A new cycloartane, monocarpinine (1), incorporating a fused tetrahydrofuranyl ring, and a cytotoxic tetracyclic lactam, monomarginine (2), were isolated from a stem bark extract of the Malayan species Monocarpia marginalis. The structures of these compounds were determined using NMR and MS analysis. Monomarginine (2) showed appreciable cytotoxicity toward human KB (both drug-sensitive and drug-resistant) and Jurkat cells.
Four new 2,3-secodammarane triterpenoids, stellatonins A-D (3-6), together with a new 3,4-secodammarane triterpenoid, stellatonin E (7), and the known silvestrol (1), 5‴-episilvestrol (2), and β-sitosterol, were isolated from a methanol extract of the stems of Aglaia stellatopilosa through bioassay-guided fractionation. The structures of the new compounds were elucidated using spectroscopic and chemical methods. The compounds were evaluated for their cytotoxic activity against three human cancer cell lines and for their antimicrobial activity using a microtiter plate assay against a panel of Gram-positive and Gram-negative bacteria and fungi.
'Pegaga' is a traditional Malay remedy for a wide range of complaints. Among the 'pegaga', Centella asiatica has been used as a remedy for diabetes mellitus. Thus, we decided to validate this claim by evaluating the in vivo antidiabetic property of C. asiatica (CA) on T2DM rat model using the holistic (1)H NMR-based metabolomics approach.
Muntingia calabura has a high phytochemical content, especially the phenolic group that can act as antioxidant. In Malaysia country, this M. calabura also known as ‘kerukup siam’ or ‘Ceri Kampung’ and it belongs to Muntingiaceae family. This research was conducted to determine the potential of antioxidant activity application of cherry leaves (M. calabura) from various solvent extracts (methanol, ethyl acetate, and n-hexane). The phytochemical contents was screening by using the established standard procedure. Total phenolic content (TPC) was determined according to the Folin-Ciocalteau colorimetric method, while the antioxidant activity was carried out using 2,2-diphenyl-1-picryhydrazyl (DPPH) radical scavenging assay. Phytochemical screening on the leaves part methanolic extracts revealed that the presence of various biochemicals like flavonoids, phenols, steroids, triterpenes, tannins, reducing sugars, and saponins except the alkaloids. Among the three extracts, the methanol leaf extract gave the highest content of phenolics (8.20 mg GAE/g extract). Analyses of antioxidant activity with DPPH method showed that cherry leaf methanolic extracts produced high antioxidant activity with IC50 value of 167.70 g/mL. The present study confirms that the presence of various phytochemicals which shows good antioxidant activity of M. calabura leaves. Therefore, it has the potential as a therapeutic antioxidant agent and can be used in cosmeceutical and food products.
Phytochemical study was conducted on the leaves of Globimetula braunii which is a hemi parasitic plant belonging to the family Loranthaceae. Extraction was carried out using cold extraction method with increasing polarity of solvents i.e n-hexane, CH2Cl2 and MeOH. The components were separated by chromatographic technique and the structures of the compounds were elucidated by extensive spectroscopic analyses including MS, FTIR, 1D and 2D NMR, HRMS and chemical methods. Six new pentacyclic triterpenoid esters named as globrauneine A (1), globrauneine B (2), globrauneine C (3), globrauneine D (4), globrauneine E (5), and globrauneine F (6), together with six known compounds (7 - 12) were successfully isolated from the leaves of G. braunii growing on Piliostigma thonningii. These results depict a substantial support to the chemotaxonomy of the genus Globimetula.
In the recent years, much attention has been focused on identifying bioactive compounds from medicinal plants that could be employed in therapeutics, which is attributed to their potent pharmacological actions and better toxicological profile. One such example that has come into the light with considerable interest is the pentacyclic triterpenoid, celastrol, which has been found to provide substantial therapeutic properties in a variety of diseases. In an effort to further accelerate its potential to be utilized in clinical practice in the future; along with advancing technologies in the field of drug discovery and development, different researchers have been investigating on the various mechanisms and immunological targets of celastrol that underlie its broad spectrum of pharmacological properties. In this review, we have collated the various research findings related to the molecular modulators responsible for different pharmacological activities shown by celastrol. Our review will be of interest to the herbal, biological, molecular scientist and by providing a quick snapshot about celastrol giving a new direction in the area of herbal drug discovery and development.
