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1.
Nat Prod Rep ; 38(10): 1720-1728, 2021 10 20.
Article in English | MEDLINE | ID: mdl-34676834

ABSTRACT

Covering: up to 2019The large and medicinally important tropical plant genus Plectranthus (Lamiaceae) was recently split into three separate genera on the basis of molecular and morphological evidence; Plectranthus sensu stricto, Coleus and Equilabium. We found striking differences between the diterpenoids which strongly support this taxonomic split. Coleus is characterised by abietanes oxygenated at C-14 such as royleanones, spirocoleons and acylhydroquinones, which could be useful chemotaxonomic markers to distinguish this genus from Plectranthus s.s. In contrast, the abietanes in Plectranthus s.s. lack C-14 oxygenation, but are often acylated with unusual acids. Equilabium species do not seem to produce diterpenoids. The structures of the nearly 240 abietanes so far reported from Coleus and Plectranthus and their distribution are presented. The aim of this Highlight is to provide an overview of the differences in diterpenoid diversity between these newly defined genera, which are relevant to predict which previously understudied species could hold untapped potential for their medicinal and other economic uses, and to underpin future research on how these plants have evolved to synthesise distinct abietane types.


Subject(s)
Coleus/classification , Diterpenes/chemistry , Plectranthus/classification , Abietanes/analysis , Abietanes/chemistry , Coleus/chemistry , Diterpenes/analysis , Plectranthus/chemistry
2.
Molecules ; 26(10)2021 May 14.
Article in English | MEDLINE | ID: mdl-34068950

ABSTRACT

Coleus amboinicus Lour., Lamiaceae, is a perennial herb that is native to Indonesia and also cultivated in Africa, Asia and Australia. The major phytochemicals responsible for its bioactivity are rosmarinic acid (RA) and its analogues, flavonoids and abietane diterpenoids. The possibility of cultivation in a colder climate would extend the use of this herb and provide new opportunities to herb growers and livestock farmers. Our study to compare feed value and phytochemical composition of C. amboinicus plants cultivated in its original region, Indonesia, and in Poland. The crude protein content was significantly higher in plants cultivated in Indonesia compared to those cultivated in Poland-21% and 13% of dry matter, respectively. The higher ADF contents were detected in C. amboinicus cultivated in Indonesia, 38-41%, in comparison to 34% in plants cultivated in Poland. The phytochemical composition was also significantly influenced by the cultivation location. Polish samples were higher in polyphenols (RA and its analogues), and also had 1.5-2-fold higher antioxidant potential, as measured by DPPH scavenging, phosphomolybdenum reduction and Fenton reaction driven lipid peroxidation. The Indonesian samples contained more diterpenoid compounds, such as dihydroxyroyleanone, and the sum of terpenoids was ca. 10 times higher than in samples from Poland (15.59-23.64 vs. 1.87 µg/g of extracts). In conclusion, C. amboinicus is suitable for cultivation in non-optimal climatic conditions but some nutritional properties and bioactivity are significantly affected.


Subject(s)
Antioxidants/pharmacology , Coleus/chemistry , Coleus/growth & development , Phytochemicals/analysis , Animals , Discriminant Analysis , Feeding Behavior , Indonesia , Least-Squares Analysis , Poland , Principal Component Analysis , Sheep
3.
Proc Natl Acad Sci U S A ; 114(13): 3393-3396, 2017 03 28.
Article in English | MEDLINE | ID: mdl-28289201

ABSTRACT

Development of a phenotyping platform capable of noninvasive biochemical sensing could offer researchers, breeders, and producers a tool for precise response detection. In particular, the ability to measure plant stress in vivo responses is becoming increasingly important. In this work, a Raman spectroscopic technique is developed for high-throughput stress phenotyping of plants. We show the early (within 48 h) in vivo detection of plant stress responses. Coleus (Plectranthus scutellarioides) plants were subjected to four common abiotic stress conditions individually: high soil salinity, drought, chilling exposure, and light saturation. Plants were examined poststress induction in vivo, and changes in the concentration levels of the reactive oxygen-scavenging pigments were observed by Raman microscopic and remote spectroscopic systems. The molecular concentration changes were further validated by commonly accepted chemical extraction (destructive) methods. Raman spectroscopy also allows simultaneous interrogation of various pigments in plants. For example, we found a unique negative correlation in concentration levels of anthocyanins and carotenoids, which clearly indicates that plant stress response is fine-tuned to protect against stress-induced damages. This precision spectroscopic technique holds promise for the future development of high-throughput screening for plant phenotyping and the quantification of biologically or commercially relevant molecules, such as antioxidants and pigments.


