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Inhibition and kinetic studies of lignin degrading enzymes of Ganoderma boninense by naturally occurring phenolic compounds

Surendran A, Siddiqui Y, Saud HM, Ali NS, Manickam S

J Appl Microbiol, 2018 Sep;125(3):876-887.
PMID: 29786938 DOI: 10.1111/jam.13922

AIM: Lignolytic (lignin degrading) enzyme, from oil palm pathogen Ganoderma boninense Pat. (Syn G. orbiforme (Ryvarden)), is involved in the detoxification and the degradation of lignin in the oil palm and is the rate-limiting step in the infection process of this fungus. Active inhibition of lignin-degrading enzymes secreted by G. boninense by various naturally occurring phenolic compounds and estimation of efficiency on pathogen suppression was aimed at.
METHODS AND RESULTS: In our work, 10 naturally occurring phenolic compounds were evaluated for their inhibitory potential towards the lignolytic enzymes of G. boninense. Additionally, the lignin-degrading enzymes were characterized. Most of the peholic compounds exhibited an uncompetitive inhibition towards the lignin-degrading enzymes. Benzoic acid was the superior inhibitor to the production of lignin-degrading enzymes, when compared between the 10 phenolic compounds. The inhibitory potential of the phenolic compounds towards the lignin-degrading enzymes are higher than that of the conventional metal ion inhibitor. The lignin-degrading enzymes were stable in a wide range of pH but were sensitive to higher temperature.
CONCLUSION: The study demonstrated the inhibitor potential of 10 naturally occurring phenolic compounds towards the lignin-degrading enzymes of G. boninense with different efficacies.
SIGNIFICANCE AND IMPACT OF THE STUDY: The study has shed a light towards a new management strategy to control basal stem rot disease in oil palm. It serves as a replacement for the existing chemical control.

Matched MeSH terms: Phenols/pharmacology*
Fulltext Optimization of Pluchea indica (L.) leaf extract using ultrasound-assisted extraction and its cytotoxicity on the HT-29 colorectal cancer cell line

Aishah Baharuddin S, Nadiah Abd Karim Shah N, Saiful Yazan L, Abd Rashed A, Kadota K, Al-Awaadh AM, et al.

Ultrason Sonochem, 2023 Dec;101:106702.
PMID: 38041881 DOI: 10.1016/j.ultsonch.2023.106702

Colorectal cancer (CRC) is the most common malignancy and the third primary cause of cancer-related mortalities caused by unhealthy diet, hectic lifestyle, and genetic damage. People aged ≥ 50 are more at risk for CRC. Nowadays, bioactive compounds from plants have been widely studied in preventing CRC because of their anticancer and antioxidant properties. Herein, ultrasound-assisted extraction (UAE) was used to extract the bioactive compounds of Pluchea indica (L.) leaves. The resultant total phenolic content (TPC) and total flavonoid content (TFC) of P. indica (L.) leaves were analyzed using a response surface methodology (RSM). The central composite design was implemented to evaluate the amplitude (10 %-70 %) and treatment time (2-10 min) on both responses, i.e., TPC and TFC of P. indica (L.) leaves. The optimum UAE conditions were observed 40 % amplitude and 6 min of treatment, where the TPC and TFC were 3.26 ± 0.00 mg GAE/g d.w. and 67.58 ± 1.46 mg QE/g d.w., respectively. The optimum P. indica (L.) leaf extract was then screened for its cytotoxicity on the HT-29 colorectal cancer cell line. This extract had strong cytotoxicity with a half-maximal inhibitory concentration value (IC50) of 12 µg/mL. The phytochemical screening of bioactive compounds revealed that the optimal P. indica (L.) leaf extract contains flavonoids, namely, kaempferol 3-[2''',3''',5'''-triacetyl]-alpha-L-arabinofuranosyl-(1->6)-glucoside, myricetin 3-glucoside-7-galactoside, quercetin 3-(3''-sulfatoglucoside), and kaempferol 7,4'-dimethyl ether 3-O-sulfate, which could be good sources for promising anticancer agents. This study employs the RSM approach to utilize UAE for bioactive compounds extraction of P. indica (L.) leaves, identified the specific compounds present in the optimized extract and revealed its potential in preventing CRC.