In this study, Centella asiatica and surface soils were collected from 12 sampling sites in Peninsular Malaysia, and the barium (Ba) concentrations were determined. The Ba concentration [μg/g dry weight (dw)] was 63.72 to 382.01 μg/g in soils while in C. asiatica, Ba concentrations ranged from 5.05 to 21.88 μg/g for roots, 3.31 to 11.22 μg/g for leaves and 2.37 to 6.14 μg/g for stems. In C. asiatica, Ba accumulation was found to be the highest in roots followed by leaves and stems. The correlation coefficients (r) of Ba between plants and soils were found to be significantly positively correlated, with the highest correlation being between roots-soils (r=0.922, p<005), followed by leaves-soils (r=0.890, p<005) and stems-soils (r=0.848, p<005). This indicates that these three parts of C. asiatica are good biomonitors of Ba pollution. For the transplantation study, four sites were selected as unpolluted [(Universiti Putra Malaysia (UPM)], semi-polluted (Seri Kembangan and Balakong) and polluted sites (Juru). Based on the transplantation study under experimental field and laboratory conditions, Ba concentrations in C. asiatica were significantly (p<0.05) higher after three weeks of exposure at Seri Kembangan, Balakong and Juru. Thus, these experimental findings confirm that the leaves, stems and roots of C. asiatica can reflect the Ba levels in the soils where this plant is found. Three weeks after back transplantation to clean soils, the Ba levels in C. asiatica were still higher than the initial Ba level even though Ba elimination occurred. In conclusion, the leaves, stems and roots of C. asiatica are good biomonitors of Ba pollution.
The preliminary ichthyotoxic test on all parts of Syzygium malaccense (Myrtaceae) revealed that the leaves fraction was the most ichthyotoxic against tilapia-fish (Tilapia oreochromis). Three compounds, namely ursolic acid (1), β-sitosterol (2) and sitost-4-en-3-one (3), were isolated and their structures were elucidated with the aid of spectroscopic data and comparison with previously reported investigations. However none of these compounds gave any significant ichthyotoxicity. The volatile constituents of the leaves and fruit were determined by Gas Chromatography-Mass Spectrometer (GC-MS), with 180 and 203 compounds being identified in the aroma concentrates, respectively.
Keupayaan Centella asiatica (CA) untuk bertindak sebagai antioksidan dan agen anti-radang telah banyak dilaporkan. Namun begitu, kaedah pengekstrakan CA untuk memperoleh hasil yang terbaik masih dipersoalkan. Dalam kajian ini, kami menilai tiga kaedah pengekstrakan CA dan membuat perbandingan ekstrak dari segi aktiviti antioksidan dan anti-radang, dan juga kandungan sebatian bioaktif, asiaticoside dan madecassoside. Centella asiatica diekstrak menggunakan pelarut etanol, metanol dan juga air. Kandungan sebatian fenolik ekstrak diukur menggunakan kaedah reagen Folin-Ciocalteu. Kandungan asiaticoside dan madecassoside ditentukan dengan kaedah HPLC. Aktiviti antioksidan diukur dengan asai 2,2-diphenyl-1-picrylhydrazyl (DPPH) dan asai penurunan kuasa Ferric Reducing Antioxidant Power (FRAP). Aktiviti anti-radang ditentukan dengan kebolehan ekstrak untuk merencatkan enzim tapakjalan keradangan, COX-1 dan COX-2, serta kebolehan ekstrak melindungi sel fibroblas aruhan 12-O-tetradecanoylphorbol-13-acetate (TPA) daripada menghasilkan prostaglandin E2 (PGE2 ). Hasil kajian menunjukkan aras sebatian fenolik, asiaticoside dan madecassoside tertinggi dalam ekstrak etanol, diikuti metanol dan esktrak akues (masing-masing 17.76 g/100g, 15.52 g/100g, 13.16 g/100g untuk sebatian fenolik, 42.86 mg/g, 36.37 mg/g, 2.82 mg/g untuk asiaticoside and 18.66 mg/g, 15.87 mg/g, 3.75 mg/g untuk madecassoside). Ketiga-tiga ekstrak menunjukkan aktiviti antioksidan sederhana berbanding kawalan positif. Kesemua ekstrak, asiaticoside dan madecassoside merencat COX-1 dan COX-2 dan menyekat penghasilan PGE2 -aruhan TPA. Ekstrak etanol dan metanol merupakan perencat COX yang lebih kuat dan lebih poten daripada ekstrak akues. Oleh itu, walaupun ekstrak akues menunjukkan kebolehan antioksidan yang lebih tinggi, dari segi aktiviti anti-radang, pelarut hidrofobik iaitu etanol dan metanol ternyata lebih baik untuk mengekstrak Centella asiatica.
