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Objective: To evaluate anti-psoriatic activity of Coleus forskohlii in rats with imiquimod-induced psoriasis. Methods: Imiquimod was used to induce psoriasis in rats. Body weight, skin thickness, erythema, scaling, spleen weight, and histological alternations were measured to assess the effect of Coleus forskohlii. Furthermore, an emulgel formulation containing Coleus forskohlii 10% was prepared and characterized along with its ex vivo permeation studies. Results: The emulgel formulation containing Coleus forskohlii 10% had a pH of 5.40±0.36, with optimum spreadability of (31.67±2.08) g/(cms) and viscosity of (15 966.67±1 274.10) cps, and enhanced both the rate and the extent of drug permeation through psoriatic skin. In an ex vivo study, the quantity of drug permeated (19.18%), deposited (52.38%), and drug remaining in the donor compartments (28.31%) was satisfactory. Coleus forskohlii significantly alleviated imiquimod-induced psoriasis by increasing glutathione and superoxide dismutase activity, decreasing malondialdehyde and nitric oxide levels, and alleviating histological alternations in rat skin. Conclusions: Coleus forskohlii can alleviate imiquimod-induced psoriasis, which may be used as a therapeutic candidate for the treatment of psoriasis.

The successful isolation and characterization of diosgenin from the roots of C. forskohlii was accomplished by a combination of multiple analytical methods, including HPTLC, HPLC, UV, FT-IR, NMR, and mass spectroscopy. The primary goal of this research was to quantify the anticancer capabilities of the human ovarian SKOV-3 cancer cell line. The acquired compound is persisted to the preparative TLC using ethyl acetate and methanol (70:30 v/v) as eluents. Maximum absorbance was reported in the UV-Vis spectrum at 232 nm. The presence of the functional group was subsequently established by a variety of peaks in the FT-IR spectra, including 3450.06, 2947.74, 1236.38, 1054.99, and 894.11 cm-1. Structural elucidation of diosgenin had been performed through spectrum analysis for instance 13C and ¹H profoundly nuclear magnetic resources. The molecular formula C27H42O3 coincides with the parent molecular ion [M+] peak at m/z 414.63 g/mol, which is apparent in the mass spectra. The presently proceeding study's findings tend to show diosgenin has an astonishing cytotoxic action (IC50:75.47 µg/ml) on human ovarian cancer cells. [ABSTRACT FROM AUTHOR]

Background: Patients taking multiple drugs and various health foods often develop acute hepatitis. We hypothesized that the interaction between health foods and drug metabolism was the cause of severe liver injury in these patients. Therefore, we studied changes in the activity of the drug-metabolizing enzyme, cytochrome P450 (CYP), using slimming health food extracts and elucidated the molecular mechanism of liver injury onset through hepatotoxicity evaluation. Methods For cytotoxicity testing, health food extract samples were added to HepG2 cells derived from hepatic parenchymal cells and culture medium, and cell viability was calculated 48 h after culture. To evaluate CYP3A4 induction, 3-1-10 cells constructed with a reporter linked to CYP3A4 gene were used, and reporter activity was measured 48 h after culture. Results: In the chronological order of the slimming health food intake history of the patient, niacinamide and Gymnema sylvestre extracts strongly inhibited HepG2 cell viability. In contrast, dietary supplements A and Coleus forskohlii extract strongly induced CYP3A4 reporter activity. To confirm CYP3A4 induction in humans, humanized CYP3A/pregnane X receptor (PXR) mice were treated with forskolin. CYP3A4 mRNA expression levels were elevated 3.9 times compared to that of the control group (P < 0.05). Conclusion: Coleus forskohlii extract showed the strongest transcriptional activation of CYP3A4 gene. In a mouse model of human-type drug metabolism, forskolin induced CYP3A4 transcription. Thus, we concluded that CYP3A4 induction by Coleus forskohlii is one of the causes of crucial hepatocellular injury, which is a type of liver injury caused by the active metabolite of acetaminophen produced by CYP3A4. [ABSTRACT FROM AUTHOR]

Coleus forskohlii Briq., a medicinal plant from the Lamiaceae family, has been utilized worldwide to treat various disorders. The primary active compound in this plant is forskolin, a diterpene that accumulates in its rhizome. This study aims to assess the in vitro culture of C. forskohlii by investigating the effects of different concentrations of auxin hormone (1 and 2 mg L-1) and zinc oxide (ZnO) nanoparticles (10 and 20 ppm) as elicitors on biometrical traits related to rooting as well as forskolin content. Each treatment was replicated three times, and the results were analyzed using SPSS version 20. We observed that most traits examined decreased in samples treated with 1 mg L-1 of IAA hormone. In contrast, samples treated with 2 mg L-1 of IAA exhibited the highest values compared to the control samples. However, the differences in the examined characteristics among the samples were not statistically significant. Notably, the number of adventitious roots and the forskolin content increased with each increment in IAA hormone concentration. In plants treated with 2 mg L-1 IAA hormone, all measured biometrical traits surpassed those of the control group as well as those of samples co-treated with IAA (2 mg L-1) and ZnO nanoparticles (10 and 20 ppm). The forskolin content followed a similar trend. However, the lowest values for these traits were observed in the plants treated with 2 mg L-1 IAA and 20 ppm ZnO nanoparticles. These findings indicate that 2 mg L-1 of IAA hormone significantly impacts both root morphology and phytochemical characteristics compared to 1 mg L-1. Furthermore, ZnO nanoparticles at a concentration of 20 ppm exhibited an inhibitory effect on root morphology and forskolin content, which could not be mitigated by treatment with 2 mg L-1 IAA.