Subject(s)
Coleus/chemistry , Coleus/physiology , Spectrum Analysis, Raman/methods , Adaptation, Physiological , Droughts , Salinity , Soil/chemistry
4.
J Appl Toxicol ; 33(9): 924-32, 2013 Sep.
Article in English | MEDLINE | ID: mdl-22729658

ABSTRACT

Coleus forskohlii root extract (CFE) represented by its bioactive constituent 'forskolin' is popularly used as a natural weight-lowering product, but the association of its use with liver-related risks is very limited. In the present study, the effect of standardized CFE with 10% forskolin on liver function of mice was examined. Mice were given 0-5% CFE in an AIN93G-based diet for 3-5 weeks. Food intake, body weights, relative organ weights and liver marker enzymes [aspartate aminotransferase (AST), alanine aminotransferase (ALT), and alkaline phosphatase (ALP)] combined with histophatological analysis were assessed. CFE (0-0.5%) only had minimal effects on food intake and body weight whereas a significant difference was observed in mice receiving the highest dose (5% CFE). The extract 0.05-5% dose-dependently decreased visceral fat weight by between 16% and 63%, and a dose-dependent several folds increase was observed in liver weights and plasma AST, ALT and ALP activities with quick onset apparent after only 1 week of 0.5% CFE intake. The hepatic effect persisted throughout the 3-weeks course but was restored towards normalization within 1 week after withdrawal of treatment. Liver histology of mice fed 0.5% CFE for 3 weeks showed hepatocyte hypertrophy and fat deposition. In contrast, none of the hepatic responses measured were altered when mice were given a diet containing pure forskolin alone at the dose corresponding to its content in 0.5% CFE. The present study clearly indicated that forskolin was not involved in the CFE-induced hepatotoxicity and was caused by other unidentified constituents in CFE which warrants further studies.


Subject(s)
Coleus/chemistry , Liver/drug effects , Liver/pathology , Plant Extracts/adverse effects , Alanine Transaminase/blood , Alkaline Phosphatase/blood , Animals , Aspartate Aminotransferases/blood , Biomarkers/blood , Body Weight , Colforsin/adverse effects , Colforsin/toxicity , Diet , Dose-Response Relationship, Drug , Hepatocytes/cytology , Hepatocytes/drug effects , Hepatocytes/metabolism , Male , Mice , Mice, Inbred ICR , Organ Size/drug effects , Plant Extracts/administration & dosage , Plant Roots/chemistry
5.
Parasitol Res ; 112(11): 3713-21, 2013 Nov.
Article in English | MEDLINE | ID: mdl-23933878

ABSTRACT

Diseases transmitted by blood-feeding mosquitoes, such as dengue fever, dengue hemorrhagic fever, Japanese encephalitis, malaria, and filariasis, are increasing in prevalence, particularly in tropical and subtropical zones. To control mosquitoes and mosquito-borne diseases, which have a worldwide health and economic impacts, synthetic insecticide-based interventions are still necessary, particularly in situations of epidemic outbreak and sudden increases of adult mosquitoes. However, the indiscriminate use of conventional insecticides is fostering multifarious problems like widespread development of insecticide resistance, toxic hazards to mammals, undesirable effects on nontarget organisms, and environmental pollution. The aim of this research was to evaluate the toxicity of mosquito larvicidal activity of essential oil from Coleus aromaticus and its pure isolated constituent thymol against larvae of Culex tritaeniorhynchus, Aedes albopictus, and Anopheles subpictus. The chemical composition of the essential oil was analyzed using gas chromatography-mass spectroscopy. A total of 14 components of the essential oil of C. aromaticus were identified. The major chemical components identified were thymol (82.68%), terpinen-4-ol (3.2%), and trans-Caryophyllene (3.18%). Twenty-five early third instar larvae of C. tritaeniorhynchus, A. albopictus, and A. subpictus were exposed and assayed in the laboratory. Thymol and essential oil were tested in concentrations of 10, 20, 30, 40, and 50 and 30, 60, 90, 120, and 150 ppm, respectively. The larval mortality was observed after 24 h of treatment. The thymol had a significant toxic effect against early third-stage larvae of C. tritaeniorhynchus, A. albopictus, and A. subpictus with an LC50 values of 28.19, 24.83, and 22.06 µg/mL respectively, whereas the essential oil of C. aromaticus had an LC50 values of 72.70, 67.98, and 60.31 µg/mL, respectively. No mortality was observed in controls. The Chi-square values were significant at p < 0.05 level. The result indicated that the essential oil of C. aromaticus and the isolated constituent have a potential for use in control of C. tritaeniorhynchus, A. albopictus, and A. subpictus larvae and could be useful in search of newer, safer, and more effective natural compounds as larvicides.