Callus was induced from mangosteen (Garcinia mangostana L.) young purple-red leaves on Murashige and Skoog basal medium with various combinations of plant growth regulators. Murashige and Skoog medium with 4.44 µM 6-benzylaminopurine and 4.52 µM 2,4-dichlorophenoxyacetic acid was the best for friable callus induction. This friable callus was used for the initiation of cell suspension culture. The effects of different combinations of 6-benzylaminopurine and 2,4-dichlorophenoxyacetic acid, carbon sources and inoculum sizes were tested. It was found that combination of 2.22 µM 6-benzylaminopurine + 2.26 µM 2,4-dichlorophenoxyacetic acid, glucose (30 g/l) and 1.5 g/50 ml inoculum size was the best for cell growth. Callus and cell suspension cultures were then treated either with 100 µM methyl jasmonate as an elicitor for 5 days, or 0.5 g/l casein hydrolysate as an organic supplement for 7 days. Metabolites were then extracted and profiled using liquid chromatography-time of flight mass spectrometry. Multivariate discriminant analyses revealed significant metabolite differences (P ≤ 0.05) for callus and suspension cells treated either with methyl jasmonate or casein hydrolysate. Based on MS/MS data, methyl jasmonate stimulated the production of an alkaloid (thalsimine) and fatty acid (phosphatidyl ethanolamine) in suspension cells while in callus, an alkaloid (thiacremonone) and glucosinolate (7-methylthioheptanaldoxime) was produced. Meanwhile casein hydrolysate stimulated the production of alkaloids such as 3ß,6ß-dihydroxynortropane and cis-hinokiresinol and triterpenoids such as schidigerasaponin and talinumoside in suspension cells. This study provides evidence on the potential of secondary metabolite production from in vitro culture of mangosteen.
Centella asiatica, a weakly aromatic plant that flourishes in wet tropical and sub-tropical areas as
a medicinal species since ancient times. It contained important terpenoids that impart important
medicinal values. Currently, studies on the terpenoid content of various Centella asiatica
phenotypes have shown not only variable content but variable growth rates of different
phenotypes that can affect future selection of phenotypes. The use of mathematical growth
modelling can reveal important growth constants and discriminate between faster and slower
growth phenotypes. Two Centella asiatica phenotypes from South Africa is modelled using the
modified Gompertz model and the results showed that the C. asiatica Type-1 exhibited a faster
growth rates and a shorter lag period at 0.152 day-1 and 2.313 day than another phenotype; C.
asiatica Type 2 with a growth rate and a lag period of 0.067 day-1 and 3.363 day, respectively.
The data indicates that different phenotypes of C. asiatica can have different growth rates and
lag period and this can be important for selection of phenotypes to be used as the best bioactive
peptides producer.
Microfungi isolated from Malay traditional vegetables such as Centella asiatica, Cosmos caudatus, Oenanthe javanica, Persicaria odorata and Psophocarpus tetragonolobus are well diverse. A total of 40 isolates of the fungi were identified and classified into four genera such as Aspergillus, Fusarium, Penicillium and Trichoderma. Five species of Fusarium were morphologically identified as F. oxysporum, F. semitectum, F. proliferatum, F. solani and F. konzum. Three species of Aspergillus were identified as A. niger, A. fumigatus and A. flavus. The highest number of microfungi was isolated from Cosmos caudatus (12 isolates), followed by Persicaria odorata (9 isolates), Oenanthe javanica (8 isolates), Centella asiatica (6 isolates) and Psophocarpus tetragonolobus (5 isolates). Four isolates of Fusarium species were able to produce moniliformin (MON) and five isolates were able to produce fumonisin B1 (FB1). This is the first report on diversity of microfungi associated with some Malay traditional vegetables.
