed (IC50 > 50 μm).
Introduction: Piper sarmentosum is one of the herbaceous plants that has been used as natural antioxidant to source to treat diseases. This study was conducted to determine the total phenolic contents (TPC) and free radical scavenging capacity in free and bound (soluble and insoluble) of P. sarmentosum. Methods: Free phenolic extract was acquired through direct methanol extraction while acidic and alkaline hydrolyses were adopted to release the bound phenolic acids. The TPC was determined by using Folin-Ciocalteu assay and is expressed as Gallic Acid equivalent (GAE) in miligrams per gram of extracts. The antioxidant scavenging capacity was determined by using DPPH (2, 2-diphenyl-1-picrylhydrazyl) assay. Results: Insoluble bound phenolic extract of P. sarmentosum showed the highest TPC value (1.54 ± 0.04 mg GAE/g DW) followed by soluble phenolic extract and free extract (1.13 ± 0.10 and 0.57 ± 0.06 mg GAE/g DW, respectively). The soluble phenolic fraction has expressed the highest free radical scavenging capacity (76.57± 4.12%) followed by insoluble (69.79± 2.33 %) and free extracts (58.15± 4.44 %). The IC50 values for free, soluble and insoluble bound phenolic were 24.05 ± 3.81, 16.17 ± 1.84 and 18.49 ± 1.92 mg/ml, respectively. Conclusions: The significant differences between all the extracts and antioxidant inhibition in this present study suggested that different forms (free and bound) of extracts did influence the radical scavenging capacity as a whole.
Introduction: Clinacanthus nutans is used as natural nutraceuticals for prevention and treatment of cancer. The purpose of this study is to (i) determine the total phenolic content and antioxidant scavenging capacities of C. nutans in free and bound phenolic acid and (ii) study the relationship between TPC and antioxidant scavenging capacities of C. nutans. Methods: The total phenolic contents were measured using Folin-Ciocalteu assay. Free and bound phenolic were examined by using spectrophotometer while antioxidant capacity were evaluated using DPPH (2, 2-diphenyl-1-picrylhydrazyl) scavenging activity assay. Results: Insoluble phenolic acids showed the highest amount of total phenolic content in C. nutans extracts (6.09+ 0.45 mg gallic acid equivalent (GAE)/ g DW) and exhibited highest antioxidant activity (73.3+0.82 %) as compared to free and soluble phenolic extracts. The IC50 values for free phenolic, soluble bound and insoluble bound phenolic extracts were 0.69+0.02 mg/mL, 0.64+0.04 and 0.60+0.006 mg/mL, respectively. There were positive correlation between insoluble bound phenolic content of C. nutans extracts with antioxidant radical scavenging capacity (R2 = 0.893). Conclusions: These results indicate that different phenolic acid forms affect the total phenolic content and antioxidant properties. Natural compounds such as phenolics from C. nutans could be a good source of antioxidant.