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
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.
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.
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.
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.
Oxadiazole derivatives (6-28) having hydrazone linkage, were synthesized through condensation reaction between benzohydrazide 5 with various benzaldehydes. The oxadiazoles derivatives (6-28) were evaluated for their α-glucosidase inhibitory activity. The IC50 values for inhibition activity vary in the range between 2.64 ± 0.05 and 460.14 ± 3.25 μM. The IC50 values were being compared to the standard acarbose (IC50=856.45 ± 5.60 μM) and it was found that compounds 6-9, 12, 13, 16, 18, 20, 22-28 were found to be more active than acarbose, while other compounds showed no activity. Structure-activity relationship (SAR) studies suggest that oxadiazole benzohydrazones (6-28) inhibitory potential is dependent on substitution of the N-benzylidene part. Compound 18 (IC50=2.64 ± 0.05 μM), which has trihydroxy substitution at C-2', C-4', and C-5' on N-benzylidene moiety, recorded the highest inhibition activity that is three-hundred times more active than the standard drug, acarbose (IC50=856.45 ± 5.60 μM). Compound 23 (IC50=34.64 ± 0.35 μM) was found to be the most active among compounds having single hydroxyl substitution. Shifting hydroxyl from C-2' to C-4' (6) and C-3' (7) reduces inhibitory activity significantly. Compounds with chlorine substituent (compounds 16, 28, and 27) showed potent activities but lower as compared to hydroxyl analogs. Substituent like nitro or methyl groups at any position suppresses enzyme inhibition activity. This reveals the important presence of hydroxyl and halo groups to have enzyme inhibitory potential.
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.
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.
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.
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
Acetylcholinesterase (AChE) is usually used as an inhibitive assay for insecticides. A lesserknown
property of AChE is its inhibition by heavy metals. In this work, we evaluate an AChE
from brains of Clarias batrachus (catfish) exposed to wastes from aquaculture industry as an
inhibitive assay for heavy metals. We discovered that the AChE was inhibited completely by
Hg2+, Ag2+, Pb2+, Cu2+, Cd2+, Cr6+ and Zn2+ during initial screening. When tested at various
concentrations, the heavy metals exhibited exponential decay type inhibition curves. The
calculated IC50 (mg/L) for the heavy metals Ag2+, Cu2+, Hg2+, Cr6+ and Cd2+ were 0.088, 0.078,
0.071, 0.87 and 0.913, respectively. The IC50 for these heavy metals are comparable, and some
are lower than the IC50 values from the cholinesterases from previously studied fish. The assay
can be carried out in less than 30 minutes at ambient temperature.
Acetylcholinesterase (AChE) is usually used as an inhibitive assay for insecticides. A lesser
known property of AChE is its inhibition by heavy metals. In this work we evaluate an AChE
from brains of striped snakehead (Channa striatus) wastes from aquaculture industry as an
inhibitive assay for heavy metals. We discovered that the AChE was inhibited almost completely
by Hg2+, Ag2+ and Cu2+ during an initial screening. When tested at various concentrations, the
heavy metals exhibited exponential decay type inhibition curves. The calculated IC50 for the
heavy metals Hg2+, Ag2+, Pb2+, Cu2+ and Cr6+ were 0.08432, 0.1008, 0.1255, 0.0871, and 0.1771,
respectively. The IC50 for these heavy metals are comparable and some are lower than the IC50
values from the cholinesterases from previously studied fish. The assay can be carried out in less
than 30 minutes at ambient temperature.
Ganoderma lucidum has been recognized as a precious fungus in both Chinese and Japanese traditional medicine for
centuries. It contains many bioactive ingredients such as triterpenoids and polysaccharides. The present study used
supercritical carbon dioxide (SC-CO2
) fractionation to fractionate Ganoderma lucidum extract into four fractions (R,
F1, F2, & F3) and evaluate the correlation between the content of functional components and their antioxidant ability.
Relatively high concentrations of the three types of bioactive constituents were simultaneously partitioned into different
fractionation collecting vessels. The free radical scavenging ability was greatest in F1. The IC50 of DPPH scavenging ability
was 0.90 mg/mL and that of ABTS radicals scavenging activity was 0.45 mg/mL. The correlation analysis of antioxidant
ability with total triterpenoids and total polyphenols showed a positive relationship. In conclusion, this study showed
that fractionation of Ganoderma lucidum extract using SC-CO2 fractionation technology was able to effectively partition
its bioactive components including triterpenoids, polysaccharides and phenolic compounds and also to increase the
antioxidant activities of the fractions.
Metaldehyde is used widely in Malaysia for the control of molluscs. This communication reports the cytotoxic effects of this chemical on cultured cells as assessed by cell morphology and the DNA synthesising capability as well as its transport into cells. After 15 days of exposure with 20.0 ppm of the compound, the DNA synthesising capability was shown to be unaffected. The IC50 for Vero cells was 276.0 ppm. Transport of thymidine across cells was found to be not significantly affected even at high metaldehyde concentrations (up to 320.0 ppm) suggesting integrity of cells were not significantly affected. The present cellular studies have therefore shown that the cytotoxic effects of this chemical is rather low.
