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.
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.
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.
A new series of some novel pyrazinamide condensed 1,2,3,4-tetrahydropyrimidines was prepared by reacting of N-(3-oxobutanoyl)pyrazine-2-carboxamide with urea/thiourea and appropriate aldehyde in the presence of catalytic amount of laboratory made p-toluenesulfonic acid as an efficient catalyst. Confirmation of the chemical structure of the synthesized compounds (4a-l) was substantiated by TLC, different spectral data IR, (1)H NMR, mass spectra and elemental analysis. The synthesized compounds were evaluated for acetyl and butyl cholinesterase (AChE and BuChE) inhibitor activity. The titled compounds exhibited weak, moderate or high AChE and BuChE inhibitor activity. Especially, compound (4l) showed the best AChE and BuChE inhibitory activity of all the 1,2,3,4-tetrahydropyrimidine derivatives, with an IC50 value of 0.11 μM and 3.4 μM.
Naturally occurring anti-glycation compounds have drawn much interest in recent years as they show potential in reducing or preventing the risk of chronic complications for diabetic patients. In this study, annotation of the genome-transcriptome data from tiger milk mushroom (Lignosus rhinocerus, syn.Lignosus rhinocerotis) to PlantCyc enzymes database identified transcripts that are related to anti-diabetic properties, and these include genes that are involved in carotenoid and abscisic acid biosynthesis as well as genes that code for glyoxalase I, catalase-peroxidases, and superoxide dismutases. The existence of these genes suggests thatL. rhinocerusmay contain bioactive compound(s) with anti-glycation properties that can be exploited for management of diabetic complications. A medium-molecular-weight (MMW) fraction which was obtained from a combination of cold water extraction and Sephadex®G-50 (fine) gel filtration chromatography ofL. rhinocerussclerotia powder was demonstrated to exhibit potent anti-glycation activity. The fraction specifically inhibited the formation of N𝜀-(carboxymethyl)lysine, pentosidine, and other advanced glycation end-product (AGE) structures in a human serum albumin-glucose system, with an IC50value of 0.001 mg/ml, almost 520 times lower than that of the positive control, aminoguanidine hydrochloride (IC50= 0.52 mg/ml). Its ability to suppress protein glycation may be partly associated with its strong superoxide anion radical scavenging activity (10.16 ± 0.12 mmol TE/g). Our results suggest that the MMW fraction ofL. rhinocerusshows potential to be developed into a potent glycation inhibitor for preventing AGE-mediated diabetic complications.
Stenochlaena palustris fronds are popular as a vegetable in Southeast Asia. The objectives of this study were to evaluate the anticholinesterase properties and phytochemical profiles of the young and mature fronds of this plant. Both types of fronds were found to have selective inhibitory effect against butyrylcholinesterase compared with acetylcholinesterase. However, different sets of compounds were responsible for their activity. In young fronds, an antibutyrylcholinesterase effect was observed in the hexane extract, which was comprised of a variety of aliphatic hydrocarbons, fatty acids, and phytosterols. In the mature fronds, inhibitory activity was observed in the methanol extract, which contained a series of kaempferol glycosides. Our results provided novel information concerning the ability of S. palustris to inhibit cholinesterase and its phytochemical profile. Further research to investigate the potential use of this plant against Alzheimer's disease is warranted, however, young and mature fronds should be distinguished due to their phytochemical differences.
This study was designed to determine the effect of osmotic dehydration (OD) process temperature (35-55 °C), sucrose concentration (40-60% w/w) and immersion time (90-210 min) on the water loss (WL), solid gain (SG), DPPH radical scavenging activity, ferric reducing antioxidant power (FRAP) and sensory quality of the dehydrated Terung Asam slices. Response Surface Methodology with Central Composite Design was applied to investigate the influence of these variables on the aforementioned responses. The increase in the levels of these processing parameters increased the WL and SG. The antioxidant activities also increased with sugar concentration, but reduced with immersion time and temperature elevation. About 36-80% of IC50 and 47-72% of FRAP were depleted after osmotic process. The loss of antioxidants was predominantly due to leaching during osmotic treatment rather than hot air drying. Despite the losses of these compounds, osmotic pretreatment was able to improve the sensory quality of the product. The optimum OD process condition was predicted as process temperature 38.1 °C, sucrose concentration 55.6% and osmotic duration 126.3 min.