Subject(s)
Aedes/drug effects , Anopheles/drug effects , Coleus/chemistry , Culex/drug effects , Insecticides/pharmacology , Oils, Volatile/pharmacology , Thymol/pharmacology , Animals , Biological Assay , Gas Chromatography-Mass Spectrometry , Insecticides/chemistry , Insecticides/isolation & purification , Larva/drug effects , Oils, Volatile/chemistry , Oils, Volatile/isolation & purification , Survival Analysis , Thymol/chemistry , Thymol/isolation & purification
6.
Biomed Environ Sci ; 26(4): 295-302, 2013 Apr.
Article in English | MEDLINE | ID: mdl-23534470

ABSTRACT

OBJECTIVE: To investigate protective effect of Coleus aromaticus leaf extract against naphthalene induced hepatotoxicity in rats. METHODS: Eighteen male rats were divided into three groups. Group I rats were treated as control. Group II rats were intraperitoneally administered with naphthalene (435 mg/kg b.wt) dissolved in corn oil once a day for a period of 30 days. Group III rats were treated with leaf extract (100 mg/kg b.wt) dissolved in 0.9% saline and naphthalene (435 mg/kg b.wt) dissolved in corn oil once a day for a period of 30 days. RESULTS: Significant protective effect was observed against naphthalene induced liver damage, which appeared evident from the response levels of marker enzymes (aspartate transaminase, alanine transaminase, acid phosphatase, alkaline phosphatase and lactate dehydrogenase). The biochemical components viz. triglycerides, free fatty acids, cholesterol acyl transferase, high-density lipoprotein, low-density lipoprotein, cholesterol and bilirubin were found to be increased in liver and serum of naphthalene stressed rats when compared to control. CONCLUSION: Treatment of naphthalene intoxicated rats with plant extract reversed these distorted parameters to near normal levels. Liver histology showed supportive evidence regarding the protective nature of plant extract against fatty changes induced by naphthalene. The present study provides a scientific rationale for using C. aromaticus in the management of liver disorders.


Subject(s)
Chemical and Drug Induced Liver Injury/prevention & control , Coleus/chemistry , Naphthalenes/toxicity , Phytotherapy , Plant Extracts/therapeutic use , Animals , Chemical and Drug Induced Liver Injury/enzymology , Chemical and Drug Induced Liver Injury/pathology , Drug Evaluation, Preclinical , Free Radical Scavengers/analysis , Liver/drug effects , Liver/enzymology , Liver/pathology , Male , Phenols/analysis , Plant Leaves/chemistry , Plants, Medicinal/chemistry , Rats , Rats, Wistar
7.
Phytochem Anal ; 24(2): 117-23, 2013 Feb.
Article in English | MEDLINE | ID: mdl-22782930

ABSTRACT

INTRODUCTION: The quality of Coleus forskohlii is often evaluated by high performance liquid chromatography (HPLC), using bioactive labdane diterpenoids as chemical markers. However, the existing sample preparation methods for the analysis of diterpenoids in C. forskohlii are generally labour-intensive, time-consuming and require large volumes of solvents. OBJECTIVE: To establish an efficient matrix solid-phase dispersion (MSPD) extraction method for the simultaneous analysis of five bioactive diterpenoids in C. forskohlii by HPLC. METHODOLOGY: Herbal samples were prepared by an optimised MSPD procedure using C(18) as the sorbent. The quantification of the diterpenoids was achieved by HPLC with evaporative light scattering detector (ELSD), and the identification of the five compounds was performed by HPLC with tandem mass detector (MS/MS). The efficiency of the MSPD method was also compared with other extraction techniques including Soxhlet extraction, heat reflux extraction, ultrasonic-assisted extraction and microwave-assisted extraction. RESULTS: The MSPD extracted five diterpenoids with satisfactory recoveries ranging from 98.36% to 102.08%. Compared with other extraction methods, the proposed MSPD method had the advantages of combining extraction and clean-up into a single step, consuming less time and requiring lower solvent volumes. CONCLUSION: The MSPD method is simple, rapid and efficient for the extraction of labdane diterpenoids from C. forskohlii. The MSPD procedure coupled with HPLC-ELSD or HPLC-MS/MS is suitable for the quantification and identification of the diterpenoids in C. forskohlii.


Subject(s)
Chromatography, High Pressure Liquid/methods , Coleus/chemistry , Diterpenes/analysis , Solid Phase Extraction/methods , Diterpenes/isolation & purification , Microwaves , Reproducibility of Results , Tandem Mass Spectrometry/methods , Time Factors
8.
Yao Xue Xue Bao ; 48(3): 383-9, 2013 Mar.
Article in Zh | MEDLINE | ID: mdl-23724652

