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Pharmacological, phytochemical and in-vivo toxicological perspectives of a xero-halophyte medicinal plant: Zaleya pentandra (L.) Jeffrey

Saleem H, Zengin G, Locatelli M, Ahmad I, Khaliq S, Mahomoodally MF, et al.

Food Chem Toxicol, 2019 Sep;131:110535.
PMID: 31154083 DOI: 10.1016/j.fct.2019.05.043

This study endeavours to investigate the phytochemical composition, biological properties and in vivo toxicity of methanol and dichloromethane extracts of Zaleya pentandra (L.) Jeffrey. Total bioactive contents, antioxidant (phosphomolybdenum and metal chelating, DPPH, ABTS, FRAP and CUPRAC) and enzyme inhibition (cholinesterases, tyrosinase α-amylase, and α-glucosidase) potential were assessed utilizing in vitro bioassays. UHPLC-MS phytochemical profiling was carried out to identify the essential compounds. The methanol extract was found to contain highest phenolic (22.60 mg GAE/g) and flavonoid (31.49 mg QE/g) contents which correlate with its most significant radical scavenging, reducing potential and tyrosinase inhibition. The dichloromethane extract was most potent for phosphomolybdenum, ferrous chelation, α-amylase, α-glucosidase, and cholinesterase inhibition assays. UHPLC-MS analysis of methanol extract unveiled to identify 11 secondary metabolites belonging to five sub-groups, i.e., phenolic, alkaloid, carbohydrate, terpenoid, and fatty acid derivatives. Additionally, in vivo toxicity was conducted for 21 days and the methanol extract at different doses (150, 200, 250 and 300 mg/kg) was administered in experimental chicks divided into five groups each containing five individuals. Different physical, haematological and biochemical parameters along with the absolute and relative weight of visceral body organs were studied. Overall, no toxic effect was noted for the extract at tested doses.

Matched MeSH terms: Plant Extracts/administration & dosage
Formulation strategies for achieving high delivery efficiency of thymoquinone-containing Nigella sativa extract to the colon based on oral alginate microcapsules for treatment of inflammatory bowel disease

Samak YO, Santhanes D, El-Massik MA, Coombes AGA

J Microencapsul, 2019 Mar;36(2):204-214.
PMID: 31164027 DOI: 10.1080/02652048.2019.1620356

Nigella sativa extract (NSE) was incorporated in alginate microcapsules using aerosolisation and homogenisation methods, respectively, with the aim of delivering high concentrations of the active species, thymoquinone (TQ), directly to sites of inflammation in the colon following oral administration. Encapsulation of NSE was accomplished either by direct loading or diffusion into blank microparticles. Microcapsules in the size range 40-60 µm exhibited significantly higher NSE loading up to 42% w/w and encapsulation efficiency (EE) up to 63% when the extract was entrapped by direct encapsulation compared with 4.1 w/w loading, 6.2% EE when NSE was incorporated by diffusion loading. Sequential exposure of samples to simulated intestinal fluids (SIFs) revealed that the microcapsules suppressed NSE release in simulated gastric fluid (SGF) for 2 h and SIF for 4 h and liberated most of the NSE content (80%) in simulated colonic fluid (SCF) over 18 h. NSE released in SCF at 12 h exhibited antioxidant activity, when measured using the 1,1-diphenyl-2-picryl-hydrazyl (DPPH) assay at levels comparable with the activity of unencapsulated extract. These findings demonstrate the potential of oral alginate microcapsules as highly efficient, targeted carriers for colonic delivery of NSE in the treatment of inflammatory bowel disease.

Matched MeSH terms: Plant Extracts/administration & dosage*
Hibiscus vitifolius (Linn.) root extracts shows potent protective action against anti-tubercular drug induced hepatotoxicity

Samuel AJ, Mohan S, Chellappan DK, Kalusalingam A, Ariamuthu S

J Ethnopharmacol, 2012 May 7;141(1):396-402.
PMID: 22421378 DOI: 10.1016/j.jep.2012.02.051

The roots of Hibiscus vitifolius Linn. (Malvaceae) is used for the treatment of jaundice in the folklore system of medicine in India. This study is an attempt to evaluate the hepatoprotective activity of the roots of Hibiscus vitifolius against anti-tubercular drug induced hepatotoxicity.

