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Fulltext Cytotoxic, Anti-Proliferative and Apoptosis Activity of l-Amino Acid Oxidase from Malaysian Cryptelytrops purpureomaculatus (CP-LAAO) Venom on Human Colon Cancer Cells

Zainal Abidin SA, Rajadurai P, Hoque Chowdhury ME, Othman I, Naidu R

Molecules, 2018 06 08;23(6).
PMID: 29890640 DOI: 10.3390/molecules23061388

The aim of this study is to investigate the potential anti-cancer activity of l-amino acid oxidase (CP-LAAO) purified from the venom of Cryptelytrops purpureomaculatus on SW480 and SW620 human colon cancer cells. Mass spectrometry guided purification was able to identify and purify CP-LAAO. Amino acid variations identified from the partial protein sequence of CP-LAAO may suggest novel variants of these proteins. The activity of the purified CP-LAAO was confirmed with o-phenyldiamine (OPD)-based spectrophotometric assay. CP-LAAO demonstrated time- and dose-dependent cytotoxic activity and the EC50 value was determined at 13 µg/mL for both SW480 and SW620 cells. Significant increase of caspase-3 activity, reduction of Bcl-2 levels, as well as morphological changes consistent with apoptosis were demonstrated by CP-LAAO. Overall, these data provide evidence on the potential anti-cancer activity of CP-LAAO from the venom of Malaysian C. purpureomaculatus for therapeutic intervention of human colon cancer.
Cytotoxic, Antiproliferative and Apoptosis-inducing Activity of L-Amino Acid Oxidase from Malaysian Calloselasma rhodostoma on Human Colon Cancer Cells

Zainal Abidin SA, Rajadurai P, Chowdhury MEH, Ahmad Rusmili MR, Othman I, Naidu R

Basic Clin Pharmacol Toxicol, 2018 Nov;123(5):577-588.
PMID: 29908095 DOI: 10.1111/bcpt.13060

The aim of this study was to investigate the cytotoxic, antiproliferative activity and the induction of apoptosis by L-amino acid oxidase isolated from Calloselasma rhodostoma crude venom (CR-LAAO) on human colon cancer cells. CR-LAAO was purified using three chromatographic steps: molecular exclusion using G-50 gel filtration resin, ion-exchange by MonoQ column and desalted on a G25 column. The purity and identity of the isolated CR-LAAO was confirmed by SDS-PAGE and LC-MS/MS. CR-LAAO demonstrated time- and dose-dependent cytotoxic activity on SW480 (primary human colon cancer cells) and SW620 (metastatic human colon cancer cells) with an EC50 values of 6 μg/ml and 7 μg/ml at 48 hr, respectively. Quantification of apoptotic cells based on morphological features demonstrated significant increase in apoptotic cell population in both SW480 and SW620 cells which peaked at 48 hr. Significant increase in caspase-3 activity and reduction in Bcl-2 levels were demonstrated following CR-LAAO treatment. These data provide evidence on the potential anticancer activity of CR-LAAO from the venom of C. rhodostoma for therapeutic intervention of human colon cancer.
Proteomic Characterization and Comparison of Malaysian Tropidolaemus wagleri and Cryptelytrops purpureomaculatus Venom Using Shotgun-Proteomics

Zainal Abidin SA, Rajadurai P, Chowdhury ME, Ahmad Rusmili MR, Othman I, Naidu R

Toxins (Basel), 2016 10 18;8(10).
PMID: 27763534

Tropidolaemus wagleri and Cryptelytrops purpureomaculatus are venomous pit viper species commonly found in Malaysia. Tandem mass spectrometry analysis of the crude venoms has detected different proteins in T. wagleri and C. purpureomaculatus. They were classified into 13 venom protein families consisting of enzymatic and nonenzymatic proteins. Enzymatic families detected in T. wagleri and C. purpureomaculatus venom were snake venom metalloproteinase, phospholipase A₂, ʟ-amino acid oxidase, serine proteases, 5'-nucleotidase, phosphodiesterase, and phospholipase B. In addition, glutaminyl cyclotransferase was detected in C. purpureomaculatus. C-type lectin-like proteins were common nonenzymatic components in both species. Waglerin was present and unique to T. wagleri-it was not in C. purpureomaculatus venom. In contrast, cysteine-rich secretory protein, bradykinin-potentiating peptide, and C-type natriuretic peptide were present in C. purpureomaculatus venom. Composition of the venom proteome of T. wagleri and C. purpureomaculatus provides useful information to guide production of effective antivenom and identification of proteins with potential therapeutic applications.
Cord IgE and ECP levels of Malay neonates