ABSTRACT

This paper is to report the study of the metabolism of forscolin in plasma and liver microsomes for guiding clinical therapy. Forscolin was quantified by HPLC-MS/MS. The metabolic stability of forscolin in rat, Beagle dog, monkey and human plasma and liver microsomes, mediated enzymes of forscolin and its inhibition on cytochrome P450 isoforms in human liver microsomes were studied. Results showed that forscolin was not metabolized in plasma of the four species but metabolized in liver microsomes of the four species. The t1/2 of forscolin in rat, Beagle dog, monkey and human liver microsomes were (52.0 +/- 15.0), (51.2 +/- 5.9), (6.0 +/- 0.2) and (11.9 +/- 1.8) min; CL(int) were (75.6 +/- 18.7), (60.9 +/- 6.8), (513.8 +/- 14.3) and (176.2 +/- 25.6) mL x min(-1) x kg(-1); CL were (34.8 +/- 4.5), (23.3 +/- 1.0), (40.3 +/- 0.5) and (17.9 +/- 0.3) mL x min(-1) x kg(-1), respectively. Forscolin was metabolized by CYP3A4 in human liver microsomes. There was definite inhibition on CYP3A4 at the concentrations of forscolin between 0.1 ng x mL(-1) and 5 microg x mL(-1). Therefore, forscolin is rapidly excreted from liver microsomes. Attention should be paid to the drug interaction when forscolin was used along with other drugs metabolized by CYP3A4 in clinics.


Subject(s)
Coleus/chemistry , Colforsin/metabolism , Microsomes, Liver/metabolism , Animals , Chromatography, High Pressure Liquid , Colforsin/blood , Colforsin/isolation & purification , Cytochrome P-450 CYP3A/metabolism , Dogs , Humans , Macaca , Metabolic Clearance Rate , Plants, Medicinal/chemistry , Rats , Tandem Mass Spectrometry
9.
Plant Foods Hum Nutr ; 68(3): 213-21, 2013 Sep.
Article in English | MEDLINE | ID: mdl-23666454

ABSTRACT

As obesity has reached epidemic proportions, the management of this global disease is of clinical importance. The availability and popularity of natural dietary supplements for the treatment of obesity has risen dramatically in recent years. The purpose of this paper was to review the effect of commonly available over the counter plant-derived supplements used to suppress appetite for obesity control and management. The data were obtained from the electronic databases PubMed, SpringerLink, Google Scholar, ScienceDirect, and MEDLINE with full text (via EBSCOHost) and the databases were accessed during late 2012 - early January 2013. The botanical species discussed in this review include Camellia sinensis, Caralluma fimbriata, Citrus aurantium, Coleus forskohlii, Garcinia cambogia and Phaseolus vulgaris. This review found that many botanical species including crude extracts and isolated compounds from plants have been shown to provide potentially promising therapeutic effects including appetite control and weight loss. However, many of these crude extracts and compounds need to be further investigated to define the magnitude of the effects, optimal dosage, mechanisms of action, long term safety, and potential side effects.


Subject(s)
Appetite Depressants/administration & dosage , Obesity/drug therapy , Plant Extracts/administration & dosage , Weight Loss , Apocynaceae/chemistry , Appetite/drug effects , Camellia sinensis/chemistry , Citrus/chemistry , Coleus/chemistry , Dietary Supplements , Garcinia cambogia/chemistry , Humans , MEDLINE , Phaseolus/chemistry , Phytotherapy , Plant Extracts/adverse effects
10.
Planta Med ; 78(7): 698-702, 2012 May.
Article in English | MEDLINE | ID: mdl-22411728

ABSTRACT

The intestinal permeability of forskolin was investigated using a single pass intestinal perfusion (SPIP) technique in rats. SPIP was performed in different intestinal segments (duodenum, jejunum, ileum, and colon) with three concentrations of forskolin (11.90, 29.75, and 59.90 µg/mL). The investigations of adsorption and stability were performed to ensure that the disappearance of forskolin from the perfusate was due to intestinal absorption. The results of the SPIP study indicated that forskolin could be absorbed in all segments of the intestine. The effective permeability (P (eff)) of forskolin was in the range of drugs with high intestinal permeability. The P (eff) was highest in the duodenum as compared to other intestinal segments. The decreases of P (eff) in the duodenum and ileum at the highest forskolin concentration suggested a saturable transport process. The addition of verapamil, a P-glycoprotein inhibitor, significantly enhanced the permeability of forskolin across the rat jejunum. The absorbed fraction of dissolved forskolin after oral administration in humans was estimated to be 100 % calculated from rat P (eff). In conclusion, dissolved forskolin can be absorbed readily in the intestine. The low aqueous solubility of forskolin might be a crucial factor for its poor oral bioavailability.