Matched MeSH terms: Plant Extracts/administration & dosage
Fungicidal effect and oral acute toxicity of Cassia spectabilis leaf extract

Sangetha S, Zuraini Z, Sasidharan S, Suryani S

Nihon Ishinkin Gakkai Zasshi, 2008;49(4):299-304.
PMID: 19001757

The fungicidal activity of Cassia spectabilis leaf extracts was investigated using the disk diffusion technique and the broth dilution method. The extract showed a favorable antimicrobial activity against Candida albicans with a minimum inhibition concentration(MIC) value of 6.25 mg / ml. Apart from the fungicidal effects, imaging using scanning electron microscopy (SEM) was done to determine the major alterations in the microstructure of the C. albicans. The main abnormalities noted in the SEM studies were the alterations in morphology and complete collapse of the yeast cells after 36 h of exposure to the extract. The in vitro time-kill study performed using the leaf extract at 1/2, 1 or 2 times of the MIC significantly inhibited the yeast growth with a noticeable drop in optical density (OD) of yeast culture, thus confirming the fungicidal effect of the extract on C. albicans. In addition, in vivo antifungal activity studies on candidiasis in mice showed a 5-fold decrease in Candida in kidneys and blood samples in the groups of animals treated with the extract (2.5 g / kg body weight). In an acute toxicity study using mice, the acute minimum fatal dose of the extract was greater than 2000 mg / kg, and we found no histopathological changes in macroscopic examination by necropsy of mice treated with extract. We conclude that the extract may be safely used as an anticandidal agent.

Matched MeSH terms: Plant Extracts/administration & dosage
Fulltext Bioactive Constituents of Zanthoxylum rhetsa Bark and Its Cytotoxic Potential against B16-F10 Melanoma Cancer and Normal Human Dermal Fibroblast (HDF) Cell Lines

Santhanam RK, Ahmad S, Abas F, Safinar Ismail I, Rukayadi Y, Tayyab Akhtar M, et al.

Molecules, 2016 May 24;21(6).
PMID: 27231889 DOI: 10.3390/molecules21060652

Zanthoxylum rhetsa is an aromatic tree, known vernacularly as "Indian Prickly Ash". It has been predominantly used by Indian tribes for the treatment of many infirmities like diabetes, inflammation, rheumatism, toothache and diarrhea. In this study, we identified major volatile constituents present in different solvent fractions of Z. rhetsa bark using GC-MS analysis and isolated two tetrahydrofuran lignans (yangambin and kobusin), a berberine alkaloid (columbamine) and a triterpenoid (lupeol) from the bioactive chloroform fraction. The solvent fractions and purified compounds were tested for their cytotoxic potential against human dermal fibroblasts (HDF) and mouse melanoma (B16-F10) cells, using the MTT assay. All the solvent fractions and purified compounds were found to be non-cytotoxic to HDF cells. However, the chloroform fraction and kobusin exhibited cytotoxic effect against B16-F10 melanoma cells. The presence of bioactive lignans and alkaloids were suggested to be responsible for the cytotoxic property of Z. rhetsa bark against B16-F10 cells.

Matched MeSH terms: Plant Extracts/administration & dosage*
Fulltext Reversal of ampicillin resistance in MRSA via inhibition of penicillin-binding protein 2a by Acalypha wilkesiana