Coleus forskohlii (Willd.) Briq. is a medicinal herb of the Lamiaceae family. It is native to India and widely present in the tropical and sub-tropical regions of Egypt, China, Ethiopia, and Pakistan. The roots of C. forskohlii are edible, rich with pharmaceutically bioactive compounds, and traditionally reported to treat a variety of diseases, including inflammation, respiratory disorders, obesity, and viral ailments. Notably, the emergence of viral diseases is expected to quickly spread; consequently, these data impose a need for various approaches to develop broad active therapeutics for utilization in the management of future viral infectious outbreaks. In this study, the naturally occurring labdane diterpenoid derivative, Forskolin, was obtained from Coleus forskohlii. Additionally, we evaluated the antiviral potential of Forskolin towards three viruses, namely the herpes simplex viruses 1 and 2 (HSV-1 and HSV-2), hepatitis A virus (HAV), and coxsackievirus B4 (COX-B4). We observed that Forskolin displayed antiviral activity against HAV, COX-B4, HSV-1, and HSV-2 with IC50 values of 62.9, 73.1, 99.0, and 106.0 μg/mL, respectively. Furthermore, we explored the Forskolin's potential antiviral target using PharmMapper, a pharmacophore-based virtual screening platform. Forskolin's modeled structure was analyzed to identify potential protein targets linked to its antiviral activity, with results ranked based on Fit scores. Cathepsin L (PDB ID: 3BC3) emerged as a top-scoring hit, prompting further exploration through molecular docking and MD simulations. Our analysis revealed that Forskolin's binding mode within Cathepsin L's active site, characterized by stable hydrogen bonding and hydrophobic interactions, mirrors that of a co-crystallized inhibitor. These findings, supported by consistent RMSD profiles and similar binding free energies, suggest Forskolin's potential in inhibiting Cathepsin L, highlighting its promise as an antiviral agent. [ABSTRACT FROM AUTHOR]

Coleus forskohlii, an Indian-origin medicinal plant is the sole natural source of the labdane terpenoid forskolin (C22H34O7), with growing demand. Forskolin emerged as an industrially important bioactive compound, with many therapeutic applications in human health. It has established potential effects in the treatment of various diseases and conditions such as glaucoma, asthma, obesity, allergies, skin conditions and cardiovascular diseases. Moreover, clinical trials against different types of cancers are progressing. The mechanism of action of forskolin mainly involves activating adenylyl cyclase and elevating cAMP, thereby regulating different cellular processes. For the extraction of forskolin, tuberous roots of C. forskohlii are used as they contain the highest concentration of this metabolite. Approximately 2500 tonnes of the plant are cultivated annually to produce a yield of 2000–2200 kg ha−1 of dry tubers. The forskolin content of the root is distributed in the range of 0.01–1%, which cannot meet the increasing commercial demands from industries such as pharmaceuticals, cosmetics, dietary supplements, food and beverages. Hence, various aspects of micropropagation with different culture methods that employ precursors or elicitors to improve the forskolin content have been explored. Different extraction and analytical methods are also introduced to examine the yield and purity of forskolin. This review discusses the significance, clinical importance, mechanism of action and different approaches used for mass production including tissue culture for the lead compound forskolin to meet market needs. [ABSTRACT FROM AUTHOR]

Aim: To evaluate and compare the anti-cariogenic efficacy of Coleus forskohlii root extract, cranberry extract and magnetized water as mouthrinses by analysing pH and buffering capacity of saliva and Streptococcus mutans count in 6-12 years old children. Methods: The current study was an in vivo experimental study where 120 children were randomly assigned to four groups of 30 each. Group 1: Coleus forskohlii root extract, Group 2: Cranberry extract, Group 3: Magnetized water, Group 4: Chlorhexidine mouthrinse. Unstimulated saliva was collected and tested for salivary pH, buffering capacity and S. mutans count at 0, 30, 60, and 90 minutes after rinsing and the results were evaluated. Comparison between groups was carried out using one-way ANOVA, independent t test and paired t test. Results: While magnetized water showed the maximum alteration in the salivary pH, Chlorhexidine mouthrinse showed the maximum reduction in the microbial count followed by Coleus forskohlii root extract. All the groups maintained a favourable salivary buffering capacity. Conclusions: Coleus forskohlii root extract, cranberry extract and magnetized water have proven to be effective anti-cariogenic agents and can be used as alternatives to chlorhexidine in improving the oral health with added systemic benefits and minimal side effects.

Coleus forskohlii (Willd.) Briq. is a medicinal herb of the Lamiaceae family. It is native to India and widely present in the tropical and sub-tropical regions of Egypt, China, Ethiopia, and Pakistan. The roots of C. forskohlii are edible, rich with pharmaceutically bioactive compounds, and traditionally reported to treat a variety of diseases, including inflammation, respiratory disorders, obesity, and viral ailments. Notably, the emergence of viral diseases is expected to quickly spread; consequently, these data impose a need for various approaches to develop broad active therapeutics for utilization in the management of future viral infectious outbreaks. In this study, the naturally occurring labdane diterpenoid derivative, Forskolin, was obtained from Coleus forskohlii. Additionally, we evaluated the antiviral potential of Forskolin towards three viruses, namely the herpes simplex viruses 1 and 2 (HSV-1 and HSV-2), hepatitis A virus (HAV), and coxsackievirus B4 (COX-B4). We observed that Forskolin displayed antiviral activity against HAV, COX-B4, HSV-1, and HSV-2 with IC50 values of 62.9, 73.1, 99.0, and 106.0 μg/mL, respectively. Furthermore, we explored the Forskolin’s potential antiviral target using PharmMapper, a pharmacophore-based virtual screening platform. Forskolin’s modeled structure was analyzed to identify potential protein targets linked to its antiviral activity, with results ranked based on Fit scores. Cathepsin L (PDB ID: 3BC3) emerged as a top-scoring hit, prompting further exploration through molecular docking and MD simulations. Our analysis revealed that Forskolin’s binding mode within Cathepsin L’s active site, characterized by stable hydrogen bonding and hydrophobic interactions, mirrors that of a co-crystallized inhibitor. These findings, supported by consistent RMSD profiles and similar binding free energies, suggest Forskolin’s potential in inhibiting Cathepsin L, highlighting its promise as an antiviral agent.

