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Vasodilator effect of Phlomis bracteosa constituents is mediated through dual endothelium-dependent and endothelium-independent pathways

Khan AU, Ullah R, Khan A, Mustafa MR, Hussain J, Murugan DD, et al.

Clin Exp Hypertens, 2012;34(2):132-9.
PMID: 21967029 DOI: 10.3109/10641963.2011.601383

This study describes the vasorelaxant potential of some pure compounds isolated from Phlomis bracteosa L. marrubiin, phlomeoic acid, and two new constituents labeled as RA and RB. In rat thoracic aortic rings denuded of endothelium, marrubiin, phlomeoic acid, RA, and RB caused relaxation of high K(+) (80 mM) and phenylephrine (1 μM)-induced contractions at the concentration range of 1.0-1000 μg/mL. Marrubiin, phlomeoic acid, RA, and RB concentration dependently (3.0-10 μg/mL) shifted the Ca(++) curves to the right obtained in Ca(++)-free medium. The vasodilator effect of marrubiin, phlomeoic acid, RA, and RB was partially blocked by N(ω)-nitro-L-arginine methyl ester in endothelium-intact aorta preparations. These results reveal that P. bracteosa constituents: marrubiin, phlomeoic acid, RA, and RB exhibit vasodilator action occurred via a combination of endothelium-independent Ca(++) antagonism and endothelium-dependent N(ω)-nitro-L-arginine methyl ester-sensitive nitric oxide-modulating mechanism.

Matched MeSH terms: Plants, Medicinal/chemistry
Fulltext Screening of antiviral activities in medicinal plants extracts against dengue virus using dengue NS2B-NS3 protease assay

Rothan HA, Zulqarnain M, Ammar YA, Tan EC, Rahman NA, Yusof R

Trop Biomed, 2014 Jun;31(2):286-96.
PMID: 25134897 MyJurnal

Dengue virus infects millions of people worldwide and there is no vaccine or anti-dengue therapeutic available. Screening large numbers of medicinal plants for anti-dengue activities is an alternative strategy in order to find the potent therapeutic compounds. Therefore, this study was designed to identify anti-dengue activities in nineteen medicinal plant extracts that are used in traditional medicine. Local medicinal plants Vernonia cinerea, Hemigraphis reptans, Hedyotis auricularia, Laurentia longiflora, Tridax procumbers and Senna angustifolia were used in this study. The highest inhibitory activates against dengue NS2B-NS3pro was observed in ethanolic extract of S. angustifolia leaves, methanolic extract of V. cinerea leaves and ethanol extract of T. procumbens stems. These findings were further verified by in vitro viral inhibition assay. Methanolic extract of V. cinerea leaves, ethanol extract of T. procumbens stems and at less extent ethanolic extract of S. angustifolia leaves were able to maintain the normal morphology of DENV2-infected Vero cells without causing much cytopathic effects (CPE). The percentage of viral inhibition of V. cinerea and T. procumbens extracts were significantly higher than S. angustifolia extract as measured by plaque formation assay and RT-qPCR. In conclusion, The outcome of this study showed that the methanolic extract of V. cinerea leaves and ethanol extract of T. procumbens stems possessed high inhibitory activates against dengue virus that worth more investigation.

Matched MeSH terms: Plants, Medicinal/chemistry*
Bronchodilator effects of Lignosus rhinocerotis extract on rat isolated airways is linked to the blockage of calcium entry

Lee MK, Lim KH, Millns P, Mohankumar SK, Ng ST, Tan CS, et al.

Phytomedicine, 2018 Mar 15;42:172-179.
PMID: 29655683 DOI: 10.1016/j.phymed.2018.03.025

BACKGROUND: Lignosus rhinocerotis (Cooke) Ryvarden is a popular medicinal mushroom used for centuries in Southeast Asia to treat asthma and chronic cough. The present study aimed to investigate the effect of this mushroom on airways patency.
MATERIALS AND METHODS: The composition of L. rhinocerotis TM02 cultivar was analyzed. Organ bath experiment was employed to study the bronchodilator effect of Lignosus rhinocerotis cold water extract (CWE) on rat isolated airways. Trachea and bronchus were removed from male Sprague-Dawley rats, cut into rings of 2 mm, pre-contracted with carbachol before adding CWE into the bath in increasing concentrations. To investigate the influence of incubation time, tissues were exposed to intervals of 5, 15 and 30 min between CWE concentrations after pre-contraction with carbachol in subsequent protocol. Next, tissues were pre-incubated with CWE before the addition of different contractile agents, carbachol and 5-hydroxytrptamine (5-HT). The bronchodilator effect of CWE was compared with salmeterol and ipratropium. In order to uncover the mechanism of action of CWE, the role of beta-adrenoceptor, potassium and calcium channels was investigated.
RESULTS: Composition analysis of TM02 cultivar revealed the presence of β-glucans and derivatives of adenosine. The extract fully relaxed the trachea at 3.75 mg/ml (p 