Synthesis of 2,5-bisarylthiophenes was accomplished by sequential Suzuki cross coupling reaction of 2-bromo-5-chloro thiophenes. Density functional theory (DFT) studies were carried out at the B3LYP/6-31G(d, p) level of theory to compare the geometric parameters of 2,5-bisarylthiophenes with those from X-ray diffraction results. The synthesized compounds are screened for in vitro bacteria scavenging abilities. At the concentration of 50 and 100 μg/mL, compounds 2b, 2c, 2d, 3c, and 3f with IC50-values of 51.4, 52.10, 58.0, 56.2, and 56.5 μg/mL respectively, were found most potent against E. coli. Among all the synthesized compounds 2a, 2d, 3c, and 3e with the least values of IC50 77, 76.26, 79.13 μg/mL respectively showed significant antioxidant activities. Almost all of the compounds showed good antibacterial activity against Escherichia coli, whereas 2-chloro-5-(4-methoxyphenyl) thiophene (2b) was found most active among all synthesized compound with an IC50 value of 51.4 μg/mL. All of the synthesized compounds were screened for nitric oxide scavenging activity as well. Frontier molecular orbitals (FMOs) and molecular electrostatic potentials of the target compounds were also studied theoretically to account for their relative reactivity.
The extraction of phenolics from Citrus hystrix leaf was carried out using supercritical fluid extraction and was optimized using response surface methodology (RSM). The effects of CO2 flow rate, extraction pressure and extraction temperature on yield, total phenolic content and diphenyl-picrylhydrazyl-IC50 were evaluated and compared with ethanol extraction. The extraction pressure was the most significant factor affecting the yield, TPC and DPPH-IC50 of the extracts, followed by CO2 flow rate and the extraction temperature. The optimum conditions of pressure, CO2 flow rate and temperature were at 267 bars, 18 g/min and 50°C, respectively. The yield, TPC and DPPH-IC50 obtained were 5.06%, 116.53 mg GAE/g extract and IC50 of 0.063 mg/ml, respectively. These values were not significantly different (p
The study was aimed to determine the antioxidant and α-glucosidase inhibition activities of
the stem and leaf of five different traditional medicinal plants. The studied plants exhibited
varied antioxidant and α-glucosidase inhibition activities. The antioxidant activities of the
plants were determined through their free radical scavenging capabilities using DPPH assay.
The most potent antioxidant activity was demonstrated by Neptunia oleracea with an IC50 of
35.45 and 29.72 μg/mL for leaf and stem, respectively. For α-glucosidase inhibition activity,
Neptunia oleracea exhibited potential α-glucosidase inhibition activity with IC50 value of
19.09 and 19.74 μg/mL for leaf and stem, respectively. The highest total phenolic content
(TPC) was also marked in Neptunia oleracea leaf and stem with value of 40.88 and 21.21 mg
GAE/g dry weight, respectively. The results also showed that Strobilanthes crispus collected
from two different locations possessed different levels of phenolic content, antioxidant and
α-glucosidase inhibition activities. The study revealed that phenolic compounds could be the
main contributors to the antioxidant and α-glucosidase inhibition activities with R values of 78.9
and 67.4%, respectively. In addition, antioxidant and α-glucosidase were positively correlated
(R = 81.9%). Neptunia oleracea could be suggested as a potential natural source of antioxidant
and antidiabetic compounds that can be used for the prevention or treatment of diabetes.
This study was undertaken to evaluate the antioxidant and acetylcholinesterase inhibition properties of stems and leaves of hexane and methanolic extracts of Pluchea indica. Methanolic extract of leaves showed the highest antioxidant activity (IC50 = 24.45 ± 0.34 µg/ml) and total phenolic contents (573.52 ± 6.2 mg GAE/100 g crude extract), in DPPH radical scavenging and Folin-Ciocalteu assays respectively, however, it failed to inhibit acetylcholinesterase in TLC bioautographic detection. The rest of plant extracts, including methanolic extract of stems, hexane extract of both leaves and stems, were detected to have acetylcholinesterase inhibitory properties. Hexane extract of both leaves and stems exhibited lower or negligible level of antioxidant activity and phenolic contents. Pluchea indica may provide a potential natural source of bioactive compounds, and maybe beneficial to the human health.
Breast cancer is considered as one of the most common cancers all over the world. A huge effort has been made to create a safe and cost effective breast cancer treatment. All of these features exist in the plants sources. In this study, the effect of local vegetable salad, Premna serratifolia (Bebuas) against MCF-7 cells (human breast adenocarcinoma) was determined. The optimum condition to extract breast cancer cytotoxic compound from the plant was investigated and the exact cytotoxic compound was identified as well. To determine the plant cytotoxicity effect against MCF-7 cells, MTT assay was used. Two important parameters in the sonication extraction method which are duration of time and temperature were optimized by carrying out a series of experiments which were designed by Face Centered Central Composite Design (FCCCD). The extraction efficiency of each experiment was determined by measuring the yield of extract and the half maximal inhibitory concentration (IC50) of the extract against MCF-7 cells. The results obtained from the experiments were fitted to the second order polynomial model to generate equation that was used to determine best extraction processing condition. Based on the generated equation, the best sonication processing condition to extract the cytotoxic compound is at 30oC for 67 min. Analysis of variance (ANOVA) showed that the duration of extraction time has great influence (p