The effect of inoculation with arbuscular mycorrhizal fungi Claroideoglomus claroideum on Coleus forskohlii (Willd.) Briq. plants propagated by seeds or in vitro, and subsequently exposed to drought stress has been studied. Stress tolerance and yield stability are closely related to coping with oxidative stress, which occurs at prolonged water deprivation.The plants inoculated with Claroideoglomus claroideum were grown in well-watered and drought-stressed conditions. The parameters of the inoculation with arbuscular mycorrhizal fungi (root colonization, total and easy-extractable-glomalin-related soil proteins, acid and alkaline phosphatases in roots and soil) and antioxidant activity (enzyme and non-enzyme parameters) were evaluated. In the inoculation of in vitro and in vivo propagated Coleus forskohlii (Willd.) Briq.with arbuscular mycorrizal fungi (AMF), an increase in the growth parameters, the activity of enzymes with antioxidant capacity and the content of total phenols and flavonoids and water- and lipid-soluble metabolites with antioxidant capacity were recorded compared with non inoculated plants. The results showed that arbuscular mycorrhizal fungi Claroideoglomus claroideum activate plants' antioxidant system, leading to reduced oxidative stress damage. The reduction in oxidative stress markers (hydrogen peroxide, malondialdehyde and proline) content as a result of AMF inoculation was higher in adapted in vitro propagated plants compared to in vivo plants. The same trend is observed in drought stressed plants. When grown in water-deficient conditions, adapted micro-propagated plants showed higher plant growth parameters such as shoot height, root length, plant biomass, antioxidant activity, and lower levels of oxidative stress markers, suggesting that they are more resistant to drought than the individuals which were grown from seeds. [ABSTRACT FROM AUTHOR]

Coleus barbatus is a medicinal herb belonging to Lamiaceae. It is the only living organism known to produce forskolin, which is a labdane diterpene and is reported to activate adenylate cyclase. Microbes associated with plants play an important role in maintaining plant health. Recently, the targeted application of beneficial plant-associated microbes and their combinations in abiotic and biotic stress tolerance has gained momentum. In this work, we carried out the rhizosphere metagenome sequencing of C. barbatus at different developmental stages to understand how rhizosphere microflora are affected by and affect the metabolite content in plants. We found that the Kaistobacter genus was abundantly present in the rhizosphere of C. barbatus and its accumulation pattern appears to correlate with the quantities of forskolin in the roots at different developmental stages. Members of the Phoma genus, known for several pathogenic species, were in lower numbers in the C. barbatus rhizosphere in comparison with C. blumei. To our knowledge, this is the first metagenomic study of the rhizospheric microbiome of C. barbatus, which may help to explore and exploit the culturable and non-culturable microbial diversity present in the rhizosphere. [ABSTRACT FROM AUTHOR]

Introduction: In obese humans, Coleus forskohlii root extract (CF) protects against weight gain owing to the presence of forskolin, an adenylate cyclase (AC) activator. As AC increases intracellular cyclic adenosine monophosphate (cAMP) levels in osteoblasts that has an osteogenic effect, we thus tested the skeletal effects of a standardized CF (CFE) in rats. Methods: Concentrations of forskolin and isoforskolin were measured in CFE by HPLC. CFE and forskolin (the most abundant compound present in CFE) were studied for their osteogenic efficacy in vitro by alkaline phosphatase (ALP), cAMP and cyclic guanosine monophosphate (cGMP) assays. Femur osteotomy model was used to determine the osteogenic dose of CFE. In growing rats, CFE was tested for its osteogenic effect in intact bone. In adult ovariectomized (OVX) rats, we assessed the effect of CFE on bone mass, strength and material. The effect of forskolin was assessed in vivo by measuring the expression of osteogenic genes in the calvarium of rat pups. Results: Forskolin content in CFE was 20.969%. CFE increased osteoblast differentiation and intracellular cAMP and cGMP levels in rat calvarial osteoblasts. At 25 mg/kg (half of human equivalent dose), CFE significantly enhanced calcein deposition at the osteotomy site. In growing rats, CFE promoted modeling-directed bone formation. In OVX rats, CFE maintained bone mass and microarchitecture to the level of sham-operated rats. Moreover, surface-referent bone formation in CFE treated rats was significantly increased over the OVX group and was comparable with the sham group. CFE also increased the pro-collagen type-I N-terminal propeptide: cross-linked C-telopeptide of type-I collagen (PINP : CTX-1) ratio over the OVX rats, and maintained it to the sham level. CFE treatment decreased the OVX-induced increases in the carbonate-to-phosphate, and carbonate-to-amide-I ratios. CFE also prevented the OVX-mediated decrease in mineral crystallinity. Nanoindentation parameters, including modulus and hardness, were decreased by OVX but CFE maintained these to the sham levels. Forskolin stimulated ALP, cAMP and cGMP in vitro and upregulated osteogenic genes in vivo. Conclusion: CFE, likely due to the presence of forskolin displayed a bone-conserving effect via osteogenic and anti-resorptive mechanisms resulting in the maintenance of bone mass, microarchitecture, material, and strength. [ABSTRACT FROM AUTHOR]