Matched MeSH terms: Plants, Medicinal/chemistry
Polyphenolic profiling of Ipomoea carnea Jacq. by HPLC-DAD and its implications in oxidative stress and cancer

Khan MZI, Zahra SS, Ahmed M, Fatima H, Mirza B, Haq IU, et al.

Nat Prod Res, 2019 Jul;33(14):2099-2104.
PMID: 29873254 DOI: 10.1080/14786419.2018.1482551

Ipomoea carnea Jacq. is an important folklore medicinal plant, assessed for its underexplored biological potential. Antioxidant, cytotoxic, antiproliferative and polyphenolic profile of whole plant was evaluated using various techniques. Maximum extract recovery (29% w/w), phenolic [13.54 ± 0.27 μg GAE/mg dry weight (DW)] and flavonoid (2.11 ± 0.10 μg QE /mg DW) content were recorded in methanol-distilled water (1:1) flower extract. HPLC-DAD analysis quantified substantial amount of six different polyphenols ranging from 0.081 to 37.95 μg/mg extract. Maximum total antioxidant and reducing potential were documented in methanol-distilled water and acetone-distilled water flower extracts (42.62 ± 0.47 and 24.38 ± 0.39 μg AAE/mg DW) respectively. Ethanol-chloroform root extract manifested highest free radical scavenging (IC50 of 61.22 μg/mL) while 94.64% of the extracts showed cytotoxicity against brine shrimps. Ethanol leaf extract exhibited remarkable activity against THP-1 cell line (IC50 = 8 ± 0.05 μg/mL) and protein kinases (31 mm phenotype bald zone).

Matched MeSH terms: Plants, Medicinal/chemistry
Fulltext Anti-angiogenic activity of Middle East medicinal plants of the Lamiaceae family

Abdallah Q, Al-Deeb I, Bader A, Hamam F, Saleh K, Abdulmajid A

Mol Med Rep, 2018 Aug;18(2):2441-2448.
PMID: 29901194 DOI: 10.3892/mmr.2018.9155

Angiogenesis plays a crucial role in malignant tumor progression and development. The present study aimed to identify lead plants with selective anti-angiogenic properties. A total of 26 methanolic extracts obtained from 18 plants growing in Saudi Arabia and Jordan that belong to the Lamiaceae family were screened for their cytotoxic and anti-angiogenic activities using MTT and rat aortic ring assays, respectively. Four novel extracts of Thymbra capitata (L.) Cav., Phlomis viscosa Poir, Salvia samuelssonii Rech.f., and Premna resinosa (Hochst.) Schauer were identified for their selective anti-angiogenic effects. These extracts did not exhibit cytotoxic effects on human endothelial cells (EA.hy926) indicating the involvement of indirect anti-angiogenic mechanisms. The active extracts are potential candidates for further phytochemical and mechanistic studies.

Matched MeSH terms: Plants, Medicinal/chemistry
Novel effect and the mechanistic insights of fruiting body extract of medicinal fungus Antrodia cinnamomea against T47D breast cancer

Shang KM, Su TH, Lee WL, Hsiao WW, Chiou CY, Ho BY, et al.