Yadav A, Naidu R

Allergol Immunopathol (Madr), 2013 Nov-Dec;41(6):364-8.
PMID: 23276420 DOI: 10.1016/j.aller.2012.08.007

Cord IgE and ECP levels are major atopic markers implicated in early childhood allergy development. Most epidemiological studies to date have not utilised current technology to establish baseline cord IgE levels, further aggravated by lack of data in this region. This study also attempts to identify a relationship between cord IgE and ECP levels as a mean to improve sensitivity for early prediction of atopy.
Fulltext Clinical manifestation and sensitization of allergic children from Malaysia

Yadav A, Naidu R

Asia Pac Allergy, 2015 Apr;5(2):78-83.
PMID: 25938072 DOI: 10.5415/apallergy.2015.5.2.78

An epidemiological rise of allergic diseases in developing countries raises new challenges. Currently a paucity of data exists describing allergy symptomology and sensitization to common food and aeroallergens in young children from developing countries.
Fulltext Anticancer Mechanism of Curcumin on Human Glioblastoma

Wong SC, Kamarudin MNA, Naidu R

Nutrients, 2021 Mar 16;13(3).
PMID: 33809462 DOI: 10.3390/nu13030950

Glioblastoma (GBM) is the most malignant brain tumor and accounts for most adult brain tumors. Current available treatment options for GBM are multimodal, which include surgical resection, radiation, and chemotherapy. Despite the significant advances in diagnostic and therapeutic approaches, GBM remains largely resistant to treatment, with a poor median survival rate between 12 and 18 months. With increasing drug resistance, the introduction of phytochemicals into current GBM treatment has become a potential strategy to combat GBM. Phytochemicals possess multifarious bioactivities with multitarget sites and comparatively marginal toxicity. Among them, curcumin is the most studied compound described as a potential anticancer agent due to its multi-targeted signaling/molecular pathways properties. Curcumin possesses the ability to modulate the core pathways involved in GBM cell proliferation, apoptosis, cell cycle arrest, autophagy, paraptosis, oxidative stress, and tumor cell motility. This review discusses curcumin's anticancer mechanism through modulation of Rb, p53, MAPK, P13K/Akt, JAK/STAT, Shh, and NF-κB pathways, which are commonly involved and dysregulated in preclinical and clinical GBM models. In addition, limitation issues such as bioavailability, pharmacokinetics perspectives strategies, and clinical trials were discussed.
Fulltext Molecular Mechanisms of Antiproliferative and Apoptosis Activity by 1,5-Bis(4-Hydroxy-3-Methoxyphenyl)1,4-Pentadiene-3-one (MS13) on Human Non-Small Cell Lung Cancer Cells