IntroductionIn obese humans, Coleus forskohlii root extract (CF) protects against weight gain owing to the presence of forskolin, an adenylate cyclase (AC) activator. As AC increases intracellular cyclic adenosine monophosphate (cAMP) levels in osteoblasts that has an osteogenic effect, we thus tested the skeletal effects of a standardized CF (CFE) in rats.MethodsConcentrations of forskolin and isoforskolin were measured in CFE by HPLC. CFE and forskolin (the most abundant compound present in CFE) were studied for their osteogenic efficacy in vitro by alkaline phosphatase (ALP), cAMP and cyclic guanosine monophosphate (cGMP) assays. Femur osteotomy model was used to determine the osteogenic dose of CFE. In growing rats, CFE was tested for its osteogenic effect in intact bone. In adult ovariectomized (OVX) rats, we assessed the effect of CFE on bone mass, strength and material. The effect of forskolin was assessed in vivo by measuring the expression of osteogenic genes in the calvarium of rat pups.ResultsForskolin content in CFE was 20.969%. CFE increased osteoblast differentiation and intracellular cAMP and cGMP levels in rat calvarial osteoblasts. At 25 mg/kg (half of human equivalent dose), CFE significantly enhanced calcein deposition at the osteotomy site. In growing rats, CFE promoted modeling-directed bone formation. In OVX rats, CFE maintained bone mass and microarchitecture to the level of sham-operated rats. Moreover, surface-referent bone formation in CFE treated rats was significantly increased over the OVX group and was comparable with the sham group. CFE also increased the pro-collagen type-I N-terminal propeptide: cross-linked C-telopeptide of type-I collagen (PINP : CTX-1) ratio over the OVX rats, and maintained it to the sham level. CFE treatment decreased the OVX-induced increases in the carbonate-to-phosphate, and carbonate-to-amide-I ratios. CFE also prevented the OVX-mediated decrease in mineral crystallinity. Nanoindentation parameters, including modulus and hardness, were decreased by OVX but CFE maintained these to the sham levels. Forskolin stimulated ALP, cAMP and cGMP in vitro and upregulated osteogenic genes in vivo.ConclusionCFE, likely due to the presence of forskolin displayed a bone-conserving effect via osteogenic and anti-resorptive mechanisms resulting in the maintenance of bone mass, microarchitecture, material, and strength.

Herein, polyphenol oxidase (PPO) was purified from Coleus forskohlii via a three-step process involving precipitation by (NH4)2SO4, ion exchange chromatography and gel filtration. PPO was purified 15-fold with a total yield of 31% and a specific activity of 3168 U/mg, and the observed molecular weight was 42 kDa. To improve the reusability and stability of the purified enzyme, calcium alginate incorporated with zinc oxide nanoparticles (Ca-ALG-ZnO NPs) was successfully prepared and characterized through scanning electron microscopy and Fourier transform infrared spectroscopy and utilized as a support for PPO immobilization. The immobilization yield and enzyme activity reached 83% and 3950 U/g support, respectively. The results showed that immobilized PPO could be reused ten times while retaining 69% of its original activity. The purified and immobilized PPO exhibited an optimal pH of 7.0 and 7.5 and an optimal temperature of 40 °C and 50 °C, respectively. The purified and immobilized PPO showed Vmax values of 255.75 and 251.89 Units/ml, and Km values of 4.99 and 3.12 mM, respectively. As a result, this work provides an opportunity to understand and manage the influence of the coleus forskohlii PPO enzyme in key immobilization, industrial. Additionally, the results indicated that the Ca-ALG-ZnO NPs used as supports had a significant effect on the enzyme activity and stability of immobilized PPO. [ABSTRACT FROM AUTHOR]

Coronavirus disease 2019 (COVID–19) has spread rapidly as global pandemic affecting 187 countries/ regions and emerged as worldwide health crisis. Potential antiviral drugs used for the SARS -CoV-2 in clinical treatments have side effects. However, emergency vaccines are in use but despite that increase in the coronavirus cases are alarming. Thus, it is utmost need of safer antiviral agent to treat or inhibit the viral infection. Forskolin has been reported as a possible antiviral-agent. This molecule was docked with ACE2 receptor of human which is the target for the binding of S1 unit of viral S protein of SARS-CoV- 2. In silico docking was carried out on SwissDock, PatchDock and FireDock servers. The docked ACE2 structure was further docked with the RBD of the spike protein. Forskolin is able to H-bond with the hACE2 and ACE2-forskolin fails to interact with the receptor-binding domain (RBD) of the Spike protein of SARS-CoV-2. Instead, viral RBD is repulsed by the diterpene molecule through obliteration and reciprocated binding. We report first that forskolin plays a crucial role in the inhibition of protein-protein interaction of RBD and ACE2 when docked with either of the protein.

• Quantification of total polyphenols by HPLC. • Inhibition of aldose reductase activity by rosmarinic acid. • Μolecular docking analysis of rosmarinic acid with aldose reductase. Many complications of diabetes have been associated with the accumulation of intracellular sorbitol caused by excessive activity of aldose reductase (ALR2). ALR2 is a member of the aldo-keto reductases (AKR) superfamily and has gained significant attention due to its role in the development of diabetic complications. Inhibiting ALR2 could help prevent or delay some of these problems. Coleus forskohlii is a natural medicinal plant that is known for its medicinal effects and is also used as a beverage in several European countries. High-performance liquid chromatography (HPLC) was used to measure the polyphenol content of aqueous leaf extracts of C. forskohlii, and it was found that rosmarinic acid (RA) had the highest concentration (1.25 mg/g) compared to other polyphenols. In vitro bioassays were conducted to evaluate the inhibitory effect of RA on ALR2. RA significantly and dose-dependently reduced the build-up of sorbitol in human erythrocytes under high glucose conditions. Molecular docking studies suggest that RA, which is an essential polyphenol, could be a potential ALR2 inhibitor. This study is the first to show that RA has an IC50 value of 56 % to exhibit an inhibitory effect against ALR2. [Display omitted] [ABSTRACT FROM AUTHOR]