Matched MeSH terms: Phenols/pharmacology
Fulltext Effect of Different Extraction Methods on the Total Phenolics of Sugar Cane Products

Azlan A, Sultana S, Mahmod II

Molecules, 2023 May 28;28(11).
PMID: 37298880 DOI: 10.3390/molecules28114403

The health benefits of sugar cane products are attributed to certain antioxidant compounds in plant materials. The presence of antioxidants in plant materials depends on the extraction method in terms of yield and the number of phenolic compounds identified. This study was carried out to evaluate the performance of the three extraction methods, which were selected from previous studies to show the effect of the extraction method on the content of antioxidant compounds in different types of sugar. This study also evaluates the potential of different sugar extracts in anti-diabetic activity based on in vitro assays (α-glucosidase and α-amylase). The results showed that sugar cane extracted with acidified ethanol (1.6 M HCl in 60% ethanol) was the best condition to extract a high yield of phenolic acids compared to other methods. Among the three types of sugar, less refined sugar (LRS) showed the highest yield of phenolic compounds, 57.72 µg/g, compared to brown sugar (BS) and refined sugar (RS) sugar, which were at 42.19 µg/g and 22.06 µg/g, respectively. Whereas, among the sugar cane derivatives, LRS showed minor and BS moderate inhibition towards α-amylase and α-glucosidase activity compared to white sugar (RS). Thus, it is suggested that sugar cane extracted with acidified ethanol (1.6 M HCl in 60% ethanol) is the optimum experimental condition for antioxidant content determination and provides a basis for further exploitation of the health-beneficial resources of the sugarcane products.

Matched MeSH terms: Phenols/pharmacology
Phenolic constituents and anticancer properties of Morus alba (white mulberry) leaves

Chan EWC, Wong SK, Tangah J, Inoue T, Chan HT

J Integr Med, 2020 May;18(3):189-195.
PMID: 32115383 DOI: 10.1016/j.joim.2020.02.006

Flavonoids are by far the most dominant class of phenolic compounds isolated from Morus alba leaves (MAL). Other classes of compounds are benzofurans, phenolic acids, alkaloids, coumarins, chalcones and stilbenes. Major flavonoids are kuwanons, moracinflavans, moragrols and morkotins. Other major compounds include moracins (benzofurans), caffeoylquinic acids (phenolic acids) and morachalcones (chalcones). Research on the anticancer properties of MAL entailed in vitro and in vivo cytotoxicity of extracts or isolated compounds. Flavonoids, benzofurans, chalcones and alkaloids are classes of compounds from MAL that have been found to be cytotoxic towards human cancer cell lines. Further studies on the phytochemistry and anticancer of MAL are suggested. Sources of information were PubMed, PubMed Central, ScienceDirect, Google, Google Scholar, J-Stage, PubChem and China National Knowledge Infrastructure.

Matched MeSH terms: Phenols/pharmacology*
Studies on the antioxidant properties of Tualang honey of Malaysia

Mohamed M, Sirajudeen K, Swamy M, Yaacob NS, Sulaiman SA

Afr J Tradit Complement Altern Med, 2009 Oct 15;7(1):59-63.
PMID: 21304614

Honey has been used since ancient times for its nutritional as well as curative properties. Tualang honey is collected from wild honey bees' hives on Tualang trees found in the Malaysian rain forest. It has been used traditionally for the treatment of various diseases, where its therapeutic value has partly been related to its antioxidant properties. This study therefore assessed the colour intensity, total phenolic content, antioxidant activity and antiradical activity of gamma irradiated Tualang Honey. The colour intensity at ABS₄₅₀ was 489.5 ± 1.7 mAU, total phenolic content was 251.7 ± 7.9 mg (gallic acid) /Kg honey, total antioxidant activity by FRAP assay was 322.1 ± 9.7 (µM Fe(II)) and the antiradical activity by DPPH assay was 41.30 ± 0.78 (% inhibition). The data confirms that the antioxidant properties of gamma irradiated Tualang honey are similar to other types of honeys reported in the literature.