Wan Mohd Tajuddin WNB, Abas F, Othman I, Naidu R

Int J Mol Sci, 2021 Jul 10;22(14).
PMID: 34299042 DOI: 10.3390/ijms22147424

Diarylpentanoid (DAP), an analog that was structurally modified from a naturally occurring curcumin, has shown to enhance anticancer efficacy compared to its parent compound in various cancers. This study aims to determine the cytotoxicity, antiproliferative, and apoptotic activity of diarylpentanoid MS13 on two subtypes of non-small cell lung cancer (NSCLC) cells: squamous cell carcinoma (NCI-H520) and adenocarcinoma (NCI-H23). Gene expression analysis was performed using Nanostring PanCancer Pathways Panel to determine significant signaling pathways and targeted genes in these treated cells. Cytotoxicity screening revealed that MS13 exhibited greater inhibitory effect in NCI-H520 and NCI-H23 cells compared to curcumin. MS13 induced anti-proliferative activity in both cells in a dose- and time-dependent manner. Morphological analysis revealed that a significant number of MS13-treated cells exhibited apoptosis. A significant increase in caspase-3 activity and decrease in Bcl-2 protein concentration was noted in both MS13-treated cells in a time- and dose-dependent manner. A total of 77 and 47 differential expressed genes (DEGs) were regulated in MS13 treated-NCI-H520 and NCI-H23 cells, respectively. Among the DEGs, 22 were mutually expressed in both NCI-H520 and NCI-H23 cells in response to MS13 treatment. The top DEGs modulated by MS13 in NCI-H520-DUSP4, CDKN1A, GADD45G, NGFR, and EPHA2-and NCI-H23 cells-HGF, MET, COL5A2, MCM7, and GNG4-were highly associated with PI3K, cell cycle-apoptosis, and MAPK signaling pathways. In conclusion, MS13 may induce antiproliferation and apoptosis activity in squamous cell carcinoma and adenocarcinoma of NSCLC cells by modulating DEGs associated with PI3K-AKT, cell cycle-apoptosis, and MAPK pathways. Therefore, our present findings could provide an insight into the anticancer activity of MS13 and merits further investigation as a potential anticancer agent for NSCLC cancer therapy.
Fulltext Mechanistic Understanding of Curcumin's Therapeutic Effects in Lung Cancer

Wan Mohd Tajuddin WNB, Lajis NH, Abas F, Othman I, Naidu R

Nutrients, 2019 Dec 06;11(12).
PMID: 31817718 DOI: 10.3390/nu11122989

Lung cancer is among the most common cancers with a high mortality rate worldwide. Despite the significant advances in diagnostic and therapeutic approaches, lung cancer prognoses and survival rates remain poor due to late diagnosis, drug resistance, and adverse effects. Therefore, new intervention therapies, such as the use of natural compounds with decreased toxicities, have been considered in lung cancer therapy. Curcumin, a natural occurring polyphenol derived from turmeric (Curcuma longa) has been studied extensively in recent years for its therapeutic effects. It has been shown that curcumin demonstrates anti-cancer effects in lung cancer through various mechanisms, including inhibition of cell proliferation, invasion, and metastasis, induction of apoptosis, epigenetic alterations, and regulation of microRNA expression. Several invitro and invivo studies have shown that these mechanisms are modulated by multiple molecular targets such as STAT3, EGFR, FOXO3a, TGF-β, eIF2α, COX-2, Bcl-2, PI3KAkt/mTOR, ROS, Fas/FasL, Cdc42, E-cadherin, MMPs, and adiponectin. In addition, limitations, strategies to overcome curcumin bioavailability, and potential side effects as well as clinical trials were also reviewed.
Fulltext Insights into the Role of microRNAs in Colorectal Cancer (CRC) Metabolism

Wai Hon K, Zainal Abidin SA, Othman I, Naidu R

Cancers (Basel), 2020 Aug 31;12(9).
PMID: 32878019 DOI: 10.3390/cancers12092462

Colorectal cancer (CRC) is one of the most frequently diagnosed cancers, with a high mortality rate globally. The pathophysiology of CRC is mainly initiated by alteration in gene expression, leading to dysregulation in multiple signalling pathways and cellular processes. Metabolic reprogramming is one of the important cancer hallmarks in CRC, which involves the adaptive changes in tumour cell metabolism to sustain the high energy requirements for rapid cell proliferation. There are several mechanisms in the metabolic reprogramming of cancer cells, such as aerobic glycolysis, oxidative phosphorylation, lactate and fatty acids metabolism. MicroRNAs (miRNAs) are a class of non-coding RNAs that are responsible for post-transcriptional regulation of gene expression. Differential expression of miRNAs has been shown to play an important role in different aspects of tumorigenesis, such as proliferation, apoptosis, and drug resistance, as well as metabolic reprogramming. Increasing evidence also reports that miRNAs could function as potential regulators of metabolic reprogramming in CRC cells. This review provides an insight into the role of different miRNAs in regulating the metabolism of CRC cells as well as to discuss the potential role of miRNAs as biomarkers or therapeutic targets in CRC tumour metabolism.
Fulltext Publisher Correction to: Insights into the demographic history of Asia from common ancestry and admixture in the genomic landscape of present-day Austroasiatic speakers