Phytomedicine, 2017 Jan 15;24:39-48.
PMID: 28160860 DOI: 10.1016/j.phymed.2016.11.006

INTRODUCTION: Tamoxifen, an anti-oestrogenic drug for estrogen receptor positive (ER+) breast cancer, was observed to stimulate tumor growth or drug resistance in patients. Antrodia cinnamomea (AC), a precious medicinal fungus has been traditionally used as a folk remedy for cancers in Asian countries. The objective of this study was to investigate the bioefficacy and the underlying molecular mechanisms of the AC fruiting bodies extracts (AC-3E) against human ER+ T47D breast cancer cells, and compare the effect with that of tamoxifen.
METHODS: Cell proliferation, migration, TUNEL assay, western blotting, time-lapse confocal microscopy analyses, chorioallantoic membrane assay, and a xenograft BALB/c nude mouse system were used in this study. Chemical fingerprinting of AC-3E was established using LC-MS.
RESULTS: AC-3E attenuated T47D breast cancer cell activity by deregulating the PI3K/Akt/mTOR signaling pathway and key cell-cycle mediators, and inducing apoptosis. AC-3E also effectively inhibited tube-like structures of endothelial cells, blood vessel branching and microvessel formation ex vivo and in vivo. Significant preventive and therapeutic effects against T47D mammary tumor growth of AC-3E was observed comparable or superior to tamoxifen treatment in xenograft BALB/c nude mice. Dehydroeburicoic acid (2) was characterized as the main chemical constituent in AC-3E against breast cancer.
CONCLUSION: This study suggests that AC-3E extracts can be employed as a double-barreled approach to treat human ER+ breast cancer by attacking both cancer cells and tumor-associated blood vessel cells.

Matched MeSH terms: Plants, Medicinal/chemistry
Analysis of chemical constituents, antimicrobial and anticancer activities of dichloromethane extracts of Sordariomycetes sp. endophytic fungi isolated from Strobilanthes crispus

Jinfeng EC, Mohamad Rafi MI, Chai Hoon K, Kok Lian H, Yoke Kqueen C

World J Microbiol Biotechnol, 2017 Jan;33(1):5.
PMID: 27844243

Plants are primary source of natural product drugs. However, with every new bioactive molecule reported from a plant source, there follows reports of endangered status or even extinction of a medicinally important plant due to over-harvesting. Hence, the attention turned towards fungi namely the endophytes, which reside within medicinally important plants and thus may have acquired their medicinal properties. Strobilanthes crispus is a traditional medicinal plant which has been used traditionally to treat kidney stones, diabetes, hypertension and cancer as well as having antimicrobial activities. In our efforts to bioprospect for anticancer and antimicrobial metabolites, two fungal endophytes most closely related to the Sordariomycetes sp. showed promising results. Sample (PDA)BL3 showed highest significant antimicrobial activity against 6 bacteria at 200 µg/disc whereas sample (PDA)BL5 has highest significant anticancer activity against all 5 cancer cell lines at concentrations ranging from 30 to 300 μg/ml. As for the gas chromatography coupled with mass spectrometry (GC-MS) results, a total of 20 volatile metabolites identified from sample (PDA)BL3 and 21 volatile metabolites identified from sample (PDA)BL5 having more than 1% abundance. Both GC-MS analysis showed that compound Pyrrolo[1,2-a]pyrazine-1,4-dione, hexahydro-3-(2-methylpropyl) has the highest abundance at 15.10% abundance for sample (PDA)BL3 and 19.00% abundance for sample (PDA)BL5 respectively. In conclusion, these results have shown bio-prospecting potential of endophytic fungi having antimicrobial and anticancer activities as well as its potential secondary metabolites of interest. Therefore, this work has further indicated the medicinal and industrial potential of endophytic fungi.

Matched MeSH terms: Plants, Medicinal/microbiology*
Novel targets of pentacyclic triterpenoids in Staphylococcus aureus: A systematic review

Chung PY

Phytomedicine, 2020 Jul 15;73:152933.
PMID: 31103429 DOI: 10.1016/j.phymed.2019.152933