Ursolic acid (UA) is a pentacyclic triterpene of the ursane type. As a common chemical constituent among species of the family Lamiaceae, UA possesses a broad spectrum of pharmacological properties. This overview focuses on the anticancer properties of UA against breast cancer (BC) and colorectal cancer (CRC) that are most common among women and men, respectively. In vitro studies have shown that UA inhibited the growth of BC and CRC cell lines through various molecular targets and signaling pathways. There are several in vivo studies on the cytotoxic activity of UA against BC and CRC. UA also inhibits the growth of other types of cancer. Studies on structural modifications of UA have shown that the -OH groups at C3 and at C28 are critical factors influencing the cytotoxic activity of UA and its derivatives. Some needs for future research are suggested. Sources of information were from ScienceDirect, Google Scholar and PubMed.
Recently, we have isolated koetjapic acid (KA) from Sandoricum koetjape and identified its selective anticancer potentiality against colorectal carcinoma. KA is quite likely to be useful as a systemic anticancer agent against colorectal malignancy. However, with extremely low solubility, KA has to be converted into a biocompatible solubilized form without compromising the bioefficacy. Objective of this study is to enhance solubility of KA and to evaluate anticancer efficacy of potassium koetjapate in human colorectal cancer cells.
2α,3α,24-Thrihydroxyurs-12-en-28-oicacid (TEOA), a pentacyclic triterpenoid, isolated from the roots of Actinidia eriantha, exhibits significant cytotoxicity against SW620, BGC-823, HepG-2, A549 and PC-3 cancer cells. In this study, we investigated the underlying molecular mechanism of the anticancer activity of TEOA in SW620 cells. We demonstrated that TEOA induced apoptosis through cleavage of caspase-9 and PARP in SW620 cells. In addition, evidence of TEOA-mediated autophagy included the induction of autophagolysosomes and activation of autophagic markers LC-3B and p62. Further analysis illustrated that TEOA promoted the phosphorylation of PERK and elF2α, followed by up-regulation of the downstream protein CHOP, suggesting the involvement of PERK/eIF2α/CHOP pathway and ER stress in TEOA-induced autophagy in SW620 cells. Meanwhile, TEOA-mediated PINK1, Parkin, ubiquitin and p62 activation revealed that TEOA induced specific autophagy-mitophagy in SW620 cells. Additionally, an antioxidant NAC attenuated the TEOA-induced mitophagy, indicating that TEOA triggers mitophagy via a ROS-dependent pathway. Collectively, our findings revealed a novel cellular mechanism of TEOA in the colon cancer cell line SW620, thus providing a molecular basis for developing TEOA into an anti-tumor candidate.
Acanthamoeba species are pathogenic protozoa which account for amoebic keratitis, conjunctivitis and granulomatous amoebic encephalitis. These amoebae form cysts which resist drugs and more effective acanthamoebicidal agents are needed. Medicinal plants could be useful in improving the current treatment strategies for Acanthamoeba infections. In the present study, we examined the amoebicidal effects of Pericampylus glaucus (Lam.) Merr., a medicinal plant used for the treatment of conjunctivitis in Malaysia. Pathogenic Acanthamoeba triangularis were isolated from environmental water samples and treated with different concentrations of fractions obtained from Pericampylus glaucus (Lam.) Merr. as well as main constituents for 24-72 h. Chlorhexidine was used as a reference drug. Ethanol fraction of stem showed significant (p
Bacopa monnieri has been used in Ayurvedic medicine to improve memory and cognition. The active constituent responsible for its pharmacological effects is bacoside A, a mixture of dammarane-type triterpenoid saponins containing sugar chains linked to a steroid aglycone skeleton. Triterpenoid saponins have been reported to be transformed in vivo to metabolites that give better biological activity and pharmacokinetic characteristics. Thus, the activities of the parent compounds (bacosides), aglycones (jujubogenin and pseudojujubogenin) and their derivatives (ebelin lactone and bacogenin A1) were compared using a combination of in silico and in vitro screening methods. The compounds were docked into 5-HT1A, 5-HT2A, D1, D2, M1 receptors and acetylcholinesterase (AChE) using AutoDock and their central nervous system (CNS) drug-like properties were determined using Discovery Studio molecular properties and ADMET descriptors. The compounds were screened in vitro using radioligand receptor binding and AChE inhibition assays. In silico studies showed that the parent bacosides were not able to dock into the chosen CNS targets and had poor molecular properties as a CNS drug. In contrast, the aglycones and their derivatives showed better binding affinity and good CNS drug-like properties, were well absorbed through the intestines and had good blood brain barrier (BBB) penetration. Among the compounds tested in vitro, ebelin lactone showed binding affinity towards M1 (Ki = 0.45 μM) and 5-HT2A (4.21 μM) receptors. Bacoside A and bacopaside X (9.06 μM) showed binding affinity towards the D1 receptor. None of the compounds showed any inhibitory activity against AChE. Since the stimulation of M1 and 5-HT2A receptors has been implicated in memory and cognition and ebelin lactone was shown to have the strongest binding energy, highest BBB penetration and binding affinity towards M1 and 5-HT2A receptors, we suggest that B. monnieri constituents may be transformed in vivo to the active form before exerting their pharmacological activity.