Tagore D, Aghakhanian F, Naidu R, Phipps ME, Basu A

BMC Biol, 2021 Nov 04;19(1):238.
PMID: 34736468 DOI: 10.1186/s12915-021-01174-2
Fulltext Insights into the demographic history of Asia from common ancestry and admixture in the genomic landscape of present-day Austroasiatic speakers

Tagore D, Aghakhanian F, Naidu R, Phipps ME, Basu A

BMC Biol, 2021 03 29;19(1):61.
PMID: 33781248 DOI: 10.1186/s12915-021-00981-x

BACKGROUND: The demographic history of South and Southeast Asia (S&SEA) is complex and contentious, with multiple waves of human migration. Some of the earliest footfalls were of the ancestors of modern Austroasiatic (AA) language speakers. Understanding the history of the AA language family, comprising of over 150 languages and their speakers distributed across broad geographical region in isolated small populations of various sizes, can help shed light on the peopling of S&SEA. Here we investigated the genetic relatedness of two AA groups, their relationship with other ethno-linguistically distinct populations, and the relationship of these groups with ancient genomes of individuals living in S&SEA at different time periods, to infer about the demographic history of this region.
RESULTS: We analyzed 1451 extant genomes, 189 AAs from India and Malaysia, and 43 ancient genomes from S&SEA. Population structure analysis reveals neither language nor geography appropriately correlates with genetic diversity. The inconsistency between "language and genetics" or "geography and genetics" can largely be attributed to ancient admixture with East Asian populations. We estimated a pre-Neolithic origin of AA language speakers, with shared ancestry between Indian and Malaysian populations until about 470 generations ago, contesting the existing model of Neolithic expansion of the AA culture. We observed a spatio-temporal transition in the genetic ancestry of SEA with genetic contribution from East Asia significantly increasing in the post-Neolithic period.
CONCLUSION: Our study shows that contrary to assumptions in many previous studies and despite having linguistic commonality, Indian AAs have a distinct genomic structure compared to Malaysian AAs. This linguistic-genetic discordance is reflective of the complex history of population migration and admixture shaping the genomic landscape of S&SEA. We postulate that pre-Neolithic ancestors of today's AAs were widespread in S&SEA, and the fragmentation and dissipation of the population have largely been a resultant of multiple migrations of East Asian farmers during the Neolithic period. It also highlights the resilience of AAs in continuing to speak their language in spite of checkered population distribution and possible dominance from other linguistic groups.
Fulltext Receptor Tyrosine Kinases and Their Signaling Pathways as Therapeutic Targets of Curcumin in Cancer

Sudhesh Dev S, Zainal Abidin SA, Farghadani R, Othman I, Naidu R

Front Pharmacol, 2021;12:772510.
PMID: 34867402 DOI: 10.3389/fphar.2021.772510

Receptor tyrosine kinases (RTKs) are transmembrane cell-surface proteins that act as signal transducers. They regulate essential cellular processes like proliferation, apoptosis, differentiation and metabolism. RTK alteration occurs in a broad spectrum of cancers, emphasising its crucial role in cancer progression and as a suitable therapeutic target. The use of small molecule RTK inhibitors however, has been crippled by the emergence of resistance, highlighting the need for a pleiotropic anti-cancer agent that can replace or be used in combination with existing pharmacological agents to enhance treatment efficacy. Curcumin is an attractive therapeutic agent mainly due to its potent anti-cancer effects, extensive range of targets and minimal toxicity. Out of the numerous documented targets of curcumin, RTKs appear to be one of the main nodes of curcumin-mediated inhibition. Many studies have found that curcumin influences RTK activation and their downstream signaling pathways resulting in increased apoptosis, decreased proliferation and decreased migration in cancer both in vitro and in vivo. This review focused on how curcumin exhibits anti-cancer effects through inhibition of RTKs and downstream signaling pathways like the MAPK, PI3K/Akt, JAK/STAT, and NF-κB pathways. Combination studies of curcumin and RTK inhibitors were also analysed with emphasis on their common molecular targets.
Fulltext Observational study on cannulation rate during ERCP at hospital alor setar