Subject(s)
Coleus/chemistry , Colforsin/administration & dosage , Colforsin/pharmacokinetics , Intestinal Mucosa/metabolism , Plectranthus/chemistry , Administration, Oral , Animals , Biological Availability , Colon/metabolism , Duodenum/metabolism , Humans , Ileum/metabolism , Intestinal Absorption/drug effects , Jejunum/metabolism , Male , Perfusion/methods , Permeability , Phytotherapy , Plant Extracts/administration & dosage , Plant Extracts/pharmacokinetics , Rats , Rats, Sprague-Dawley , Verapamil/pharmacology
11.
J Postgrad Med ; 58(3): 199-202, 2012.
Article in English | MEDLINE | ID: mdl-23023353

ABSTRACT

Forskolin is the first pharmaceutical drug and product derived from a plant to be approved in India by the DCGI in 2006. Forskolin (7beta-acetoxy-8, 13-epoxy-1a, 6ß, 9a-trihydroxy-labd-14-en-11-one) is a diterpenoid isolated from plant Coleus forskohlii (Lamiaceae). It is a lipid-soluble compound that can penetrate cell membranes and stimulates the enzyme adenylate cyclase which, in turn, stimulates ciliary epithelium to activate cyclic adenosine monophosphate, which decreases intraocular pressure (IOP) by reducing aqueous humor inflow. The topical application of forskolin is capable of reducing IOP in rabbits, monkeys, and humans. In its drug interactions, forskolin may act synergistically with epinephrine, ephedrine and pseudoephedrine. Whereas the effects of anti-clotting medications like warfarin, clopidogre, aspirin, anoxaparin, etc., may be enhanced by forskolin. Forskolin is contraindicated in the medications for people with ulcers as forskolin may increase acid level. Forskolin has a very good shelf-life of five years. Recently, its Ophthalmic inserts and in situ gels for sustained and delayed-release drug delivery systems were tested in New Zealand Albino Rabbits for its antiglaucoma efficacy. This drug review explains Forskolin as a drug, its antiglaucoma potential and recent findings of forskolin as an antiglaucoma agent. The literature search method used for this review was different databases and search engines like PubMed, International Pharmaceutical Abstracts, Google, Medicinal and Aromatic Plants (MAPA).


Subject(s)
Coleus/chemistry , Colforsin/pharmacology , Glaucoma/drug therapy , Intraocular Pressure/drug effects , Animals , Drug Interactions , Humans , India , Phytotherapy , Plant Extracts/chemistry , Plant Roots/chemistry , Rabbits
12.
Parasitol Res ; 110(4): 1435-43, 2012 Apr.
Article in English | MEDLINE | ID: mdl-21947308

ABSTRACT

Ethanolic extracts of Cynodon dactylon, Aloe vera, Hemidesmus indicus and Coleus amboinicus were tested for their toxicity effect on the third-instar larvae of Anopheles stephensi, Culex quinquefasciatus and Aedes aegypti. The leaves of C. dactylon, A. vera, H. indicus and C. amboinicus were collected from natural habitats (forests) in Western Ghats, Tamil Nadu, India. A total of 250 g of fresh, mature leaves were rinsed with distilled water and dried in shade. The dried leaves were put in Soxhlet apparatus and extract prepared using 100% ethanol for 72 h at 30-40°C. Dried residues were obtained from 100 g of extract evaporated to dryness in rotary vacuum evaporator. Larvicidal properties of ethanolic leaf extracts showed that the extracts are effective as mosquito control agents. The larval mortality was observed after 24 h exposure. No mortality was observed in the control. The median lethal concentration (LC(50)) values observed for the larvicidal activities are 0.44%, 0.51%, 0.59% and 0.68% for extracts of C. dactylon, A. vera, H. indicus and C. amboinicus, respectively. The observed mortality were statistically significant at P < 0.05 level. C. dactylon showed the highest mortality rate against the three species of mosquito larvae in laboratory and field. The selected plants were shown to exhibit water purification properties. Water quality parameters such as turbidity, pH and water clarity were analyzed in the water samples (pre-treatment and post-treatment of plant extracts) taken from the different breeding sites of mosquitoes. Water colour, turbidity and pH were reduced significantly after treatment with C. dactylon (13 HU, 31.5 mg/l and 6.9), H. indicus (13.8 HU, 33 mg/l and 7.1), A. vera (16 HU, 33.8 mg/l and 7.4) and C. amboinicus (21 HU, 35 mg/l and 7.5) extracts. The study proved that the extracts of C. dactylon, A. vera, H. indicus and C. amboinicus have both mosquitocidal and water sedimentation properties.