BACKGROUND: Staphylococcus aureus is an important pathogen both in community-acquired and healthcare-associated infections, and has successfully evolved numerous strategies for resisting the action to practically all antibiotics. Resistance to methicillin is now widely described in the community setting (CMRSA), thus the development of new drugs or alternative therapies is urgently necessary. Plants and their secondary metabolites have been a major alternative source in providing structurally diverse bioactive compounds as potential therapeutic agents for the treatment of bacterial infections. One of the classes of natural secondary metabolites from plants with the most bioactive compounds are the triterpenoids, which comprises structurally diverse organic compounds. In nature, triterpenoids are often found as tetra- or penta-cyclic structures.
AIM: This review highlights the anti-staphylococcal activities of pentacyclic triterpenoids, particularly α-amyrin (AM), betulinic acid (BA) and betulinaldehyde (BE). These compounds are based on a 30-carbon skeleton comprising five six-membered rings (ursanes and lanostanes) or four six-membered rings and one five-membered ring (lupanes and hopanes).
METHODS: Electronic databases such as ScienceDirect, PubMed and Scopus were used to search scientific contributions until March 2018, using relevant keywords. Literature focusing on the antimicrobial and antibiofilms of effects of pentacyclic triterpenoids on S. aureus were identified and summarized.
RESULTS: Pentacyclic triterpenoids can be divided into three representative classes, namely ursane, lupane and oleananes. This class of compounds have been shown to exhibit analgesic, immunomodulatory, anti-inflammatory, anticancer, antioxidant, antifungal and antibacterial activities. In studies of the antimicrobial activities and targets of AM, BA and BE in sensitive and multidrug-resistant S. aureus, these compounds acted synergistically and have different targets from the conventional antibiotics.
CONCLUSION: The inhibitory mechanisms of S. aureus in novel targets and pathways should stimulate further researches to develop AM, BA and BE as therapeutic agents for infections caused by S. aureus. Continued efforts to identify and exploit synergistic combinations by the three compounds and peptidoglycan inhibitors, are also necessary as alternative treatment options for S. aureus infections.

Matched MeSH terms: Plants/metabolism
A New Plant Expression System for Producing Pharmaceutical Proteins

Abd-Aziz N, Tan BC, Rejab NA, Othman RY, Khalid N

Mol Biotechnol, 2020 Apr;62(4):240-251.
PMID: 32108286 DOI: 10.1007/s12033-020-00242-2

In the past decade, interest in the production of recombinant pharmaceutical proteins in plants has tremendously progressed because plants do not harbor mammalian viruses, are economically competitive, easily scalable, and capable of carrying out complex post-translational modifications required for recombinant pharmaceutical proteins. Mucuna bracteata is an essential perennial cover crop species widely planted as an underground cover in oil palm and rubber plantations. As a legume, they have high biomass, thrive in its habitat, and can fix nitrogen. Thus, M. bracteata is a cost-efficient crop that shows ideal characteristics as a platform for mass production of recombinant protein. In this study, we established a new platform for the transient production of a recombinant protein in M. bracteata via vacuum-assisted agro-infiltration. Five-week-old M. bracteata plants were vacuum infiltrated with Agrobacterium tumefaciens harboring a plasmid that encodes for an anti-toxoplasma immunoglobulin (IgG) under different parameters, including trifoliate leaf positional effects, days to harvest post-infiltration, and the Agrobacterium strain used. Our results showed that vacuum infiltration of M. bracteata plant with A. tumefaciens strain GV3101 produced the highest concentration of heterologous protein in its bottom trifoliate leaf at 2 days post-infiltration. The purified anti-toxoplasma IgG was then analyzed using Western blot and ELISA. It was demonstrated that, while structural heterogeneity existed in the purified anti-toxoplasma IgG from M. bracteata, its transient expression level was two-fold higher than the model platform, Nicotiana benthamiana. This study has laid the foundation towards establishing M. bracteata as a potential platform for the production of recombinant pharmaceutical protein.

Matched MeSH terms: Plants, Genetically Modified/genetics
Fulltext Antioxidant, α-Glucosidase, and Nitric Oxide Inhibitory Activities of Six Algerian Traditional Medicinal Plant Extracts and 1H-NMR-Based Metabolomics Study of the Active Extract

Hellal K, Maulidiani M, Ismail IS, Tan CP, Abas F

Molecules, 2020 Mar 10;25(5).
PMID: 32164186 DOI: 10.3390/molecules25051247

Claims of effective therapy against diabetes using plants including Peganum harmala L., Zygophyllum album, Anacyclus valentinus L., Ammodaucus leucotrichus, Lupinus albus, and Marrubium vulgare in Algerian empirical medicine prompted our interest in evaluating their antidiabetic activity by screening their free radical scavenging (DPPH), α-glucosidase, and nitric oxide (NO) inhibitory activities as well as the total phenolic content (TPC). Extracts of the selected plants were prepared using different ratios of ethanol (0, 50, 80, and 100%). In this study, 100%, and 80% ethanol extracts of L. albus were found to be the most potent, in inhibiting α-glucosidase activity with IC50 values of 6.45 and 8.66 μg/mL, respectively. The 100% ethanol extract of A. leucotrichus exhibited the highest free radical scavenging activity with an IC50 value of 26.26 μg/mL. Moreover, the highest TPC of 612.84 μg GAE/mg extract was observed in M. vulgare, extracted with 80% ethanol. Metabolite profiling of the active extract was conducted using 1H-NMR metabolomics. Partial least square analysis (PLS) was used to assess the relationship between the α-glucosidase inhibitory activity of L. albus and the metabolites identified in the extract. Based on the PLS model, isoflavonoids (lupinoisoflavone G, lupisoflavone, lupinoisolone C), amino acids (asparagine and thiamine), and several fatty acids (stearic acid and oleic acid) were identified as metabolites that contributed to the inhibition of α-glucosidase activity. The results of this study have clearly strengthened the traditional claim of the antihyperglycemic effects of L. albus.