Sivasubramaniam M, Naidu RR

Malays J Med Sci, 2001 Jan;8(1):25-30.
PMID: 22973152 MyJurnal

ERCP (Endoscopic Retrograde Cholangiopancreaticography) was introduced in this hospital in late 1995. Since then, a lot of improvement have been achieved in the management of biliary tract diseases. Various general surgeons posted to this hospital have been trained in this procedure. A study was done to include all patients admitted for ERCP from August 1998 to July 1999. A total of 322 new patients with a mean of 26.9 cases a month had underwent this procedure. The duration of cannulation varied from 2 minutes to 45 minutes with a mean of 12 minutes. Cannulation rate by various surgeons differed. Overall success rate was 80%. Mortality was 0.6 % and morbidity was 0.9%. ERCP is safe and it takes at least 6 months of regular duodenoscopy before one can master the technique. Achieving 80% cannulation rate, has definitely reduced unnecessary common bile duct (CBD) explorations. During this study we have trained various surgeons in this procedure and at least 2 surgeons could be credentialled according to the guidelines provided by the Malaysian Society of Gastroenterology and Hepatology. During this study we have identified various reasons for the failure of cannulation which are useful for future training of endoscopists.
Fulltext Twisted fate of bladder catheters

Sithasanan N, Kihne M, Naidu RR, Ramanujam TM

Med J Malaysia, 2006 Aug;61(3):369-70.
PMID: 17240594 MyJurnal

Catheter knotting is a rare complication of bladder catheterisation. Retention of catheter parts resulting in calculus formation is even rarer. We report a case of a vesical calculus formed over a broken and retained supra-pubic catheter which to the best of our knowledge has yet to be reported, along with three other cases of bladder catheter knotting.
Fulltext Renal papillary necrosis in the east coast of Peninsular Malaysia

Segasothy M, Kamal A, Das D, Naidu RR, Sivalingam S

Singapore Med J, 1990 Jun;31(3):250-2.
PMID: 2392703

Six hundred and one intravenous Urograms (IVU) done at the General Hospital, Kuala Trengganu from 1981 to 1985 were reviewed retrospectively for Renal Papillary Necrosis (RPN). It was found that 1.3% of IVUs had RPN. There was a higher incidence of RPN amongst males as compared to females. RPN occurred more commonly in the younger age groups.
Paraquat and Parkinson's Disease: The Molecular Crosstalk of Upstream Signal Transduction Pathways Leading to Apoptosis

See WZC, Naidu R, Tang KS

Curr Neuropharmacol, 2024;22(1):140-151.
PMID: 36703582 DOI: 10.2174/1570159X21666230126161524

Parkinson's disease (PD) is a heterogeneous disease involving a complex interaction between genes and the environment that affects various cellular pathways and neural networks. Several studies have suggested that environmental factors such as exposure to herbicides, pesticides, heavy metals, and other organic pollutants are significant risk factors for the development of PD. Among the herbicides, paraquat has been commonly used, although it has been banned in many countries due to its acute toxicity. Although the direct causational relationship between paraquat exposure and PD has not been established, paraquat has been demonstrated to cause the degeneration of dopaminergic neurons in the substantia nigra pars compacta. The underlying mechanisms of the dopaminergic lesion are primarily driven by the generation of reactive oxygen species, decrease in antioxidant enzyme levels, neuroinflammation, mitochondrial dysfunction, and ER stress, leading to a cascade of molecular crosstalks that result in the initiation of apoptosis. This review critically analyses the crucial upstream molecular pathways of the apoptotic cascade involved in paraquat neurotoxicity, including mitogenactivated protein kinase (MAPK), phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K)/AKT, mammalian target of rapamycin (mTOR), and Wnt/β-catenin signaling pathways.
Phytochemical profiling, antioxidant, enzyme inhibition and cytotoxic potential of Bougainvillea glabra flowers