Greater celandine and Coleus forskohlii are designated as ingredients that require special attention (designated ingredients) under the Food Hygiene Act. In this study, we developed a method for the simultaneous quantitative analysis of coptisine and forskolin in dietary supplements containing the designated ingredients using ultra-high performance liquid chromatography (UHPLC). We also developed a simultaneous qualitative analysis method for coptisine, sanguinarine, forskolin, and isoforskolin in dietary supplements containing the designated ingredients using a UHPLC-quadrupole-Kingdon trap mass spectrometry with photodiode array detector. Extraction of samples was carried out by ultrasonication using methanol as the extraction solvent. An ODS column was used for quantitative and qualitative analyses. Quantitative analysis was performed on a gradient of 10 mmol/L phosphate buffer (pH 3.0)-acetonitrile, and qualitative analysis was performed on a gradient of 10 mmol/L ammonium formate buffer (pH 3.0)-acetonitrile. The recovery test results showed recoveries of between 97.23 and 102.14%; the standard deviation was within 2%, indicating good precision. In the application of our quantitative analysis method to commercial dietary supplements, maximums of 10.71 mg/bottle of coptisine and 27.73 mg/tablet of forskolin were detected. When a product containing 27.73 mg/tablet of forskolin was consumed as indicated on the label, the daily intake of forskolin was 110.92 mg. In the qualitative analysis, we confirmed the presence of coptisine, sanguinarine and forskolin in the dietary supplements. The isoforskolin content was confirmed except for one product that contained the minimum amount of forskolin. [ABSTRACT FROM AUTHOR]

Coleus forskohlii is an important medicinal plant native to India. It grows wild across a wide range of altitudes in the Indian Himalayan region and contains some important phytochemicals that possess remarkable medicinal properties. This plant is the only known source of a medicinally important terpenoid, forskolin, found in its roots. This study was conducted looking at its availability over a wide altitudinal range and medicinal importance. Samples of the five C. forskohlii populations were collected from five altitudes of Uttarakhand, India. HPTLC and HPLC were employed for metabolic diversity analysis. Secondary metabolites were extracted using the Soxhlet extraction, followed by HPTLC fingerprinting and HPLC. Significant differences observed in the HPTLC chromatograms across altitudes. Maximum bands were observed in the HPTLC chromatogram of Gopeshwar population (1488 m a.s.l.). HPLC revealed differences in forskolin quantity among studied populations with the Pipalkoti population (1339 m a.s.l.) showing highest forskolin accumulation. Thus, the present study confirms that altitude and changing environment can affect the nature and quantity of secondary metabolites in C. forskohlii and might be contributory factors for intraspecific metabolic diversity. The Pipalkoti and Gopeshwar populations were found suitable for forskolin and other metabolite production; further, these two populations can be propagated for commercial use. [ABSTRACT FROM AUTHOR]

The present study was designed to determine protective effects of Coleus forskohlii hydroalcoholic leaf-extract along with its fractions against fructose-induced cataract rat model. The Coleus forskolii leaf extract was subjected to silica gel column chromatography and fractions were collected. A major high yielding fraction of the leaf extract, designated as fraction B6 was pharmacologically evaluated in Sprague Dawley albino rats at three doses 0.1, 1 and 10 mg/kg respectively. Compound B2; isolated from B6 fraction, identified as 'gallic acid' was also pharmacologically evaluated at three different doses. Cataract was induced by concurrent administration of fructose solution (10% w/v, per oral, dissolved in drinking water) for eight consecutive weeks. Mean arterial pressure, blood glucose level and lenticular opacity were determined. At the end of eight weeks, C. forskohlii leaf extract fraction and gallic acid reduced mean arterial pressure and glucose level in a dose dependent manner. In addition, C. forskohlii led to significant restoration of lens antioxidants enzyme level and reduced cataract formation in rats. These results showed the concentration dependent protective effect by C. forskohlii leaf extract against cataract formation due to restoration of oxidative stress markers. [ABSTRACT FROM AUTHOR]

Coleus barbatus is a medicinal herb belonging to Lamiaceae. It is the only living organism known to produce forskolin, which is a labdane diterpene and is reported to activate adenylate cyclase. Microbes associated with plants play an important role in maintaining plant health. Recently, the targeted application of beneficial plant-associated microbes and their combinations in abiotic and biotic stress tolerance has gained momentum. In this work, we carried out the rhizosphere metagenome sequencing of C. barbatus at different developmental stages to understand how rhizosphere microflora are affected by and affect the metabolite content in plants. We found that the Kaistobacter genus was abundantly present in the rhizosphere of C. barbatus and its accumulation pattern appears to correlate with the quantities of forskolin in the roots at different developmental stages. Members of the Phoma genus, known for several pathogenic species, were in lower numbers in the C. barbatus rhizosphere in comparison with C. blumei. To our knowledge, this is the first metagenomic study of the rhizospheric microbiome of C. barbatus, which may help to explore and exploit the culturable and non-culturable microbial diversity present in the rhizosphere.

Background: Coleus forskohlii (Lamiaceae) cultivates imperishably over the tropical and subtropical regions of Asia; extracts from the roots and aerial parts of C. forskohlii are widely employed for the therapy of respiratory disorders, gastro-intestinal disturbance, heart diseases, and central nervous system disorders. The morphologies and structures of trichomes from C. forskohlii, as well as phytochemicals they secrete in China-origin plants are poorly unstated. Objectives: This study was intended to characterize the morphology and structure of trichomes and the profile of their secretory materials. Materials and Methods: To characterize the morphology and structure of trichomes, which happen on the vegetative and reproductive organs of C. forskohlii, it was employed light microscopy and scanning electron microscopy. The chemical qualities of volatile compounds from Glandular trichomes (GTs) of C. forskohlii were also studied using gas chromatography mass spectrometry (GC-MS) and histochemical reactions. Results: Four morphologically distinct trichomes, i.e., non GTs, peltate GTs, Type 1 and 2 capitate GTs, were categorized. Histochemical study naked the presence of polyphenols, flavonoids, lipids, and terpenes in the GTs. Essential oils, isolated from mature leaves by hydro-distillation, were investigated by GC-MS and 41 compounds were acknowledged with oxygen-containing sesquiterpenes and monoterpenes as the major compounds. Conclusion: Secretory materials of GTs attained by surface extraction also indicated the precise features in the China-origin samples. [ABSTRACT FROM AUTHOR]