Matched MeSH terms: Plants, Medicinal/chemistry*
Anthropometric status and resting metabolic rate in users of the areca nut and smokers of tobacco in rural Sarawak

Strickland SS, Duffield AE

Ann Hum Biol, 1997 Sep-Oct;24(5):453-74.
PMID: 9300122

The areca nut is chewed by many of the world's population, mainly in South and Southeast Asia. Anthropometric data for 458 Sarawaki adults aged over 24 years, measured both in 1990 and in 1996, were examined in relation to use of tobacco and areca nut. Compared to non-smokers, smoking men were significantly taller and slightly (not significantly) thinner in both years, while smoking women were thinner in 1990 and slightly (not significantly) thinner in 1996. In both sexes there was an increase in the mean and range of body mass index (BMI, W/H2) over the 6-year interval. Smoking women showed a significantly smaller increment in BMI after allowing for areca nut use, which was associated with a similar trend, and this finding depended on including areca use in the model. The trend for men was similar. Possible effects of areca use could reflect variation in 'affluence' or conservatism, or appetite suppression. However, resting metabolic rate in 54 men and 70 women aged 24-60 years was associated with areca use. This association appeared to be mediated by the maximum room temperature of the 24 h preceding measurement. In women, a significant curvilinear association of RMR with maximum temperature was found in users of areca nut but not in non-users. In men, RMR was 7% higher (p < 0.05) in users of areca nut than in non-users, after allowing for age, height, weight, the sum of four skinfold thicknesses, and haemoglobin, but the association with maximum temperature was similar in both groups. It is speculated that constituents of areca nut modulate thermoregulatory pathways, resulting in prolonged temperature-dependent and hyperthermic heat production in this population; that males are more responsive to this effect than females; and that by this mechanism, and possibly also through centrally mediated effects on appetite for food, areca use could contribute to long-term variation in energy balance represented by change in BMI.

Matched MeSH terms: Plants, Medicinal*
Strobilanthes crispus attenuates renal carcinogen, iron nitrilotriacetate (Fe-NTA)-mediated oxidative damage of lipids and DNA

Iqbal M, Shah MD, Lie CA, San CK

Mol Cell Biochem, 2010 Aug;341(1-2):271-7.
PMID: 20376534 DOI: 10.1007/s11010-010-0458-x

This study was aimed to evaluate the effect of Strobilanthes crispus extract for possible protection against lipid peroxidation and DNA damage induced by iron nitrilotriacetate (Fe-NTA) and hydrogen peroxide (H(2)O(2)). Fe-NTA is a potent nephrotoxic agent and induces acute and subacute renal proximal tubular necrosis by catalyzing the decomposition of H(2)O(2)-derived production of hydroxyl radicals, which are known to cause lipid peroxidation and DNA damage. Incubation of postmitochondrial supernatant and/or calf thymus DNA with H(2)O(2) (40 mM) in the presence of Fe-NTA (0.1 mM) induces lipid peroxidation and DNA damage to about 2.3-fold and 2.9-fold, respectively, as compared to control (P < 0.05). In lipid peroxidation protection studies, S. crispus treatment showed a dose-dependent inhibition (45-53% inhibition, P < 0.05) of Fe-NTA and H(2)O(2) induced lipid peroxidation. Similarly, in DNA damage protection studies, S. crispus treatment also showed a dose-dependent inhibition (18-30% inhibition, P < 0.05) of DNA damage. In addition, the protection was closely related to the content of phenolic compounds as evident by S. crispus extract showing the value of 124.48 mg/g total phenolics expressed as gallic acid equivalent (GAE, mg/g of extract). From these studies, it is concluded that S. crispus inhibits peroxidation of membrane lipids and DNA damage induced by Fe-NTA and H(2)O(2) and possesses the potential to be used to treat or prevent degenerative diseases where oxidative stress is implicated.