Matched MeSH terms: Phenols/pharmacology*
Antioxidant capacity and phenolic composition of fermented Centella asiatica herbal teas

Ariffin F, Heong Chew S, Bhupinder K, Karim AA, Huda N

J Sci Food Agric, 2011 Dec;91(15):2731-9.
PMID: 21987075 DOI: 10.1002/jsfa.4454

C. asiatica was exposed to various fermentations: no fermentation (0 min), partial fermentation (120 min) and full fermentation (24 h). Total phenolic content (TPC) and ferric-reducing antioxidant power (FRAP) of C. asiatica infusions were studied as a function of water temperature (60, 80 or 100 °C), the brewing stage (one, two or three) and the brewing time (1, 3, 5, 10, 15 or 20 min). The optimum brewing procedure was adopted to study the antioxidant properties and phenolic compounds in C. asiatica infusions.

Matched MeSH terms: Phenols/pharmacology*
Fulltext Antioxidant, total phenolic content and cytotoxicity evaluation of selected Malaysian plants

Qader SW, Abdulla MA, Chua LS, Najim N, Zain MM, Hamdan S

Molecules, 2011 Apr 21;16(4):3433-43.
PMID: 21512451 DOI: 10.3390/molecules16043433

Aqueous and ethanol extracts of different traditional Malaysian plants (Polygonum minus, Andrographis paniculata, Curcuma xanthorrhiza, Momordica charantia and Strobilanthes crispus) were evaluated for their antioxidant properties, total phenolic content and cytotoxic activity. Antioxidant activity was evaluated by using 1,1-diphenyl-1-picrylhydrazyl (DPPH) and ferric reducing antioxidant power (FRAP) assays. The results showed that ethanol extracts contain high antioxidant activities compared to aqueous extracts. The findings exhibited a strong correlation between antioxidant activity and the total phenol contents. In addition, all the plant extracts showed non-toxic effects against a normal human lung fibroblast cell line (Hs888Lu). Although traditionally aqueous extracts are used, we determined that ethanol extracts usually achieved better activity in the assays.

Matched MeSH terms: Phenols/pharmacology*
Fulltext Characterization of bioactive compounds produced by endophytic fungi isolated from Gynura procumbens (Sambung Nyawa)

Jamal HAA, Husaini A, Sing NN, Roslan HA, Zulkharnain A, Akinkunmi WA

Braz J Microbiol, 2022 Dec;53(4):1857-1870.
PMID: 36109458 DOI: 10.1007/s42770-022-00827-w

This research evaluates the bioactivity of twelve endophytic fungi successfully isolated and characterised from Gynura procumbens. The fungal extracts displayed inhibitory activity against Staphylococcus aureus, Pseudomonas aeruginosa, Methicillin-resistant Staphylococcus aureus (MRSA), Escherichia coli and Salmonella typhi with the MIC and MBC of 5000 µg/mL. High antioxidant activity using DPPH free radical scavenging assay with inhibition of 86.6% and IC50 value of 104.25 ± 18.51 µg/mL were exhibited by ethyl acetate extract of Macrophomina phaseolina SN6. In contrast, the highest scavenging activity percentage of methanolic extract was exhibited by Mycoleptodiscus indicus SN4 (50.0%). Besides that, the highest ferric reducing antioxidant power (FRAP) value of ethyl acetate and methanolic extract was recorded from M. phaseolina SN6 (239.9 mg Fe (II)/g) and M. indicus SN4 (44.7 mg Fe (II)/g), respectively. Total phenolic content (TPC) and total flavonoid content (TFC) of ethyl acetate and methanolic fungal extracts were determined using Folin-Ciocalteu and aluminium chloride, respectively. The highest TPC for ethyl acetate and methanolic extracts were exhibited by Colletotrichum gloeosporioides SN11 (87.0 mg GAE/g) and M. indicus SN4 (35.0 mg GAE/g), whereas the highest TFC of ethyl acetate and methanolic extracts were showed by M. phaseolina SN6 (122.8 mg QCE/g) and M. indicus SN4 (60.4 mg QCE/g), respectively. Bioactive metabolites of isoelemicin (50.8%), terpinen-4-ol (21.5%), eucalyptol (24.3%), oleic acid (19.8%) and β-pinene (10.9%) were detected. Owing to the higher content of phytochemicals represented in the ethyl acetate extract of M. phaseolina, SN6 is therefore identified to be a superior candidate in exhibiting strong antioxidant and antimicrobial properties be fit for further pharmaceutical studies.