The present study was on the analysis of phytochemical constituents of Coleus forskohlii rhizome collected from Thiruvannamalai of Tamil Nadu and testing for its antimicrobial potential against human bacterial pathogens. The dried tubers were extracted using different solvents such as ethanol, aqueous, acetone, chloroform and petroleum ether and screened. The total tannin and saponin content in the extract was estimated. The crude ethanolic solvent extract of C. forskohlii was tested for its antimicrobial activity using disc diffusion method. Phytochemical screening of the crude solvent extracts revealed the presence of tannins, phenols, saponins, quinone, flavonoids, cardiac glycoside, terpenoids, steroids, alkaloids, and coumarins. Tannic acid was found in the level of 53.47 ±0.37 mg TAE/g. Saponin content was 2.42±0.63 mg/g dry weight. The crude ethanolic rhizome extract was tested in three different concentrations (10, 20 and 30mg/ml). Maximum antibacterial activity was noted against Bacillus subtilis (15 mm), followed by Bacillus cereus (14 mm), P. aeruginosa (12 mm) and S. aureus (12mm). E. coli was not inhibited even at the highest concentration tested (i.e.) 30mg/ml. The minimum inhibitory concentration (MIC) values of the pathogens tested were 1.4±0.02, 1.590±0.02, 1.820±0.02 and 2.350±0.02 mg/ml respectively to B. subtilis, B. cereus, P. aeruginosa , and S. aureus. Similarly, the minimum bactericidal concentration (MBC) for B. subtilis, B. cereus, P. aeruginosa , and S. aureus were respectively of 2.89±0.02, 3.833±0.05, 3.842±0.01 and 4.856±0.05 mg/ml. In time-kill assay 3 Log reduction was found to be around 11 h for B. subtilis, around 12 h for B. cereus for P. aeruginosa around 13 h and above 14 and less than 15 h for S. aureus. The study showed the antimicrobial potential of ethanol extract of C. forskohlii tuber against human bacterial pathogens and hence it seems to be useful in the preparation of drug formulations.

Coronavirus disease 2019 (COVID-19) has spread rapidly as global pandemic affecting 187 countries/regions and emerged as worldwide health crisis. Potential antiviral drugs used for the SARS-CoV-2 in clinical treatments have side effects. However, emergency vaccines are in use but despite that increase in the coronavirus cases are alarming. Thus, it is utmost need of safer antiviral agent to treat or inhibit the viral infection. Forskolin has been reported as a possible antiviral-agent. This molecule was docked with ACE2 receptor of human which is the target for the binding of S1 unit of viral S protein of SARSCoV-2. In silico docking was carried out on SwissDock, PatchDock and FireDock servers. The docked ACE2 structure was further docked with the RBD of the spike protein. Forskolin is able to H-bond with the hACE2 and ACE2-forskolin fails to interact with the receptor-binding domain (RBD) of the Spike protein of SARS-CoV-2. Instead, viral RBD is repulsed by the diterpene molecule through obliteration and reciprocated binding. We report first that forskolin plays a crucial role in the inhibition of proteinprotein interaction of RBD and ACE2 when docked with either of the protein. [ABSTRACT FROM AUTHOR]

Vitiligo is a chronic autoimmune disease affecting around 1% of the population worldwide. No existing treatment is giving fully satisfactory results. Further investigations are welcomed for innovative and safe treatments bringing better results. This trial aimed to compare the efficacy and tolerance of various treatment protocols on vitiligo lesions. Four randomized groups of 10 patients with vitiligo covering 8% to 14% of skin surface, except hands and feet were assigned during 8 weeks to (a) UVB microphototherapy 300 to 320 nm (Bioskin‒) 1 x week; (b) VITILSI‒ gel 2 x day; (c) VITILSI‒ gel 2xday + Bioskin‒ 1 x week; and (d) placebo 2 x day. Efficacy of the treatment was assessed by planimetry, comparing the photographs of the patients taken at baseline and after 8‐week treatment. After completion of the treatment, the increase of the pigment area was 28% in G1 (Bioskin‒), 19% in G2 (VITILSI‒), 41% in G3 (Bioskin‒ + VITILSI‒) and null in G4. No subject stopped the treatment and no side effect was observed. It was demonstrated that the gel under study was able per se to induce repigmentation in vitiligo lesions and that the results were significantly better when combined with NB‐UVB. The protocols used in this trial resulted safe and efficient. [ABSTRACT FROM AUTHOR]

Background: Patients taking multiple drugs and various health foods often develop acute hepatitis. We hypothesized that the interaction between health foods and drug metabolism was the cause of severe liver injury in these patients. Therefore, we studied changes in the activity of the drug-metabolizing enzyme, cytochrome P450 (CYP), using slimming health food extracts and elucidated the molecular mechanism of liver injury onset through hepatotoxicity evaluation., Methods: For cytotoxicity testing, health food extract samples were added to HepG2 cells derived from hepatic parenchymal cells and culture medium, and cell viability was calculated 48 h after culture. To evaluate CYP3A4 induction, 3-1-10 cells constructed with a reporter linked to CYP3A4 gene were used, and reporter activity was measured 48 h after culture., Results: In the chronological order of the slimming health food intake history of the patient, niacinamide and Gymnema sylvestre extracts strongly inhibited HepG2 cell viability. In contrast, dietary supplements A and Coleus forskohlii extract strongly induced CYP3A4 reporter activity., To confirm CYP3A4 induction in humans, humanized CYP3A/pregnane X receptor (PXR) mice were treated with forskolin. CYP3A4 mRNA expression levels were elevated 3.9 times compared to that of the control group ( P < 0.05)., Conclusion: Coleus forskohlii extract showed the strongest transcriptional activation of CYP3A4 gene. In a mouse model of human-type drug metabolism, forskolin induced CYP3A4 transcription. Thus, we concluded that CYP3A4 induction by Coleus forskohlii is one of the causes of crucial hepatocellular injury, which is a type of liver injury caused by the active metabolite of acetaminophen produced by CYP3A4., Competing Interests: The authors declare no conflict of interest., (©2024 Tottori University Medical Press.)