Matched MeSH terms: Plants, Medicinal/chemistry
Efficacy of Contrasperm as a male contraceptive: clinical trials in Malaysian men

Hamid A, Jaffar A

Malays J Reprod Health, 1983 Jan;1(1):75-82.
PMID: 12279893

PIP:
The efficacy of a recently marketed posttesticular male oral contraceptive, Contrasperm, was assessed in a clinical trial involving 32 Malaysian volunteers ages 21-39 years. Contrasperm is claimed to be a pure botanical extract free of toxic chemicals, steroids, and hormones. The drug is believed to cause cells surrounding the sperm in the seminiferous tubules to secrete carbon dioxide, producing a weakly acidic environment that greatly increases the sperms' metabolism and reduces the pH of semen from its normal level of 7.5 to 1.5. The manufacturer claims that this drop in pH decreases motility from 95% to 0%. Semen samples were collected by masturbation from subjects to provide baseline data. 3 days after the initial sperm analysis, subjects were given 1 capsule of Contrasperm containing 10 mcg of the active ingredient. Additional semen analyses were conducted 30 minutes, 6 hours, and 24 hours after ingestion. Sperm count and sperm motility were greatly reduced in most subjects 30 minutes after ingestion. However, 6 subjects had increased sperm counts and 4 subjects demonstrated increased sperm motility, indicating an enhancing effect. At 6 hours after ingestion, 20 subjects had lowered sperm motility and 12 subjects showed normal sperm motility, contradicting the manufacturer's claim that motility is reduced to 0%. Although Contrasperm is claimed to be effective for 6-8 hours after ingestion, its effect wore off in less than 6 hours in 37% of subjects. Both sperm count and sperm motility returned to normal levels 24 hours after ingestion, confirming the reversibility of this drug. Most subjects reported mild side effects such as muscle weakness, blurred vision, dizziness, perspiration, urgency, abnormal muscle tension, and dry throat which persisted longer than 24 hours. Further studies, with proper controls, are needed to assess the reliability and toxicity of this preparation.

Matched MeSH terms: Plants, Medicinal*
Comparative X-ray and conformational analysis of a new crystal of 13α,21-dihydroeurycomanone with eurycomanone from Eurycoma longifolia and their anti-estrogenic activity using the uterotrophic assay

Teh CH, Abdulghani M, Morita H, Shiro M, Hussin AH, Chan KL

Planta Med, 2011 Jan;77(2):128-32.
PMID: 20665368 DOI: 10.1055/s-0030-1250159

13 α,21-Dihydroeurycomanone (1), a known quassinoid of Eurycoma longifolia Jack was recrystallized from chloroform into a novel crystal structure in space group P2 (1). Its X-ray data were compared with those of eurycomanone ( 2). Following intraperioneal injections at similar doses of 2.44 µmol/kg/day for 3 consecutive days, 2 displayed comparable potency with tamoxifen but was more potent than 1 in the anti-estrogenic effect against 17 α-ethynylestradiol (EE)-induced uterotrophy of immature rats.

Matched MeSH terms: Plants, Medicinal/chemistry
Characterisation of an extract and fractions of Azadirachta indica flower on cholesterol lowering property and intestinal motility

Duangjai A, Nuengchamnong N, Lee LH, Goh BH, Saokaew S, Suphrom N

Nat Prod Res, 2019 May;33(10):1491-1494.
PMID: 29258345 DOI: 10.1080/14786419.2017.1416386

Azadirachta indica has long been used in traditional medicine. This study focused on isolation and characterisation of active ingredients in the extract, its fractions (NF-EA, NF-AQ, NF-G) and its effect on the cholesterol absorption activity. The NF-EA fraction was identified by marker compounds by LC-ESI-QTOF/MS. Cholesterol absorption activity was performed by measuring the solubility and size of cholesterol micelles. The intestinal motility was also examined by isolated rat's ileum to test the contraction. The extract and its fractions consist of flavonoids and phenolic compounds, like quercetin, kaempferol and myricetin. We found that A. indica extract and NF-EA increase cholesterol micelles size, while the extract, NF-AQ, myricetin and quercetin, reduced the solubility of cholesterol in micelles. The extract and quercetin inhibited the contraction induced by KCl up to 29 and 18%, respectively, and also decreased CaCl2-induced contraction. This finding is in support to traditional uses of A. indica as cholesterol-lowering agents and regulator of gastrointestinal motility.