Santiago C, Pang EL, Lim KH, Loh HS, Ting KN

Biomed Res Int, 2014;2014:965348.
PMID: 25101303 DOI: 10.1155/2014/965348

The inhibitory activity of a semipure fraction from the plant, Acalypha wilkesiana assigned as 9EA-FC-B, alone and in combination with ampicillin, was studied against methicillin-resistant Staphylococcus aureus (MRSA). In addition, effects of the combination treatment on PBP2a expression were investigated. Microdilution assay was used to determine the minimal inhibitory concentrations (MIC). Synergistic effects of 9EA-FC-B with ampicillin were determined using the fractional inhibitory concentration (FIC) index and kinetic growth curve assay. Western blot experiments were carried out to study the PBP2a expression in treated MRSA cultures. The results showed a synergistic effect between ampicillin and 9EA-FC-B treatment with the lowest FIC index of 0.19 (synergism ≤ 0.5). The presence of 9EA-FC-B reduced the MIC of ampicillin from 50 to 1.56 μg mL(-1). When ampicillin and 9EA-FC-B were combined at subinhibitory level, the kinetic growth curves were suppressed. The antibacterial effect of 9EA-FC-B and ampicillin was shown to be synergistic. The synergism is due the ability of 9EA-FC-B to suppress the activity of PBP2a, thus restoring the susceptibility of MRSA to ampicillin. Corilagin was postulated to be the constituent responsible for the synergistic activity showed by 9EA-FC-B.

Matched MeSH terms: Plant Extracts/administration & dosage*
Fulltext Anthelmintic activity of papaya seeds on Hymenolepis diminuta infections in rats

Sapaat A, Satrija F, Mahsol HH, Ahmad AH

Trop Biomed, 2012 Dec;29(4):508-12.
PMID: 23202594

The purpose of this study is to see the anthelmintic activity potential of papaya seeds against Hymenolepis diminuta in rats. The objectives of this study were: (1) to determine the effectiveness of papaya seeds on helminths especially H. diminuta in rats and (2) to determine the effective dose level on helminths in rats. Thirty six male rats from strain Sprague-Dawley were chosen as samples in this experiment. Two types of dose level were used for papaya seeds treatments such as 0.6 g kg-1 and 1.2 g kg-1. The geometric mean (GEM) was used to calculate mean for eggs per gram (EPG) before and after the treatment to be included in the reduction percentage calculation. After 21 days post treatment, necropsies were done to get the worm count and the GEM was used to calculate the efficacy percentage for the treatment. Results from this study showed that the reduction percentages in EPG for papaya seeds treatment for both doses level were very high which is 96.8% for 0.6g kg-1 dose level and 96.2% for 1.2 g kg-1 dose level. Whereas the efficacy percentage based on the worm counts for both doses level were also very high that was 90.77% for 0.6 g kg-1 dose level and 93.85% for 1.2 g kg-1.

Matched MeSH terms: Plant Extracts/administration & dosage*
Hypoglycemic effects of cocoa (Theobroma cacao L.) autolysates

Sarmadi B, Aminuddin F, Hamid M, Saari N, Abdul-Hamid A, Ismail A

Food Chem, 2012 Sep 15;134(2):905-11.
PMID: 23107706 DOI: 10.1016/j.foodchem.2012.02.202

Fat, alkaloid and polyphenol contents of two clones of cocoa (UIT1 and PBC 140) were removed and the remaining powder was autolyzed at pH 3.5 and 5.2. Based on the results, autolysates of UIT produced at pH 3.5 exhibited the highest ability to inhibit α-amylase activity. However, no α-glucosidase inhibition activity was observed under the conditions specified. Autolysates produced under pH 3.5 caused the highest amount of insulin secretion. In streptozotocin-diabetic rats, all cocoa autolysates significantly decreased blood glucose at 4h. To assure that the results from the assays were not due to the polyphenols of cocoa autolysates qualitative and quantitative tests were applied. According to their results cocoa autolysates were found to be free from polyphenols. Analysis of amino acid composition revealed that cocoa autolysates were abundant in hydrophobic amino acids. It can be suggested that besides other compounds of cocoa, its peptides and amino acids could contribute to its health benefits.