Matched MeSH terms: Phenols/pharmacology
Fulltext Conjugating uncoupler compounds with hydrophobic hydrocarbon chains to achieve adipose tissue selective drug accumulation

Ng MY, Song ZJ, Venkatesan G, Rodriguez-Cuenca S, West JA, Yang S, et al.

Sci Rep, 2024 Feb 28;14(1):4932.
PMID: 38418847 DOI: 10.1038/s41598-024-54466-2

One potential approach for treating obesity is to increase energy expenditure in brown and white adipose tissue. Here we aimed to achieve this outcome by targeting mitochondrial uncoupler compounds selectively to adipose tissue, thus avoiding side effects from uncoupling in other tissues. Selective drug accumulation in adipose tissue has been observed with many lipophilic compounds and dyes. Hence, we explored the feasibility of conjugating uncoupler compounds with a lipophilic C8-hydrocarbon chain via an ether bond. We found that substituting the trifluoromethoxy group in the uncoupler FCCP with a C8-hydrocarbon chain resulted in potent uncoupling activity. Nonetheless, the compound did not elicit therapeutic effects in mice, likely as a consequence of metabolic instability resulting from rapid ether bond cleavage. A lipophilic analog of the uncoupler compound 2,6-dinitrophenol, in which a C8-hydrocarbon chain was conjugated via an ether bond in the para-position (2,6-dinitro-4-(octyloxy)phenol), exhibited increased uncoupling activity compared to the parent compound. However, in vivo pharmacokinetics studies suggested that 2,6-dinitro-4-(octyloxy)phenol was also metabolically unstable. In conclusion, conjugation of a hydrophobic hydrocarbon chain to uncoupler compounds resulted in sustained or improved uncoupling activity. However, an ether bond linkage led to metabolic instability, indicating the need to conjugate lipophilic groups via other chemical bonds.

Matched MeSH terms: Phenols/pharmacology
Effects of heavy metals on bacterial growth parameters in degradation of phenol by an Antarctic bacterial consortium

Tengku-Mazuki TA, Darham S, Convey P, Shaharuddin NA, Zulkharnain A, Khalil KA, et al.

Braz J Microbiol, 2024 Mar;55(1):629-637.
PMID: 38110706 DOI: 10.1007/s42770-023-01215-8

Antarctica has often been perceived as a pristine continent until the recent few decades as pollutants have been observed accruing in the Antarctic environment. Irresponsible human activities such as accidental oil spills, waste incineration and sewage disposal are among the primary anthropogenic sources of heavy metal contaminants in Antarctica. Natural sources including animal excrement, volcanism and geological weathering also contribute to the increase of heavy metals in the ecosystem. A microbial growth model is presented for the growth of a bacterial cell consortium used in the biodegradation of phenol in media containing different metal ions, namely arsenic (As), cadmium (Cd), aluminium (Al), nickel (Ni), silver (Ag), lead (Pb) and cobalt (Co). Bacterial growth was inhibited by these ions in the rank order of Al

Matched MeSH terms: Phenols/pharmacology
Fulltext Subcritical Water Technology for Extraction of Phenolic Compounds from Chlorella sp. Microalgae and Assessment on Its Antioxidant Activity