Matched MeSH terms: Plants, Medicinal/chemistry
Chemical constituents and medical benefits of Plantago major

Adom MB, Taher M, Mutalabisin MF, Amri MS, Abdul Kudos MB, Wan Sulaiman MWA, et al.

Biomed Pharmacother, 2017 Dec;96:348-360.
PMID: 29028587 DOI: 10.1016/j.biopha.2017.09.152

The medicinal benefits of Plantago major have been acknowledged around the world for hundreds of years. This plant contains a number of effective chemical constituents including flavonoids, alkaloids, terpenoids, phenolic acid derivatives, iridoid glycosides, fatty acids, polysaccharides and vitamins which contribute to its exerting specific therapeutic effects. Correspondingly, studies have found that Plantago major is effective as a wound healer, as well as an antiulcerative, antidiabetic, antidiarrhoeal, anti-inflammatory, antinociceptive, antibacterial, and antiviral agent. It also combats fatigue and cancer, is an antioxidant and a free radical scavenger. This paper provides a review of the medicinal benefits and chemical constituents of Plantago major published in journals from year 1937 to 2015 which are available from PubMed, ScienceDirect and Google Scholar.

Matched MeSH terms: Plants, Medicinal/chemistry*
Evaluation of Herb-Drug Interaction of Synacinn™ and Individual Biomarker through Cytochrome 450 Inhibition Assay

Ab Rahman NS, Abd Majid FA, Abd Wahid ME, Zainudin AN, Zainol SN, Ismail HF, et al.

Drug Metab Lett, 2018;12(1):62-67.
PMID: 29542427 DOI: 10.2174/1872312812666180314112457

BACKGROUND: SynacinnTM contains five standardized herbal extracts of Orthosiphon Stamineus (OS), Syzygium polyanthum (SZ), Curcuma xantorrizza (CX), Cinnamomum zeylanicum (CZ) and Andrographis paniculata (AP) and is standardized against phytochemical markers of rosmarinic acid, gallic acid, curcumin, catechin and andrographolide respectively. This herbal medicine has been used as health supplement for diabetes. SynacinnTM is recommended to be consumed as supplement to the diabetic drugs. However, herb-drug interaction of SynacinnTM polyherbal with present drugs is unknown.
METHODS: This study was designed to investigate the effect of SynacinnTM and its individual biomarkers on drug metabolizing enzymes (CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP3A4 (Midazolam), CYP3A4 (Testosteron)), to assess its herb-drug interaction potential through cytochrome P450 inhibition assay. This study was conducted using liquid chromatography- tandem mass spectroscopy (LC-MS/MS) using probe substrates using human liver microsomes against CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP3A4 (Midazolam) and CYP3A4 (Testosteron).
RESULTS: Result showed that SynacinnTM at maximum concentration (5000 µg/ml) 100% inhibit CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP3A4 (Midazolam) and CYP3A4 (Testosteron). IC50 values determined were 0.23, 0.60, 0.47, 0.78, 1.23, 0.99, 1.01, and 0.91 mg/ml for CYP 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 3A4 (midazolam) and 3A4 (testosterone), respectively. Meanwhile, all individual biomarkers showed no, less or moderate inhibitory effect towards all the tested CYP450 except for curcumin that showed inhibition of CYP2C8 (91%), CYP2C9 (81%) and CYP2C19 (72%) at 10µM.
CONCLUSION: Curcumin was found to be an active constituent that might contribute to the inhibition of SynacinnTM against CYP2C8, CYP2C9 and CYP2C19. It can be suggested that SynacinnTM can be consumed separately from a drug known to be metabolized by all tested CYP450 enzymes.

Matched MeSH terms: Plants, Medicinal/chemistry*
Bisnicalaterines B and C, atropisomeric bisindole alkaloids from Hunteria zeylanica, showing vasorelaxant activity

Hirasawa Y, Hara M, Nugroho AE, Sugai M, Zaima K, Kawahara N, et al.