Subject(s)
Aloe/chemistry , Coleus/chemistry , Cynodon/chemistry , Hemidesmus/chemistry , Insecticides/chemistry , Plant Extracts/chemistry , Water Purification/methods , Aedes/drug effects , Animals , Anopheles/drug effects , Culex/drug effects , Hydrogen-Ion Concentration , India , Insecticides/analysis , Larva/drug effects , Lethal Dose 50 , Mosquito Control/methods , Plant Extracts/analysis , Plant Leaves/chemistry , Water Quality
13.
J Chromatogr Sci ; 60(10): 916-925, 2022 Dec 13.
Article in English | MEDLINE | ID: mdl-35511495

ABSTRACT

Coleus forskohlii Briq. is an important medicinal herb, endowed with a wide range of medicinal properties against the variety of ailments. Seven germplasm of C. forskohlii collected from different phyto-geographical locations and identification of elite chemotype was performed with the help of high performance thin layer chromatography. Data of soil analysis correlated with the bioactive compounds and inhibitory potential of the species. Quantification of forskolin and its isomer (iso-forskolin) content were done in all the collected samples of C. forskohlii, which revealed a wide range of variations, varying from 1.15-0.004% and 0.0091 to 0.1077% per dry weights basic, respectively. Variation in the bioactive content may be due to the soil nature and environmental factors. Soil analysis of collected samples demonstrated that there is significant variation in available NPK and micronutrient content and may be reasoned for existing chemotypic variability. In vitro biological activity (antioxidant and antidiabetic) analyses were performed, which reveals that germplasms have a high amount of forskolin and iso-forskolin, both show more activity. The aim of this study was to elucidate the effect of elicitors and precursors on the production of bioactive compounds and identification of best elite germplasm among the populations, to provide basic lead to the industry for commercial exploitability including its location-specific commercial cultivation.


Subject(s)
Coleus , Plectranthus , Coleus/chemistry , Colforsin/analysis , Colforsin/chemistry , Chromatography, Thin Layer , Soil
14.
J Chromatogr A ; 1676: 463198, 2022 Aug 02.
Article in English | MEDLINE | ID: mdl-35704959

ABSTRACT

A new multianalytical methodology based on gas chromatography (GC) and liquid chromatography (LC) coupled to mass spectrometry (MS) has been proposed to evaluate frauds affecting the composition of Coleus forskohlii root supplements (FKS). After optimization and validation of chromatographic methods, 24 FKS were analyzed. Forskolin, their main bioactive component, was only found in 50% of the FKS evaluated (in the 0.032-17.1% range), with 27% of these supplements showing concentrations of this bioactive lower than those declared in their labels. Application of this methodology also proved to be successful for the detection of frauds regarding the replacement of C. forskohlii by other vegetable sources (green tea, soy leaves and a plant of the Berberidaceae family) in 17% of supplements analyzed. A study on stability of forskolin under accelerated conditions allowed to rule out its degradation as responsible for the lack of this bioactive or other natural constituents in 25% of FKS evaluated. It can be concluded that the multianalytical methodology here developed is an advantageous alternative to address the wide diversity of frauds affecting these supplements.


Subject(s)
Coleus , Plectranthus , Coleus/chemistry , Coleus/metabolism , Colforsin/analysis , Colforsin/metabolism , Gas Chromatography-Mass Spectrometry , Plant Roots/chemistry , Plectranthus/metabolism
15.
Zhong Yao Cai ; 34(3): 375-8, 2011 Mar.
Article in Zh | MEDLINE | ID: mdl-21823451

ABSTRACT

OBJECTIVE: To study the chemical constituents of Coleus forskohlii. METHODS: Isolation and purification were carried out by silica gel column chromatographic and Toyopearl HW-40F. Compounds were identified and elucidated by spectral and chemical methods. RESULTS: Seven compounds were obtained from ethyl acetate extract fraction. Their structures were identified as lupeol (1), oleanolic acid (2), uvalo(3), beta-sitosterol (4), colonic acid (5), demethylcryptojaponol (6), coleolic acid (7). Compounds 1, 2, 6, 7 showed obviously antitumor activity. CONCLUSION: Compound 1 and 3 are isolated from the genus for the first time. Moreover, compound 1 is firstly found to have antitumor activity from the plants.


Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Coleus/chemistry , Oleanolic Acid/isolation & purification , Pentacyclic Triterpenes/isolation & purification , Triterpenes/isolation & purification , Antineoplastic Agents, Phytogenic/chemistry , Cell Line, Tumor , Coleus/growth & development , HeLa Cells , Humans , Lactones/chemistry , Lactones/isolation & purification , Lactones/pharmacology , Lethal Dose 50 , Magnetic Resonance Spectroscopy , Molecular Structure , Oleanolic Acid/chemistry , Oleanolic Acid/pharmacology , Pentacyclic Triterpenes/chemistry , Pentacyclic Triterpenes/pharmacology , Plants, Medicinal/chemistry , Plants, Medicinal/growth & development , Triterpenes/chemistry , Triterpenes/pharmacology
16.
Phytomedicine ; 91: 153701, 2021 Oct.
Article in English | MEDLINE | ID: mdl-34438230