Zakaria SM, Kamal SMM, Harun MR, Omar R, Siajam SI

Molecules, 2017 Jul 03;22(7).
PMID: 28671617 DOI: 10.3390/molecules22071105

Chlorella sp. microalgae is a potential source of antioxidants and natural bioactive compounds used in the food and pharmaceutical industries. In this study, a subcritical water (SW) technology was applied to determine the phenolic content and antioxidant activity of Chlorella sp. This study focused on maximizing the recovery of Chlorella sp. phenolic content and antioxidant activity measured by 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay as a function of extraction temperature (100-250 °C), time (5-20 min) and microalgae concentration (5-20 wt. %) using response surface methodology. The optimal operating conditions for the extraction process were found to be 5 min at 163 °C with 20 wt. % microalgae concentration, which resulted in products with 58.73 mg gallic acid equivalent (GAE)/g phenolic content and 68.5% inhibition of the DPPH radical. Under optimized conditions, the experimental values were in close agreement with values predicted by the model. The phenolic content was highly correlated (R² = 0.935) with the antioxidant capacity. Results indicated that extraction by SW technology was effective and that Chlorella sp. could be a useful source of natural antioxidants.

Matched MeSH terms: Phenols/pharmacology
Inhibition and kinetic studies of cellulose- and hemicellulose-degrading enzymes of Ganoderma boninense by naturally occurring phenolic compounds

Surendran A, Siddiqui Y, Ali NS, Manickam S

J Appl Microbiol, 2018 Jun;124(6):1544-1555.
PMID: 29405525 DOI: 10.1111/jam.13717

AIM: Ganoderma sp, the causal pathogen of the basal stem rot (BSR) disease of oil palm, secretes extracellular hydrolytic enzymes. These play an important role in the pathogenesis of BSR by nourishing the pathogen through the digestion of cellulose and hemicellulose of the host tissue. Active suppression of hydrolytic enzymes secreted by Ganoderma boninense by various naturally occurring phenolic compounds and estimation of their efficacy on pathogen suppression is focused in this study.
METHODS AND RESULTS: Ten naturally occurring phenolic compounds were assessed for their inhibitory effect on the hydrolytic enzymes of G. boninense. The enzyme kinetics (Vmax and Km ) and the stability of the hydrolytic enzymes were also characterized. The selected compounds had shown inhibitory effect at various concentrations. Two types of inhibitions namely uncompetitive and noncompetitive were observed in the presence of phenolic compounds. Among all the phenolic compounds tested, benzoic acid was the most effective compound suppressive to the growth and production of hydrolytic enzymes secreted by G. boninense. The phenolic compounds as inhibitory agents can be a better replacement for the metal ions which are known as conventional inhibitors till date. The three hydrolytic enzymes were stable in a wide range of pH and temperature.
CONCLUSION: These findings highlight the efficacy of the applications of phenolic compounds to control Ganoderma.
SIGNIFICANCE AND IMPACT OF THE STUDY: The study has proved a replacement for chemical controls of G. boninense with naturally occurring phenolic compounds.

Matched MeSH terms: Phenols/pharmacology*
Fulltext Vermicompost Supplementation Improves the Stability of Bioactive Anthocyanin and Phenolic Compounds in Clinacanthus nutans Lindau