J Org Chem, 2010 Jun 18;75(12):4218-23.
PMID: 20469917 DOI: 10.1021/jo1006762

Two new bisindole alkaloids, bisnicalaterines B and C (1 and 2) consisting of an eburnane and a corynanthe type of skeletons, were isolated from the bark of Hunteria zeylanica. Their absolute structures were determined by combination of NMR, CD, and computational methods, and each of them was shown to be in an atropisomeric relationship. Bisnicalaterines B and C (1 and 2) showed potent vasorelaxant activity on isolated rat aorta.

Matched MeSH terms: Plants, Medicinal/chemistry
The stearoyl-acyl-carrier-protein desaturase promoter (Des) from oil palm confers fruit-specific GUS expression in transgenic tomato

Saed Taha R, Ismail I, Zainal Z, Abdullah SN

J Plant Physiol, 2012 Sep 01;169(13):1290-300.
PMID: 22658816 DOI: 10.1016/j.jplph.2012.05.001

The stearoyl-acyl-carrier-protein (ACP) desaturase is a plastid-localized enzyme that catalyzes the conversion of stearoyl-ACP to oleoyl-ACP and plays an important role in the determination of the properties of the majority of cellular glycerolipids. Functional characterization of the fatty acid desaturase genes and their specific promoters is a prerequisite for altering the composition of unsaturated fatty acids of palm oil by genetic engineering. In this paper, the specificity and strength of the oil palm stearoyl-ACP desaturase gene promoter (Des) was evaluated in transgenic tomato plants. Transcriptional fusions between 5' deletions of the Des promoter (Des1-4) and the β-glucuronidase (GUS) reporter gene were generated and their expression analyzed in different tissues of stably transformed tomato plants. Histochemical analysis of the Des promoter deletion series revealed that GUS gene expression was confined to the tomato fruits. No expression was detected in vegetative tissues of the transgenic plants. The highest levels of GUS activity was observed in different tissues of ripe red fruits (vascular tissue, septa, endocarp, mesocarp and columella) and in seeds, which harbored the promoter region located between -590 and +10. A comparison of the promoter-deletion constructs showed that the Des4 promoter deletion (314bp) produced a markedly low level of GUS expression in fruits and seeds. Fluorometric analysis of the GUS activity revealed a 4-fold increase in the activity of the full-length Des promoter compared to the CaMV35S promoter. RNA-hybridization analyses provided additional evidence of increased GUS expression in fruits driven by a Des fragment. Taken together, these results demonstrate the potential of the Des promoter as a tool for the genetic engineering of oil palms and other species, including dicots, in improving the quality and nutritional value of the fruits.

Matched MeSH terms: Plants, Genetically Modified/enzymology
Overexpression of monodehydroascorbate reductase from a mangrove plant (AeMDHAR) confers salt tolerance on rice

Sultana S, Khew CY, Morshed MM, Namasivayam P, Napis S, Ho CL

J Plant Physiol, 2012 Feb 15;169(3):311-8.
PMID: 22024734 DOI: 10.1016/j.jplph.2011.09.004

Monodehydroascorbate reductase (MDHAR), an important enzyme of the ascorbate-glutathione cycle, is involved in salt tolerance of plants through scavenging of reactive oxygen species (ROS). In this study, a cDNA encoding MDHAR from the mangrove plant Acanthus ebracteatus was introduced into rice to examine its role in salt tolerance. Three stable transgenic lines (MT22, MT24 and MT25) overexpressing AeMDHAR were selected in vitro using hygromycin and confirmed by PCR, quantitative reverse-transcription (qRT) PCR and enzyme assay. The transgenic line MT24 was predicted to possess a single copy of the transgene while the other two transgenic lines were predicted to have multiple transgene integrations. The AeMDHAR transcripts were detected only in transgenic rice lines but not in untransformed rice. The abundance of AeMDHAR transcripts in transgenic lines MT22 and MT25 was approximately 2.75 times the amount found in MT24. The transgenic rice lines overexpressing AeMDHAR showed a significant increase in MDHAR enzyme activity compared to untransformed plants under both NaCl and control conditions. All transgenic lines showed better yield attributes such as a higher tiller number and increased 1000-grain weight compared to non-transgenics. They also showed tolerance to salt at germination and seedling stages. The transgenic line MT24, which harbors a single copy of AeMDHAR, displayed a lower rate of sterility, a higher number of tillers and longer panicle compared to untransformed plants when subjected to salt stress.

Matched MeSH terms: Plants, Genetically Modified/genetics*

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