ABSTRACT

BACKGROUND: Chronic obstructive pulmonary disease (COPD) is characterized by limited airflow due to pulmonary and alveolar abnormalities from exposure to cigarette smoke (CS). Current therapeutic drugs are limited and the development of novel treatments to prevent disease progression is challenging. Isoforskolin (ISOF) from the plant Coleus forskohlii is an effective activator of adenylyl cyclase (AC) isoforms. Previously we found ISOF could attenuate acute lung injury in animal models, while the effect of ISOF on COPD has not been elucidated. PURPOSE: In this study, we aimed to evaluate the efficacy of ISOF on COPD and reveal its potential mechanisms. METHODS: A rat model of COPD was established by long-term exposure to CS, then the rats were orally administered with ISOF (0.5, 1 and 2 mg/kg). The pulmonary function, lung morphology, inflammatory cells and cytokines in serum or bronchoalveolar lavage fluid (BALF) were evaluated. Transcriptomics, proteomics and network pharmacology analysis were utilized to identify potential mechanisms of ISOF. Droplet digital PCR was used to detect the mRNA expression of AC1-10 in donor lung tissues. AC activation was determined in recombinant human embryonic kidney 293 (HEK293) cells stably expressing human AC isoforms. In addition, ISOF caused trachea relaxation ex vivo were assessed in isolated trachea rings from guinea pigs. RESULTS: ISOF significantly ameliorated pathological damage of lung tissue and improved pulmonary function in COPD rats. ISOF treatment decreased the number of inflammatory cells in peripheral blood, and also the levels of pro-inflammatory cytokines in serum and BALF. Consistent with omics-based analyses, ISOF markedly downregulated the mTOR level in lung tissue. Flow cytometry analysis revealed that ISOF treatment reduced the ratio of Th17/Treg cells in peripheral blood. Furthermore, the expression levels of AC1 and AC2 are relatively higher than other AC isoforms in normal lung tissues, and ISOF could potently activate AC1 and AC2 in vitro and significantly relax isolated guinea pig trachea. CONCLUSION: Collectively, our studies suggest that ISOF exerts its anti-COPD effect by improving lung function, anti-inflammation and trachea relaxation, which may be related to AC activation, mTOR signaling and Th17/Treg balance.


Subject(s)
Adenylyl Cyclases , Colforsin/pharmacology , Pulmonary Disease, Chronic Obstructive , Smoke , Animals , Coleus/chemistry , Guinea Pigs , HEK293 Cells , Humans , Phytochemicals/pharmacology , Pulmonary Disease, Chronic Obstructive/chemically induced , Pulmonary Disease, Chronic Obstructive/drug therapy , Rats , Smoke/adverse effects , Smoking
17.
Nat Prod Res ; 35(18): 3033-3039, 2021 Sep.
Article in English | MEDLINE | ID: mdl-31691584

ABSTRACT

Two heretofore uncharacterised abietane diterpenes, sincoetsin C (1) and 3-hydroxyspirocoleon 7-O-ß-D-glucoside (4), were isolated from a methanolic extract of Coleus blumei Benth. (Lamiaceae), along with the known compounds, scutellarioidone A (2) and spirocoleon 7-O-ß-D-glucoside (3) using chromatographic techniques. Their structures were determined by 1D and 2D nuclear magnetic resonance including HSQC, HMBC, COSY and NOESY experiments, mass spectrometry (HR-MS) and other spectroscopic methods (UV, IR). Their antibacterial activity against the reference strain of methicillin-resistant Staphylococcus aureus subsp. aureus CCM 4750 (MRSA) was evaluated using optical absorption to obtain quantitative information on their growth. All isolated compounds displayed anti-MRSA 4750 activity at the concentration of 512 µg/mL. Sincoetsin C (1) was the abietane diterpene most active against MRSA 4750, with a minimum inhibitory concentration of 128 µg/mL.


Subject(s)
Abietanes/pharmacology , Coleus , Diterpenes , Methicillin-Resistant Staphylococcus aureus , Abietanes/isolation & purification , Coleus/chemistry , Diterpenes/isolation & purification , Diterpenes/pharmacology , Methicillin-Resistant Staphylococcus aureus/drug effects , Phytochemicals/isolation & purification , Phytochemicals/pharmacology , Staphylococcus/drug effects
18.
Chem Biodivers ; 7(5): 1267-75, 2010 May.
Article in English | MEDLINE | ID: mdl-20491082

ABSTRACT

Bioassay-guided fractionation of a MeOH extract of tubers of Coleus tuberosus afforded the active anti-tumor-promoting compounds identified as the triterpenoid 2alpha,3beta-dihydroxyolean-12-en-28-oic acid (maslinic acid; CT2) and a phytosterol mixture (CT1). CT1 consists of stigmasterol (32%), beta-sitosterol (40.3%), and campesterol (27.7%) as determined by capillary gas chromatography. CT1 and CT2 showed very strong anti-tumor-promoting activities at IC(50) 0.7 microg/ml and 0.1 microg/ml, respectively, in a convenient, short-term in vitro assay, i.e., the inhibition of Epstein-Barr virus (EBV) activation induced by phorbol 12-myristate 13-acetate (PMA) and sodium butyrate. We report for the first time the anti-tumor-promoting activity of 2alpha,3beta-dihydroxyolean-12-en-28-oic acid and show that a mixture of stigmasterol, beta-sitosterol, and campesterol is more potent than the individual components in inhibiting tumor-promoting activity.