Yusof Z, Ramasamy S, Mahmood NZ, Yaacob JS

Molecules, 2018 Jun 04;23(6).
PMID: 29867000 DOI: 10.3390/molecules23061345

This project studied the effect of vermicompost application on the composition of bioactive anthocyanin and phenolic compounds, and the antioxidant activity of Clinacanthus nutans. The correlation between the bioactive constituents and antioxidant capacity was also evaluated. In this project, a field study was conducted using a randomized complete block design (RCBD) with four treatment groups, including control plants (CC), plants supplied with chemical fertilizer (CF), plants supplied with vermicompost (VC), and plants supplied with mixed fertilizer (MF). The leaves of C. nutans from all treatment groups were harvested, subjected to solvent extraction, and used for quantification of total anthocyanin content (TAC), total phenolic content (TPC), and total flavonoid content (TFC). The initial antioxidant activity of the extracts was evaluated using 2,2-Diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assays, as well as after two and four weeks of storage at -20 °C and 4 °C. Data analysis showed that CC plants contained the highest TAC (2180.14 ± 338.43 µg/g dry weight) and TFC (276.25 ± 3.09 mg QE/g dry weight). On the other hand, CF plants showed the highest TPC (181.53 ± 35.58 mg GAE/g dry weight). Moreover, we found that CC plants had the highest antioxidant potential against DPPH radicals whereas MF plants showed the lowest antioxidant potential. After four weeks of extract storage at -20 °C and 4 °C, the TPC, TFC, TAC, and antioxidant potential of the extracts decreased. Extracts from VC showed the lowest percentage of total phenolic and total flavonoid loss after extract storage at -20 °C and 4 °C compared with other plant extracts. At this juncture, it could be deduced that the application of vermicompost had little effect on the expression of phenolics, flavonoids, or anthocyanin in C. nutans. However, the extract from plants treated with vermicompost (VC and MF) showed better stability compared with CC and CF after extract storage at different temperatures.

Matched MeSH terms: Phenols/pharmacology
Anticancer Potential of Syzygium Species: a Review

Chua LK, Lim CL, Ling APK, Chye SM, Koh RY

Plant Foods Hum Nutr, 2019 Mar;74(1):18-27.
PMID: 30535971 DOI: 10.1007/s11130-018-0704-z

Cancer is a preventable and treatable disease, however, the incidence rates are on the rise. Classical treatment modalities for cancer include surgery, radiotherapy and chemotherapy. However, these are associated with detrimental side effects such as nausea and emesis. Therefore, researchers currently vest interest in complementary and alternative medicines for cancer treatment and prevention. Plants such as Syzygium sp. are a common basis of complementary medicines due to its abundance of bioactive phytochemicals. Numerous natural compounds derived from Syzygium sp., such as phenolics, oleanolic acids, and betulinic acids, and dimethyl cardamonins, were reported to have anticancer effects. Many possess the ability to inhibit cell proliferation and induce apoptosis. In this review, we discuss the vast potential Syzygium sp. harbours as a source of anticancer natural compounds due to its abundance, easy acceptability, affordability and safety for regular consumption.

Matched MeSH terms: Phenols/pharmacology
Fulltext Phenolic Compounds as Promising Drug Candidates in Tuberculosis Therapy

Mazlun MH, Sabran SF, Mohamed M, Abu Bakar MF, Abdullah Z

Molecules, 2019 Jul 04;24(13).
PMID: 31277371 DOI: 10.3390/molecules24132449

Tuberculosis (TB), caused by Mycobacterium tuberculosis (MTB) remains one of the deadliest, infectious diseases worldwide. The detrimental effects caused by the existing anti-TB drugs to TB patients and the emergence of resistance strains of M. tuberculosis has driven efforts from natural products researchers around the globe in discovering novel anti-TB drugs that are more efficacious and with less side effects. There were eleven main review publications that focused on natural products with anti-TB potentials. However, none of them specifically emphasized antimycobacterial phenolic compounds. Thus, the current review's main objective is to highlight and summarize phenolic compounds found active against mycobacteria from 2000 to 2017. Based on the past studies in the electronic databases, the present review also focuses on several test organisms used in TB researches and their different distinct properties, a few types of in vitro TB bioassay and comparison between their strengths and drawbacks, different methods of extraction, fractionation and isolation, ways of characterizing and identifying isolated compounds and the mechanism of actions of anti-TB phenolic compounds as reported in the literature.

Matched MeSH terms: Phenols/pharmacology
Identification of Novel Sesamol Dimers with Unusual Methylenedioxy Ring-Opening Skeleton and Evaluation of Their Antioxidant and Cytotoxic Activities

Murthy S, Hazli UHAM, Kong KW, Mai CW, Leong CO, Rahman NA, et al.