Coleus forskohlii is an herb, well-known for its medicinal compound forskolin present in its roots, with wide range of pharmaceutical applications. Here, we report, for the first time, the role of plant–probiotic bacterial endophytes of C. forskohlii, CFLB1 and CFRB1, isolated from leaf and root, which regulate plant growth and in plant forskolin content. Native bacterial endophyte, CFRB1 (Alcaligenes faecalis), significantly modulates primary plant productivity and forskolin content under pot and field conditions. Under field conditions, CFRB1 endophyte application significantly enhanced photosynthetic pigments and reduced the severity of root-knot and root rot diseases. Expression analyses of functional genes involved in the forskolin biosynthesis in C. forskohlii plants treated with CFRB1 endophyte under field conditions revealed differential upregulation of four C. forskohlii diterpene synthases (CfTPSs), CfTPS1, CfTPS2, CfTPS3 and CfTPS4, along with cytochrome P450 (CfCYP76AH15) and acyltransferase (CfACT1–8) genes. CFRB1 treatment reduced the severity of nematode infection and root rot in C. forskohlii plants by 81 and 78%, respectively. Overall, we demonstrate that cross-talk of plant–endophyte interaction in C. forskohlii is beneficial, leading to enhanced forskolin content through modulation of forskolin biosynthetic pathway genes along with increased plant yield and reduced disease incidence. Thus, endophytic isolate, A. faecalis (CFRB1), could be deployed as a novel bio-stimulant for enhancing in planta forskolin content during cultivation of C. forskohlii. [ABSTRACT FROM AUTHOR]

Since ancient times, plant roots have been widely used in traditional medicine for treating various ailments and diseases due to their beneficial effects. A large number of studies have demonstrated that—besides their aromatic properties—their biological activity can often be attributed to volatile constituents. This review provides a comprehensive overview of investigations into the chemical composition of essential oils and volatile components obtained from selected aromatic roots, including Angelica archangelica, Armoracia rusticana, Carlina sp., Chrysopogon zizanioides, Coleus forskohlii, Inula helenium, Sassafras albidum, Saussurea costus, and Valeriana officinalis. Additionally, their most important associated biological impacts are reported, such as anticarcinogenic, antimicrobial, antioxidant, pesticidal, and other miscellaneous properties. Various literature and electronic databases—including PubMed, ScienceDirect, Springer, Scopus, Google Scholar, and Wiley—were screened and data was obtained accordingly. The results indicate the promising properties of root-essential oils and their potential as a source for natural biologically active products for flavor, pharmaceutical, agricultural, and fragrance industries. However, more research is required to further establish the mechanism of action mediating these bioactivities as well as essential oil standardization because the chemical composition often strongly varies depending on external factors.

Coleus forskohlii is a perennial medicinal shrub cultivated mainly for its forskolin content. The plant has been used since ancient times in ayurvedic traditional medicines for the treatment of hypertension, glaucoma, asthma, congestive heart failures, obesity, and cancer. Use of endophytic microorganisms presents a special interest for the development of value-added bioactive compounds through agriculture. Limited investigations have been undertaken on in planta enhancement of forskolin content using endophytic fungus in sustainable agriculture. Here we report specific roles of three fungal endophytes, Fusarium redolens (RF1), Phialemoniopsis cornearis (SF1), and Macrophomina pseudophaseolina (SF2), functionally acting as plant probiotic fungus, regulating secondary metabolite (forskolin) biosynthesis in C. forskohlii. The root endophyte, RF1, and shoot endophytes, SF1 and SF2, were found to enhance forskolin content by 52 to 88% in pot and 60 to 84% in field experiments as compared to uninoculated control plants. The three endophytes also enhanced total biomass owing to plant growth promoting properties. The expression of diterpene synthases (CfTPSs) like CfTPS1, CfTPS2, CfTPS3, and CfTPS4 were significantly upregulated in endophyte-treated C. forskohlii plants. Elevated expression of key diterpene synthases (CfTPS2) in the forskolin biosynthesis pathway, exclusively present in the root cork of C. forskohlii, was observed following SF2 endophyte treatment. Furthermore, endophyte treatments conferred a variety of antagonistic activity against nematode galls (80%) and plant pathogens like Fusarium oxysporum, Colletotricum gloeosporioides, and Sclerotium rolfsii. RF1 and SF1 fungal endophytes showed positive for IAA production; however, SF1 also indicated phosphate solubilization activity. Overall, the qualitative and quantitative improvement of in planta forskolin enhancement represents an area of high commercial interest, and hence, our work focused on novel insights for the application of three fungal endophytes for in planta enhancement of forskolin content for C. forskohlii cultivation by a sustainable approach. [ABSTRACT FROM AUTHOR]

Coleus forskohlii roots are mainly used for extraction of the bioactive diterpenoid, forskolin, which has enormous biological activities. In this study, impact of the solvent and extraction method on forskolin content from Coleus forskohlii root powder was investigated. Nine solvents from different polarity group were tested for forskolin extraction. It was found that the efficiency of the solvents used to extract forskolin varied considerably (0.18 to 2.91 %). The average values indicated that among all the extractives, forskolin content was significantly higher in methanol (2.91 %), followed by ethanol (2.59 %), and least content was found in water (0.18 %). Low polarity solvents were not found very effective for forskolin extraction. Further three different extraction methods (Soxhlet/refluxing, ultrasound and microwaveassisted solvent extraction) were also compared using safest and most effective solvent for forskolin yield. As ethanol exhibited good extraction efficiency for forskolin and is a safe solvent, it was chosen for further optimization of extraction method. Soxhlet extraction technique gave higher yield of forskolin (0.17 to 2.83 %) compared to microwave-assisted solvent extraction (0.09 to 2.29 %) and ultra sound-assisted extraction (0.08 to 1.47 %). From these results it was evident that the extraction of forskolin depended on extraction process as well as the solvent useds. [ABSTRACT FROM AUTHOR]