Metaldehida digunakan dengan meluas di Malaysia untuk mengawal perosak moluska. Kesan sitotoksik bahan kimia ini di peringkat sel dari segi ciri-ciri perubahan moifologi dan keupayaan mensintesis DNA serta kajian awal kesannya terhadap proses kemasukan ke dalam sel dilaporkan di sini. Keupayaan mensintesis DNA didapati tidak terjejas secara signifikan selepas diberikan 20.0 ppm metaldehida secara berterusan selama 15 hari. Nilai IC50 bagi sel Vero adalah 276.0 ppm. Kemasukan timidina ke dalam sel tidak terjejas secara signifikan apabila sel diperlakukan dengan metaldehida, walaupun pada kepekatan yang agak tinggi iaitu sehingga 320.0 ppm. Kajian telah menunjukkan bahawa kesan sitotoksik oleh metaldehida adalah rendah.
We have synthesized new series of bisindole analogs (1-27), characterized by 1HNMR and HR-EI-MS and evaluated for their anti-leishmanial potential. All compounds showed outstanding inhibitory potential with IC50 values ranging from 0.7 ± 0.01 to 13.30 ± 0.50 µM respectively when compared with standard pentamidine with IC50 value of 7.20 ± 0.20 µM. All analogs showed greater potential than standard except 10, 19 and 23 when compared with standard. Structure activity relationship has been also established for all compounds. Molecular docking studies were carried out to understand the binding interaction of active molecules.
New triazinoindole bearing thiazole/oxazole analogues (1-21) were synthesized and characterized through spectroscopic techniques such as HREI-MS, 1H and 13C NMR. The configuration of compound 2i and 2k was confirmed through NOESY. All analogues were evaluated against α-amylase inhibitory potential. Among the synthesized analogues, compound 1h, 1i, 1j, 2a and 2f having IC50 values 1.80 ± 0.20, 1.90 ± 0.30, 1.2 ± 0.30, 1.2 ± 0.01 and 1.30 ± 0.20 μM respectively, showed excellent α-amylase inhibitory potential when compared with acarbose as standard (IC50 = 0.91 ± 0.20 µM). All other analogues showed good to moderate inhibitory potential. Structural activity relationship (SAR) has been established and binding interactions were confirmed through docking studies.
The role of aldose reductase (ALR2) in diabetes mellitus is well-established. Our interest in finding ALR2 inhibitors led us to explore the inhibitory potential of new thiosemicarbazones. In this study, we have synthesized adamantyl-thiosemicarbazones and screened them as aldehyde reductase (ALR1) and aldose reductase (ALR2) inhibitors. The compounds bearing phenyl 3a, 2-methylphenyl 3g and 2,6-dimethylphenyl 3m have been identified as most potent ALR2 inhibitors with IC50 values of 3.99 ± 0.38, 3.55 ± 0.26 and 1.37 ± 0.92 µM, respectively, compared with sorbinil (IC50 = 3.14 ± 0.02 μM). The compounds 3a, 3g, and 3m also inhibit ALR1 with IC50 value of 7.75 ± 0.28, 7.26 ± 0.39 and 7.04 ± 2.23 µM, respectively. Molecular docking was also performed for putative binding of potent inhibitors with target enzyme ALR2. The most potent 2,6-dimethylphenyl bearing thiosemicarbazone 3m (IC50 = 1.37 ± 0.92 µM for ALR2) and other two compound 3a and 3g could potentially lead for the development of new therapeutic agents.
A methanol extract of the stem bark of the Malayan Alstonia penangiana provided seven new bisindole alkaloids, comprising six macroline-sarpagine alkaloids (angustilongines E-K, 1-6) and one macroline-pleiocarpamine bisindole alkaloid (angustilongine L, 7). Analysis of the spectroscopic data (NMR and MS) of these compounds led to the proposed structures of these alkaloids. The macroline-sarpagine alkaloids (1-6) showed in vitro growth inhibitory activity against a panel of human cancer cell lines, inclusive of KB, vincristine-resistant KB, PC-3, LNCaP, MCF7, MDA-MB-231, HT-29, HCT 116, and A549 cells (IC50 values: 0.02-9.0 μM).
A series of compounds consisting of 25 novel oxadiazole-benzohydrazone hybrids (6-30) were synthesized through a five-step reaction sequence and evaluated for their β-glucuronidase inhibitory potential. The IC50 values of compounds 6-30 were found to be in the range of 7.14-44.16μM. Compounds 6, 7, 8, 9, 11, 13, 18, and 25 were found to be more potent than d-saccharic acid 1,4-lactone (48.4±1.25μM). These compounds were further subjected for molecular docking studies to confirm the binding mode towards human β-d-glucuronidase active site. Docking study for compound 13 (IC50=7.14±0.30μM) revealed that it adopts a binding mode that fits within the entire pocket of the binding site of β-d-glucuronidase. Compound 13 has the maximum number of hydrogens bonded to the residues of the active site as compared to the other compounds, that is, the ortho-hydroxyl group forms hydrogen bond with carboxyl side chain of Asp207 (2.1Å) and with hydroxyl group of Tyr508 (2.6Å). The other hydroxyl group forms hydrogen bond with His385 side chain (2.8Å), side chain carboxyl oxygen of Glu540 (2.2Å) and Asn450 side-chain's carboxamide NH (2.1Å).