Saleem H, Htar TT, Naidu R, Zengin G, Ahmad I, Ahemad N

Nat Prod Res, 2020 Sep;34(18):2602-2606.
PMID: 30600720 DOI: 10.1080/14786419.2018.1543684

In this study, phytochemical composition, antioxidant, enzyme inhibition and cytotoxic activities of methanol and dichloromethane (DCM) extracts of Bougainvillea glabra (B. glabra) flowers were investigated. Methanol extract was found to have higher total bioactive contents and UHPLC-MS analysis of methanol extract revealed the presence of well-known phenolic and flavonoid compounds. Antioxidant activities were performed by radical scavenging (DPPH and ABTS), reducing power (FRAP and CUPRAC), phosphomolybdenum (TAC) and metal chelating assays. From our result, we observed that methanol extract had many antioxidant compounds. The DCM extract exhibited higher cholinesterases and α-glucosidase enzyme inhibition, while methanol extract showed significant urease inhibition. Both extracts exhibited strong to moderate cytotoxicity against MCF-7, MDA-MB-231, CaSki, DU-145 and SW-480 cancer cells with IC50 values ranging from 88.49 to 304.7 µg/mL. The findings showed the B. glabra to possess considerable antioxidant, enzyme inhibition and cytotoxic potentials and therefore has potential to discover novel bioactive molecules.
Investigations into the therapeutic effects of aerial and stem parts of Buxus papillosa C.K. Schneid.: In vitro chemical, biological and toxicological perspectives

Saleem H, Htar TT, Naidu R, Ahmad I, Zengin G, Ahmad M, et al.

J Pharm Biomed Anal, 2019 Mar 20;166:128-138.
PMID: 30640043 DOI: 10.1016/j.jpba.2019.01.007

In this study, different solvent extracts (methanol, dichloromethane and n-hexane) from aerial and stem parts of Buxus papillosa C.K. Schneid (Buxaceae) were investigated for a panoply of bioassays. Biological profiles were established by determining antioxidant and enzyme inhibition profiles. Toxicity was tested using MTT cell viability assay on five different human cancer cell lines i.e, MCF-7, MDA-MB-231, CaSki, DU-145 and SW-480. For chemical fingerprinting, total bioactive contents and UHPLC-MS secondary metabolites profile were determined. Generally, both aerial and stem methanol extracts had highest total bioactive contents, radical scavenging and reducing power potential. DCM and n-hexane extracts were found to be most active for total antioxidant and metal chelating activity. The UHPLC-MS analysis of methanol extracts revealed the presence of several phenolic, flavonoid, alkaloid, saponin and depsipeptide derivatives. All the extracts were significantly active against butyrylcholinesterase, whereas moderate inhibition was observed for acetylcholinesterase, α-glucosidase and urease. Similarly, a considerable level of cytotoxicity was observed against all the tested cell lines with IC50 values ranging from 26 to 225.9 μg/mL. Aerial methanol and stem n-hexane extracts were found to be most cytotoxic. Principal component analysis was also performed to find any possible correlation between biological activities and total bioactive contents. On the basis of our findings, B. papillosa may be considered as promising source of bioactive molecules.
Biological, chemical and toxicological perspectives on aerial and roots of Filago germanica (L.) huds: Functional approaches for novel phyto-pharmaceuticals

Saleem H, Htar TT, Naidu R, Nawawi NS, Ahmad I, Ashraf M, et al.