Coleus (Lamiaceae) is a large and widespread genus comprising of species with diverse ethnobotanical uses. In the present study, bacterial endophytes were isolated from Coleus forskohlii and Coleus aromaticus. Endophytes are the microorganisms which reside within the plants without showing any harmful effect on its host. Diverse types of endophytes live symbiotically within almost all plants and in turn help the plant in a number of ways such as imparting resistance against biotic and abiotic stresses, producing compounds involved in attraction of pollinators, inducing the plant defense mechanisms, etc. The bacterial endophytes isolated in this study, were characterized by microscopic examination (using gram staining) and molecularly identified by sequencing the 16S rRNA. Extracts were prepared from endophytic biomass using solvents of different polarities (methanol, ethyl acetate and butanol) and were screened for their bioactive potential (in vitro cytotoxicity anti-microbial, and anti-oxidant activity). Scale-up of endophytes showing promising results is under process, which will help in isolation of pure compounds. [ABSTRACT FROM AUTHOR]

Background: Cataract is the opacification or optical dysfunction of the crystalline lens. Diabetes has been considered to be one of the major risk factors of cataract. Objective: The present study was designed to evaluate the anticataract activity of antioxidants such as Coleus forskohlii (CF) Briq and its phytoconstituent forskolin (FS) which were subjected to prevent cataract formation in vitro on glucose-induced cataract model. Materials and Methods: Goat lenses were incubated in Krebs-Ringer bicarbonate buffer pH 7.5 (supplemented with Taxim and streptomycin) containing 55 mM glucose (cataractogenesis) with fidarestat; CF methanolic extract; and FS at a concentration of 1 μg/mL, 100 μg/mL, and 10 μg/mL for 24 h at 37°C with 5% CO2and 95% air. Glucose-induced opacification of goat lens began 8–10 h after incubation and was complete in 24 h. Polyol (galactitol) levels in incubated lenses were estimated spectrophotometrically. Results: Cataractous lenses showed higher content of galactitol. However, lens treated with fidarestat, CF methanolic extract, and its phytoconstituent FS showed lower content of galactitol. Conclusion: CF and FS prevented the formation and progress of cataract by glucose, as evidenced by lens transparencies with photographic evaluation and lens galactitol levels. [ABSTRACT FROM AUTHOR]

Coleus forskohlii extract (CFE), a popular weight-loss herbal product, induces hepatic cytochrome P450 (CYP) and fatty liver in mice; however, its main bioactive ingredient, forskolin, does not show such effects. To ensure the safety of CFE as a dietary supplement, identification of the compounds implicated in the induction of hepatic CYP and fatty liver is required. In this study, we separated a crude CFE extract into 5 fractions (Fr.) by column chromatography and administered the fractions to mice for one week to assess their ability to induce CYP and fatty liver. CYP induction was detected for all fractions, indicating that many compounds may be involved in CYP induction, while fatty liver was only detected for Fr. 2. Further isolation and purification of Fr. 2 by column chromatography identified 14-deoxycoleon U as a major compound and crocetin dialdehyde as a pigment compound. An in vivo mouse study revealed that crocetin dialdehyde had no effect on the liver and, as 14-deoxycoleon U was the major compound in Fr. 2, it is likely that the active compound inducing fatty liver in CFE is 14-deoxycoleon U. These findings will facilitate the preparation of standardized safe CFE ingredients for dietary supplements. [ABSTRACT FROM AUTHOR]

Forskolin is mainly found in the root of a plant called Coleus forskohlii (Willd.) Briq., which has been used in the traditional medicine of Indian Ayurvedic and Southeast Asia since ancient times. Forskolin is responsible for the pharmacological activity of this species. Forskolin is a labdane diterpenoid with a wide biological effect. Several studies suggested a positive role of forskolin on heart complications, respiratory disorders, high blood pressure, obesity, and asthma. There are numerous clinical and pre-clinical studies representing the effect of forskolin on the above-mentioned disorders but more clinical studies need to be performed to support its efficacy. [ABSTRACT FROM AUTHOR]

The present study was on the analysis of phytochemical constituents of Coleus forskohlii rhizome collected from Thiruvannamalai of Tamil Nadu and testing for its antimicrobial potential against human bacterial pathogens. The dried tubers were extracted using different solvents such as ethanol, aqueous, acetone, chloroform and petroleum ether and screened. The total tannin and saponin content in the extract was estimated. The crude ethanolic solvent extract of C. forskohlii was tested for its antimicrobial activity using disc diffusion method. Phytochemical screening of the crude solvent extracts revealed the presence of tannins, phenols, saponins, quinone, flavonoids, cardiac glycoside, terpenoids, steroids, alkaloids, and coumarins. Tannic acid was found in the level of 53.47 ±0.37 mg TAE/g. Saponin content was 2.42±0.63 mg/g dry weight. The crude ethanolic rhizome extract was tested in three different concentrations (10, 20 and 30mg/ml). Maximum antibacterial activity was noted against Bacillus subtilis (15 mm), followed by Bacillus cereus (14 mm), P. aeruginosa (12 mm) and S. aureus (12mm). E. coli was not inhibited even at the highest concentration tested (i.e.) 30mg/ml. The minimum inhibitory concentration (MIC) values of the pathogens tested were 1.4±0.02, 1.590±0.02, 1.820±0.02 and 2.350±0.02 mg/ml respectively to B. subtilis, B. cereus, P. aeruginosa, and S. aureus. Similarly, the minimum bactericidal concentration (MBC) for B. subtilis, B. cereus, P. aeruginosa, and S. aureus were respectively of 2.89±0.02, 3.833±0.05, 3.842±0.01 and 4.856±0.05 mg/ml. In time-kill assay 3 Log reduction was found to be around 11 h for B. subtilis, around 12 h for B. cereus for P. aeruginosa around 13 h and above 14 and less than 15 h for S. aureus. The study showed the antimicrobial potential of ethanol extract of C. forskohlii tuber against human bacterial pathogens and hence it seems to be useful in the preparation of drug formulations. [ABSTRACT FROM AUTHOR]