Matched MeSH terms: Plant Extracts/administration & dosage*
Thrombocyte counts in mice after the administration of papaya leaf suspension

Sathasivam K, Ramanathan S, Mansor SM, Haris MR, Wernsdorfer WH

Wien Klin Wochenschr, 2009 Oct;121 Suppl 3:19-22.
PMID: 19915811 DOI: 10.1007/s00508-009-1229-0

Following up a popular use of crude leaf preparations from Carica papaya for the treatment of dengue infections, a suspension of powdered Carica papaya leaves in palm oil has been investigated for its effect on thrombocyte counts in mice, administering by gavage 15 mg of powdered leaves per kg body weight to 5 mice. Equal numbers of animals received corresponding volumes of either palm oil alone or physiological saline solution. Thrombocyte counts before and at 1, 2, 4, 8, 10, 12, 24, 48 and 72 hours after dosing revealed significantly higher mean counts at 1, 2, 4, 8, 10 and 12 after dosing with the C. papaya leaf formulation as compared to the mean count at hour 0. There was only a non-significant rise of thrombocyte counts in the group having received saline solution, possibly the expression of a normal circadian rhythm in mice. The group having received palm oil only showed a protracted increase of platelet counts that was significant at hours 8 and 48 and obviously the result of a hitherto unknown stimulation of thrombocyte release. The results call for a dose-response investigation and for extending the studies to the isolation and identification of the C. papaya substances responsible for the release and/or production of thrombocytes.

Matched MeSH terms: Plant Extracts/administration & dosage*
Anti-inflammatory and antioxidant activities of the methanol extract of Gynura segetum leaf

Seow LJ, Beh HK, Umar MI, Sadikun A, Asmawi MZ

Int Immunopharmacol, 2014 Nov;23(1):186-91.
PMID: 25194675 DOI: 10.1016/j.intimp.2014.08.020

Gynura segetum, family Compositae, is a cultivated species and can be found growing in the tropical regions of Indonesia and Malaysia. The plant is known for its use for the treatment of cancer, inflammation, diabetes, hypertension and skin afflictions. In the current study, in vivo anti-inflammatory effect of the methanol extract G. segetum leaf and its antioxidant effect in vitro have been investigated for the first time. The in vitro antioxidant activities of the methanol extract were measured using common methods including total phenolic content; total flavonoid content; scavenging of 1,1-diphenyl-2-picrylhydrazyl (DPPH) and β-carotene bleaching assays. The in vivo anti-inflammatory activities were tested using the cotton pellet implanted animal model. The measurement of pro-inflammatory cytokine (TNF-α and IL-1) levels in the blood samples of the rats was carried out by using ELISA kits. The inhibitory activity on cyclooxygenase (COX) enzyme of methanol extract was also evaluated. The methanol extract exhibited good antioxidant activity which is associated with their total phenolic and flavonoid contents. Methanol extract strongly inhibited the granuloma tissue formation in rats and the anti-inflammatory potential was mediated through the inhibition of pro-inflammatory cytokines and COX-2 enzyme activities. Taken together, the present study suggests that G. segetum's leaf is a natural source of antioxidants and has potential therapeutic benefits against chronic inflammation.

Matched MeSH terms: Plant Extracts/administration & dosage*
Fulltext Genotoxicity, acute and subchronic toxicity studies of nano liposomes of Orthosiphon stamineus ethanolic extract in Sprague Dawley rats

Shafaei A, Esmailli K, Farsi E, Aisha AF, Abul Majid AM, Ismail Z

BMC Complement Altern Med, 2015;15:360.
PMID: 26467526 DOI: 10.1186/s12906-015-0885-z

Orthosiphon stamineus (OS) Benth is a medicinal plant and native in Southeast Asia. Pharmacological effects of OS are attributed to the presence of lipophilic flavones. However; lipophilic compounds suffer from poor aqueous solubility which limits the OS oral bioavailability and therapeutic applications. Therefore, OS was prepared in nano formulation form using liposomes from soybean phospholipids. The aim of the present study is to evaluate the in vitro genotoxicity and in vivo oral toxicity of nano liposomes of OS ethanolic extract (OS-EL).

Matched MeSH terms: Plant Extracts/administration & dosage
Therapeutic potential of Moringa oleifera extracts against acetaminophen-induced hepatotoxicity in rats

Sharifudin SA, Fakurazi S, Hidayat MT, Hairuszah I, Moklas MA, Arulselvan P

Pharm Biol, 2013 Mar;51(3):279-88.
PMID: 23043505 DOI: 10.3109/13880209.2012.720993

Moringa oleifera Lam. (Moringaceae) is a rich source of essential minerals and antioxidants; it has been used in human and animal nutrition. The leaves and flowers are being used by the population with great dietary importance.