We aimed to assess the efficacy of Centella asiatica for improvement of the signs and symptoms of chronic venous insufficiency (CVI). We searched 13 electronic databases including the Cochrane Central Register of Controlled Trials for randomised controlled trials assessing the efficacy of Centella asiatica for CVI. Two review authors independently selected studies, assessed the risks of bias of included studies and extracted data. The treatment effects of similar studies were pooled whenever appropriate. Eight studies met the inclusion criteria. The pooling of data of similar studies showed that Centella asiatica significantly improved microcirculatory parameters such as transcutaneous partial pressure of CO2 and O2, rate of ankle swelling and venoarteriolar response. Three out of the eight studies did not provide quantitative data. However, these studies reported that patients treated with Centella asiatica showed significant improvement in CVI signs such as leg heaviness, pain and oedema. Our results show that Centella asiatica may be beneficial for improving signs and symptoms of CVI but this conclusion needs to be interpreted with caution as most of the studies were characterised by inadequate reporting and thus had unclear risks of bias, which may threaten the validity of the conclusions.
This study compares different solvent systems with the use of spontaneous fermentation on the phytochemical composition of leaf extracts from a locally grown white variety of common fig (Ficus carica Linn.). The aim was to detect and identify bioactive compounds that are responsible for acetylcholinesterase (AChE), α-amylase and cyclooxygenase-1 (COX-1) enzyme inhibition, and compounds that exhibit antimicrobial activity. Bioactive zones in chromatograms were detected by combining High-performance thin-layer chromatography (HPTLC) with enzymatic and biological assays. A new experimental protocol for measuring the relative half-maximum inhibitory concentration (IC50) was designed to evaluate the potency of the extracts compared to the potency of known inhibitors. Although the IC50 of the fig leaf extract for α-amylase and AChE inhibition were significantly higher when compared to IC50 for acarbose and donepezil, the COX-1 inhibition by the extract (IC50 = 627 µg) was comparable to that of salicylic acid (IC50 = 557 µg), and antimicrobial activity of the extract (IC50 = 375-511 µg) was similar to ampicillin (IC50 = 495 µg). Four chromatographic zones exhibited bioactivity. Compounds from detected bioactive bands were provisionally identified by comparing the band positions to coeluted standards, and by Fourier transform infrared (FTIR) spectra from eluted zones. Flash chromatography was used to separate selected extract into fractions and isolate fractions that are rich in bioactive compounds for further characterisation with nuclear magnetic resonance (NMR) spectroscopy and liquid chromatography-mass spectrometry (LC-MS) analysis. The main constituents identified were umbelliferon (zone 1), furocoumarins psoralen and bergapten (zone 2), different fatty acids (zone 3 and 4), and pentacyclic triterpenoids (calotropenyl acetate or lupeol) and stigmasterol (zone 4).
The antinociceptive property of Centella asiatica extracts is known but the analgesic activity of its bioactive constituent asiaticoside has not been reported. We evaluated the antinociceptive activity of orally (p. o.) administered asiaticoside (1, 3, 5, and 10 mg/kg) in mice using the 0.6% acetic acid-induced writhing test, the 2.5% formalin-induced paw licking test, and the hot plate test. The capsaicin- and glutamate-induced paw licking tests were employed to evaluate the involvement of the vanilloid and glutamatergic systems, respectively. Asiaticoside (3, 5, and 10 mg/kg, p. o.) reduced the rate of writhing (p