Curr Org Synth, 2019;16(8):1166-1173.
PMID: 31984923 DOI: 10.2174/1570179416666191003095253

BACKGROUND: Sesamol is a widely used antioxidant for the food and pharmaceutical industries. The oxidation products of this compound may be accumulated in foods or ingested. Little is known about its effect on human health.
OBJECTIVE: It is of great interest to identify the oxidation products of sesamol that may be beneficial to humans. This study was undertaken to identify the oxidation products of sesamol and investigate their antioxidant and cytotoxic activities.
MATERIALS AND METHODS: Using the ferricyanide oxidation approach, four oxidation products of sesamol (2, 3, 20 & 21) have been identified. Structural elucidation of these compounds was established on the basis of their detailed NMR spectroscopic analysis, mass spectrometry and x-ray crystallography. Additionally, a formation mechanism of compound 20 was proposed based on high-resolution mass spectrometry-fragmentation method. The antioxidant activities of these compounds were determined by the DPPH, FRAP, and ABTS assays. The in vitro antiproliferative activity of these compounds was evaluated against a panel of human cancer cell lines as well as non-cancerous cells.
RESULTS: Two oxidation products of sesamol were found to contain an unusual methylenedioxy ring-opening skeleton, as evidenced by spectroscopic and x-ray crystallographic data. Among all compounds, 20 displayed impressive antiproliferative activities against a panel of human cancer cell lines yet remained non-toxic to noncancerous cells. The antioxidant activities of compound 20 are significantly weaker than sesamol as determined by the DPPH, FRAP, and ABTS assays.
CONCLUSION: The oxidation products of sesamol could be a valuable source of bioactive molecules. Compound 20 may be used as a potential lead molecule for cancer studies.

Matched MeSH terms: Phenols/pharmacology
Fulltext Recent Advances in Nanoencapsulation Systems Using PLGA of Bioactive Phenolics for Protection against Chronic Diseases

Abdul Rahim R, Jayusman PA, Muhammad N, Ahmad F, Mokhtar N, Naina Mohamed I, et al.

Int J Environ Res Public Health, 2019 Dec 06;16(24).
PMID: 31817699 DOI: 10.3390/ijerph16244962

Plant-derived polyphenolic compounds have gained widespread recognition as remarkable nutraceuticals for the prevention and treatment of various disorders, such as cardiovascular, neurodegenerative, diabetes, osteoporosis, and neoplastic diseases. Evidence from the epidemiological studies has suggested the association between long-term consumption of diets rich in polyphenols and protection against chronic diseases. Nevertheless, the applications of these phytochemicals are limited due to its low solubility, low bioavailability, instability, and degradability by in vivo and in vitro conditions. Therefore, in recent years, newer approaches have been attempted to solve the restrictions related to their delivery system. Nanoencapsulation of phenolic compounds with biopolymeric nanoparticles could be a promising strategy for protection and effective delivery of phenolics. Poly(lactic-co-glycolic acid) (PLGA) is one of the most successfully developed biodegradable polymers that has attracted considerable attention due to its attractive properties. In this review, our main goal is to cover the relevant recent studies that explore the pharmaceutical significance and therapeutic superiority of the advance delivery systems of phenolic compounds using PLGA-based nanoparticles. A summary of the recent studies implementing encapsulation techniques applied to polyphenolic compounds from plants confirmed that nanoencapsulation with PLGA nanoparticles is a promising approach to potentialize their therapeutic activity.

Matched MeSH terms: Phenols/pharmacology*
Fulltext New insights of phenolic compounds from optimized fruit extract of Ficus auriculata

Shahinuzzaman M, Akhtar P, Amin N, Ahmed Y, Anuar FH, Misran H, et al.