Matched MeSH terms: Plant Extracts/administration & dosage
Effect of Centella asiatica L (Umbelliferae) on normal and dexamethasone-suppressed wound healing in Wistar Albino rats

Shetty BS, Udupa SL, Udupa AL, Somayaji SN

Int J Low Extrem Wounds, 2006 Sep;5(3):137-43.
PMID: 16928669

Centella asiatica is a reputed medicinal plant used in the treatment of various skin diseases in the Indian system of medicine. The objective of the study presented in this article was to evaluate the wound-healing potential of the ethanolic extract of the plant in both normal and dexamethasone-suppressed wound healing. The study was done on Wistar albino rats using incision, excision, and dead space wounds models. The extract of C asiatica significantly increased the wound breaking strength in incision wound model compared to controls (P < .001). The extract-treated wounds were found to epithelize faster, and the rate of wound contraction was significantly increased as compared to control wounds (P < .001). Wet and dry granulation tissue weights, granulation tissue breaking strength, and hydroxyproline content in a dead space wound model also increased at statistically significant levels as shown. The extract of the leaves had the effect of attenuating the known effects of dexamethasone healing in all wound models (P < .001, P < .05). The results indicated that the leaf extract promotes wound healing significantly and is able to overcome the wound-healing suppressing action of dexamethasone in a rat model. These observations were supported by histology findings.

Matched MeSH terms: Plant Extracts/administration & dosage*
Fulltext Eurycoma longifolia upregulates osteoprotegerin gene expression in androgen- deficient osteoporosis rat model

Shuid AN, El-arabi E, Effendy NM, Razak HS, Muhammad N, Mohamed N, et al.

BMC Complement Altern Med, 2012;12:152.
PMID: 22967165 DOI: 10.1186/1472-6882-12-152

Eurycoma longifolia (EL) has been shown recently to protect against bone calcium loss in orchidectomised rats, the model for androgen-deficient osteoporosis. The mechanism behind this is unclear but it may be related to its ability to elevate testosterone levels or it may directly affect bone remodeling. The aim of this study is to determine the mechanism involved by investigating the effects of EL extract on serum testosterone levels, bone biomarkers, biomechanical strength and gene expression of Receptor Activator of Nuclear Factor kappa-B ligand (RANKL), Osteoprotegerin (OPG) and Macrophage-Colony Stimulating Factor (MCSF) in orchidectomised rats.

Matched MeSH terms: Plant Extracts/administration & dosage*
Assessment of gonadotropins and testosterone hormone levels in regular Mitragyna speciosa (Korth.) users

Singh D, Murugaiyah V, Hamid SBS, Kasinather V, Chan MSA, Ho ETW, et al.

J Ethnopharmacol, 2018 Jul 15;221:30-36.
PMID: 29626673 DOI: 10.1016/j.jep.2018.04.005

ETHNOPHARMACOLOGICAL RELEVANCE: Mitragyna speciosa (Korth.) also known as kratom, is a native medicinal plant of Southeast Asia with opioid-like effects. Kratom tea/juice have been traditionally used as a folk remedy and for controlling opiate withdrawal in Malaysia. Long-term opioid use is associated with depletion in testosterone levels.
AIM OF THE STUDY: Since kratom is reported to deform sperm morphology and reduce sperm motility, we aimed to clinically investigate the testosterone levels following long-term kratom tea/juice use in regular kratom users.
METHODS: A total of 19 regular kratom users were recruited for this cross-sectional study. A full-blood test was conducted including determination of testosterone level, follicle stimulating hormone (FSH) and luteinizing hormone (LH) profile, as well as hematological and biochemical parameters of participants.
RESULTS: We found long-term kratom tea/juice consumption with a daily mitragynine dose of 76.23-94.15 mg did not impair testosterone levels, or gonadotrophins, hematological and biochemical parameters in regular kratom users.
CONCLUSION: Regular kratom tea/juice consumption over prolonged periods (>2 years) was not associated with testosterone impairing effects in humans.