Subject(s)
Anticarcinogenic Agents/chemistry , Antigens, Viral/metabolism , Antineoplastic Agents, Phytogenic/chemistry , Coleus/chemistry , Phytosterols/chemistry , Triterpenes/chemistry , Anticarcinogenic Agents/isolation & purification , Anticarcinogenic Agents/pharmacology , Antineoplastic Agents, Phytogenic/isolation & purification , Antineoplastic Agents, Phytogenic/pharmacology , Butyrates/pharmacology , Cell Line , Herpesvirus 4, Human/drug effects , Humans , Molecular Conformation , Phytosterols/isolation & purification , Phytosterols/pharmacology , Plant Tubers/chemistry , Tetradecanoylphorbol Acetate/analogs & derivatives , Tetradecanoylphorbol Acetate/pharmacology , Triterpenes/isolation & purification , Triterpenes/pharmacology , Virus Activation/drug effects
19.
Curr Pharm Biotechnol ; 21(14): 1528-1538, 2020.
Article in English | MEDLINE | ID: mdl-32188380

ABSTRACT

BACKGROUND: In Saudi Arabia, the incidence and mortality rates of breast cancer are high. Although current treatments are effective, breast cancer cells develop resistance to these treatments. Numerous studies have demonstrated that active compounds in plant extracts, such as the phenolic compound Rosmarinic Acid (RA), exert anti-cancer effects. OBJECTIVE: We investigated the anticancer properties of methanolic crude extracts of seedlings and calli of Rosmarinus officinalis and Coleus hybridus, two Lamiaceae species. METHODS: MCF-7 human breast cancer cells were treated with methanolic crude extracts obtained from plant calli and seedlings generated in vitro, and cell proliferation was evaluated. Transcriptional profiling of the seedling and callus tissues was also conducted. RESULTS: The mRNA expression levels of RA genes were higher in C. hybridus seedlings than in R. officinalis seedlings, as well as in C. hybridus calli than in R. officinalis calli, except for TAT and C4H. In addition, seedling and callus extracts of both R. officinalis and C. hybridus showed anti-proliferative effects against MCF-7 cells after 24 or 48 h of treatment. DISCUSSION: At a low concentration of 10 µg/mL, C. hybridus calli and seedling extracts showed the most significant anti-proliferative effects after 24 and 48 h of exposure (p < 0.01); controls (doxorubicin) also showed significant inhibition, but lesser than that observed with C. hybridus (p < 0.05). Results with R. officinalis callus and seedling extracts did not significantly differ from those with untreated cells. CONCLUSION: Methanolic extracts of R. officinalis and C. hybridus are potentially valuable options for breast cancer treatment.


Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Cell Proliferation/drug effects , Cinnamates/pharmacology , Coleus/chemistry , Depsides/pharmacology , Plant Extracts/pharmacology , Rosmarinus/chemistry , Antineoplastic Agents, Phytogenic/isolation & purification , Cell Survival , Cinnamates/isolation & purification , Depsides/isolation & purification , Dose-Response Relationship, Drug , Humans , MCF-7 Cells , Plant Extracts/isolation & purification , Plant Shoots/chemistry , Seedlings/chemistry , Rosmarinic Acid
20.
J Hum Lact ; 25(1): 64-72, 2009 Feb.
Article in English | MEDLINE | ID: mdl-18984829

ABSTRACT

Torbangun (Coleus amboinicus Lour) has been used as a breast milk stimulant (a lactagogue) by Bataknese people in Indonesia for hundreds of years. However, the traditional use of torbangun is not well documented, and scientific evidence is limited to establish coleus as a lactagogue. This Focus Group Discussion (FGD) study was conducted to gather information regarding the practice and cultural beliefs related to the traditional use of torbangun as a lactagogue. The main findings of this investigation were: (1) torbangun, which is considered nourishing, is usually given to the mother for one month after giving birth in order to restore her state of balance; (2) in the Bataknese culture, torbangun is perceived to serve several purposes which include enhancing breast milk production and acting as a uterine cleansing agent; and (3) the tradition has been practiced for hundreds of years, and its adherence is still strong.


Subject(s)
Coleus/chemistry , Health Knowledge, Attitudes, Practice , Lactation/drug effects , Milk, Human/drug effects , Milk, Human/metabolism , Adult , Aged , Aged, 80 and over , Breast Feeding , Dietary Supplements , Female , Focus Groups , Humans , Indonesia , Infant , Infant, Newborn , Lactation/physiology , Middle Aged , Milk, Human/chemistry
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