Sci Rep, 2021 Jun 14;11(1):12503.
PMID: 34127747 DOI: 10.1038/s41598-021-91913-w

In this study, the extraction conditions extracted maximize amounts of phenolic and bioactive compounds from the fruit extract of Ficus auriculata by using optimized response surface methodology. The antioxidant capacity was evaluated through the assay of radical scavenging ability on DPPH and ABTS as well as reducing power assays on total phenolic content (TPC). For the extraction purpose, the ultrasonic assisted extraction technique was employed. A second-order polynomial model satisfactorily fitted to the experimental findings concerning antioxidant activity (R2 = 0.968, P

Matched MeSH terms: Phenols/pharmacology
Fulltext Phenolic content, antioxidant effect and cytotoxic activity of Leea indica leaves

Reddy NS, Navanesan S, Sinniah SK, Wahab NA, Sim KS

BMC Complement Altern Med, 2012 Aug 17;12:128.
PMID: 22898370 DOI: 10.1186/1472-6882-12-128

BACKGROUND: The leaves of Leea indica (Vitaceae), commonly known as 'Huo Tong Shu' in Malaysia, have been traditionally used as natural remedy in folk medicine by the locals. The current study reports the outcome of antioxidant and cytotoxic investigation of L. indica leaves. To the best of our knowledge, this is the first report of L. indica leaf crude ethanol and its fractionated extracts (hexane, ethyl acetate and water) for evaluation of total phenolic content, antioxidant effect and cytotoxic activity against colon cancer cell lines.
METHODS: In the present study, L. indica leaf crude ethanol and its fractionated extracts (hexane, ethyl acetate and water) were firstly prepared prior to phenolic content, antioxidant effect and cytotoxic activity assessment. Folin-Ciocalteau's method was used for the measurement of total phenolic content of the extracts. The antioxidant activity was measured by employing three different established testing systems, such as scavenging activity on DPPH (1,1-diphenyl-2-picrylhydrazyl) radicals, reducing power assay and SOD (superoxide dismutase) activity assay. The cytotoxic activity of the extracts were evaluated against three colon cancer cell lines with varying molecular characteristics (HT-29, HCT-15 and HCT-116) by MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] assay.
RESULTS: The total phenolic content and antioxidant capabilities differed significantly among the L. indica leaf extracts. A strong correlation between total phenolic content and antioxidant properties was found, indicating that phenolic compounds are the major contributor to the antioxidant properties of these extracts. Among the crude ethanol and its fractionated extracts, fractionated water extract showed significantly the highest total phenolic content and strongest antioxidant effect in all the antioxidant testing systems employed in this study. All the four extracts exert no damage to the selected colon cancer cells.
CONCLUSIONS: The data obtained in these testing systems clearly establish the antioxidant potency of the fractionated water extract of L. indica leaves. Additional studies should be carried out to isolate and identify the bioactive compounds in the fractionated water extract, in order to provide more convincing evidence.

Matched MeSH terms: Phenols/pharmacology*
Xanthorrhizol induced DNA fragmentation in HepG2 cells involving Bcl-2 family proteins

Tee TT, Cheah YH, Meenakshii N, Mohd Sharom MY, Azimahtol Hawariah LP

Biochem Biophys Res Commun, 2012 Apr 20;420(4):834-8.
PMID: 22465013 DOI: 10.1016/j.bbrc.2012.03.083

Xanthorrhizol is a plant-derived pharmacologically active sesquiterpenoid compound isolated from Curcuma xanthorrhiza. Previously, we have reported that xanthorrhizol inhibited the proliferation of HepG2 human hepatoma cells by inducing apoptotic cell death via caspase activation. Here, we attempt to further elucidate the mode of action of xanthorrhizol. Apoptosis in xanthorrhizol-treated HepG2 cells as observed by scanning electron microscopy was accompanied by truncation of BID; reduction of both anti-apoptotic Bcl-2 and Bcl-X(L) expression; cleavage of PARP and DFF45/ICAD proteins and DNA fragmentation. Taken together, these results suggest xanthorrhizol as a potent antiproliferative agent on HepG2 cells by inducing apoptosis via Bcl-2 family members. Hence we proposed that xanthorrhizol could be used as an anti-liver cancer drug for future studies.

Matched MeSH terms: Phenols/pharmacology*

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