Matched MeSH terms: Plant Extracts/administration & dosage*
Severity of Kratom (Mitragyna speciosa Korth.) Psychological Withdrawal Symptoms

Singh D, Narayanan S, Müller CP, Swogger MT, Rahim AA, Leong Bin Abdullah MFI, et al.

J Psychoactive Drugs, 2018 08 28;50(5):445-450.
PMID: 30152738 DOI: 10.1080/02791072.2018.1511879

Kratom leaves (Mitragyna speciosa Korth.) are traditionally used in Southeast Asia for their medicinal value. Self-report studies suggest that cessation from chronic kratom tea consumption (freshly brewed kratom tea) was associated with unpleasant psychological symptoms. This study sought to assess the severity of anxiety and depression during kratom cessation. Regular kratom users (N = 150) were recruited from the northern state of Penang (Malaysia) for this retrospective study. The Beck Depression Inventory (BDI) and Beck Anxiety Inventory (BAI) scales were used to assess the severity of the symptoms of anxiety and depression. Most respondents (70%) experienced symptoms of mild anxiety, while 81% experienced symptoms of mild depression during kratom cessation. Those who consumed higher quantities of kratom tea daily (≥4 glasses) had higher odds of reporting longer duration of kratom use history (OR = 4.8, 95% CI 2.3 -10.1, p

Matched MeSH terms: Plant Extracts/administration & dosage*
Evaluating the hematological and clinical-chemistry parameters of kratom (Mitragyna speciosa) users in Malaysia

Singh D, Müller CP, Murugaiyah V, Hamid SBS, Vicknasingam BK, Avery B, et al.

J Ethnopharmacol, 2018 Mar 25;214:197-206.
PMID: 29248450 DOI: 10.1016/j.jep.2017.12.017

ETHNOPHARMACOLOGICAL RELEVANCE: Kratom (Mitragyna speciosa Korth.) from the Rubiaceae family is an indigenous tropical medicinal tree of Southeast Asia. Kratom leaves have been used for decades in Malaysia and Thailand in traditional context for its perceived vast medicinal value, and as a mild stimulant among manual labourers. Kratom consumption has been reported to cause side-effects in kratom users.
AIM OF THE STUDY: To evaluate kratom's effects towards hematological and clinical-chemistry parameters among regular kratom users in Malaysia.
METHODS: A total of 77 subjects (n=58 regular kratom users, and n=19 healthy controls) participated in this cross-sectional study. All the surveys were conducted through face-to-face interview to elicit subject's socio-demographic characteristics and kratom use history. A full-blood test was also administered. Laboratory analysis was conducted using GC-MS to determine mitragynine content in the acquired kratom samples in order to relate mitragynine consumption with possible alterations in the blood parameters of kratom users.
RESULTS: Findings showed that there were no significant differences in the hematological and clinical-chemistry parameters of traditional kratom users and healthy controls, except for HDL and LDL cholesterol values; these were found to be above the normal reference range for the former. Similarly, long-term kratom consumption (>5 years), and quantity of daily kratom use (≥3 ½ glasses; mitragynine content 76.3-114.8mg) did not appear to alter the hematological and biochemical parameters of kratom users.
CONCLUSION: These data suggest that even long-term and heavy kratom consumption did not significantly alter the hematological and clinical-chemistry parameters of kratom users in a traditional setting.

Matched MeSH terms: Plant Extracts/administration & dosage*
Severity of Pain and Sleep Problems during Kratom (Mitragyna speciosa Korth.) Cessation among Regular Kratom Users

Singh D, Narayanan S, Vicknasingam BK, Prozialeck WC, Ramanathan S, Zainal H, et al.