Food Chem Toxicol, 2019 Jan;123:363-373.
PMID: 30419323 DOI: 10.1016/j.fct.2018.11.016

We investigated into the effects of methanol and dichloromethane extracts from aerial and roots of Filago germanica (L.) Huds (Astearaceae) on key enzymes (cholinesterases, α-glucosidase and urease), antioxidant capabilities, cytotoxic potential and secondary metabolomics profile. Total phenolic and flavonoids were determined by spectrophotometric technique and secondary metabolites composition by UHPLC-MS. Antioxidant activities were assessed employing free radical scavenging, ferric reducing power and phosphomolybdenum assays. The cell-toxicity was evaluated by MTT assay against breast (MCF-7, MDA-MB-231), cervix (CaSki) and prostate (DU-145) cancers. Overall, methanol extracts were found to have higher total bioactive contents and antioxidant potential. UHPLC-MS analysis revealed significant variation in the secondary metabolites in the methanol extracts. The most common derivatives belong to seven groups i.e. alkaloids, benzoic acids, flavones, flavonols, flavan-3-ols, terpenoids and saponins. The major polyphenolic compounds were found to be kampferol, robinin, luteolin, ferulic acid, benzoic acid and salicylic acid. All the extracts showed moderate cholinesterases inhibition, whereas methanol extracts exhibited highest urease inhibition and all extracts presented a relatively high inhibition against α-glucosidase. Similarly, all extracts showed strong to moderate cytotoxicity with IC50 values ranging from 53.02 to 382.7 μg/mL. Overall, results have suggested F. germanica to be a lead source for novel natural products.
Therapeutic propensities, phytochemical composition, and toxicological evaluation of Anagallis arvensis (L.): A wild edible medicinal food plant

Saleem H, Zengin G, Ahmad I, Htar TT, Naidu R, Mahomoodally MF, et al.

Food Res Int, 2020 11;137:109651.
PMID: 33233230 DOI: 10.1016/j.foodres.2020.109651

Anagallis arvensis (L.) is a wild edible food plant that has been used in folklore as a natural remedy for treating common ailments. This study aimed to explore the biochemical properties and toxicity of methanol (MeOH) and dichloromethane (DCM) extracts of A. arvensis (aerial and root parts). Bioactive contents were assessed spectrophotometrically, and the secondary metabolites were identified by UHPLC-MS analysis. DPPH, ABTS, FRAP, CUPRAC, phosphomolybdenum, and metal chelating assays were employed to assess antioxidant activity. Inhibitory potential against key enzymes (α-glucosidase, urease, lipoxygenase (LOX), acetylcholinesterase (AChE), and butyrylcholinesterase (BChE)) were also assessed. MTT assay was employed to test toxicity against SW-480, MDA-MB-231, CaSki, MCF-7, and DU-145 cancer cell lines. Methanolic extracts showed highest phenolic (aerial-MeOH: 27.5 mg GAE/g extract; root-MeOH: 21.17 mg GAE/g extract) and flavonoid (aerial-MeOH: 26.15 mg QE/g extract; root-MeOH: 19.07 mg QE/g extract) contents, and potent antioxidant activities. The aerial-MeOH extract was most potent for DPPH (IC50: 231 ug/mL), ABTS (131.12 mg TE/g extract), FRAP (82.97 mg TE/g extract), and CUPRAC (137.15 mg TE/g extract) antioxidant assays. All extracts were cytotoxic towards tested cancer cells with IC50 values ranging from 12.57 to 294.5 µg/mL and conferred a comparatively strong inhibition against α-glucosidase (aerial-DCM extract showed the highest inhibition against α-glucosidase with IC50 value of 20.97 µg /mL), while aerial extracts were also considerably active against BChE (aerial-MeOH IC50: 224.63 µg /mL), LOX (aerial-DCM IC50: 385.7 µg /mL). Likewise, aerial-MeOH extract was most active against urease enzyme (IC50: 129.72 µg /mL). UHPLC-MS investigation of methanolic extracts showed the existence of important phenolics, flavonoids, and saponins, including methyl gallte, quercetin, lanceoletin, and balanitesin, amongst others. Moreover, principal component analysis (PCA) highlighted the correlation amongst bioactive contents and observed biological activities. A. arvensis extracts could be regarded as a natural source of bioactive antioxidants, enzyme inhibitors and anticancer agents and can be further investigated as a lead source for food and pharmaceutical products. However, further studies to isolate, purify, and to characterize its bioactive phytochemicals are needed.

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