J Psychoactive Drugs, 2018 03 20;50(3):266-274.
PMID: 29558272 DOI: 10.1080/02791072.2018.1443234

Kratom (Mitragyna speciosa Korth.) is traditionally used in Southeast Asia for its medicinal value and psychoactive properties. Nonetheless, cessation from regular kratom use is reported to cause unpleasant dose-dependent withdrawal symptoms. This study aims to evaluate the severity of pain and sleep problems following the cessation of kratom tea/juice consumption among regular kratom users. A total of 170 regular users were recruited through snowball sampling for this cross-sectional study. The Brief Pain Inventory (BPI) and Pittsburgh Sleep Quality Index (PSQI) scales were administered to assess the severity of pain and sleep problems. Most participants experienced moderate pain intensity (84%) and moderate pain interference (70%) during kratom cessation; 46% experienced more sleep problems during kratom cessation. Individuals who consumed ≥4 glasses of kratom tea/juice (about 76-115 mg of mitragynine) daily had higher odds of reporting some pain interference (OR: 2.0; CI: 1.04-3.93: p

Matched MeSH terms: Plant Extracts/administration & dosage
Fulltext Lateral Flow Assessment and Unanticipated Toxicity of Kratom

Smith LC, Lin L, Hwang CS, Zhou B, Kubitz DM, Wang H, et al.

Chem Res Toxicol, 2019 01 22;32(1):113-121.
PMID: 30380840 DOI: 10.1021/acs.chemrestox.8b00218

The leaves of the Mitragynine speciosia tree (also known as Kratom) have long been chewed, smoked, or brewed into a tea by people in Southeastern Asian countries, such as Malaysia and Thailand. Just this past year, the plant Kratom gained popularity in the United States as a "legal opioid" and scheduling it as a drug of abuse is currently pending. The primary alkaloid found in Kratom is a μ-opioid receptor agonist, mitragynine, whose structure contains a promising scaffold for immunopharmacological use. Although Kratom is regarded as a safe opioid alternative, here we report the LD50 values determined for its two main psychoactive alkaloids, mitragynine and 7-hydroxymitragynine, as comparable to heroin in mice when administered intravenously. Given Kratom's recent emergence in the U.S., there is currently no diagnostic test available for law enforcement or health professionals, so we sought to design such an assay. Mitragynine was used as a starting point for hapten design, resulting in a hapten with an ether linker extending from the C9 position of the alkaloid. Bacterial flagellin (FliC) was chosen as a carrier protein for active immunization in mice, yielding 32 potential monoclonal antibodies (mAbs) for assay development. Antimitragynine mAbs in the range of micro- to nanomolar affinities were uncovered and their utility in producing a convenient lateral flow detection assay of human fluid samples was examined. Antibodies were screened for binding to mitragynine, 7-hydroxymitragynine, and performance in lateral flow assays. Two monoclonal antibodies were subcloned and further purified with 93 and 362 nM affinity to mitragynine. Test strip assays were optimized with a detection cut off of 0.5 μg/mL for mitragynine in buffer and urine (reflecting projected clinically relevant levels of drug in urine), which could be beneficial to law enforcement agencies and health professionals as the opioid epidemic in America continues to evolve.

Matched MeSH terms: Plant Extracts/administration & dosage
Potential action of Rumex vesicarius (L.) against potassium dichromate and gentamicin induced nephrotoxicity in experimental rats

Subramaniyan V, Shaik S, Bag A, Manavalan G, Chandiran S

Pak J Pharm Sci, 2018 Mar;31(2):509-516.
PMID: 29618442

To determine the ameliorative potential of the active fraction from different extracts of Rumex vesicarius against potassium dichromate and gentamicin induced nephrotoxicity in experimental rats and its possible mechanism of action. Both sex wistar rats were divided into 6 groups (n=6/group) were fed with a control, potassium dichromate and gentamicin supplemented with different extracts at the doses of 200 and 400mg/kg respectively. Oral administration of EERV offered a significant (p<0.01 and p<0.001) dose dependent protection against PD and GN induced nephrotoxicity. Potassium dichromate and gentamicin nephrotoxicity assessed in terms of body weight, kidney weight, creatinine, urea, uric acid, BUN, albumin and total protein. Thus the present study revealed that EERV phytochemical constituents play an important role in protection against kidney damage.

Matched MeSH terms: Plant Extracts/administration & dosage

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