Search Results (31)

Background/Objectives: Aldose reductase (AR) plays a crucial role in the accumulation of oxidative factors that lead to oxidative stress-related neuroinflammation. This study aims to find a novel agent from natural sources that can inhibit AR. Methods: Different extracts of Orthosiphon stamineus Benth (OS) leaves and its active constituents, eupatorin (EUP), rosmarinic acid (RA), sinensetin (SEN) and 3-hydroxy-5,6,7,4-tetramethoxyflavone (TMF), were used to identify the potential inhibition effect of AR. A new high-performance liquid chromatography (HPLC) method was developed to determine these phytochemicals using the Shimadzu LC-20AD HPLC system. In addition, the in vitro inhibition effect of OS ethanol extracts (95% and 50%) and OS components EUP, RA, and SEN was investigated in recombinant AR (AKR1B1). Results: In this study, the developed HPLC method was precise and accurate, and demonstrated clear separation of the four compounds—EUP, RA, SEN, and TMF—in the ethanolic extract. The contents of the four selected compounds—EUP, RA, SEN, and TMF—in 95% ethanolic extract were 2.35, 11.91, 0.94, and 0.18%, respectively. RA showed the highest concentration among the selected compounds, indicating that RA is the major constituent of this plant. The in vitro assay showed significant inhibition of the AR enzyme by RA and OS ethanol extracts 95% and 50% (IC₅₀: 41.42 µM; 63.42 µg/mL and 93.22 µg/mL, respectively). Conclusions: The ethanolic extract of OS and RA could be a promising therapeutics option for the treatment of oxidative stress-related neuroinflammation disorders by inhibiting AR. Full article

Orthosiphon stamineus is a popular folk herb used to treat diabetes and some other disorders. Previous studies have shown that O. stamineus extracts were able to balance blood glucose levels in diabetic rat animal models. However, the antidiabetic mechanism of O. stamineus is not fully known. This study was carried out to test the chemical composition, cytotoxicity, and antidiabetic activity of O. stamineus (aerial) methanol and water extracts. GC/MS phytochemical analysis of O. stamineus methanol and water extracts revealed 52 and 41 compounds, respectively. Ten active compounds are strong antidiabetic candidates. Oral treatment of diabetic mice with O. stamineus extracts for 3 weeks resulted significant reductions in blood glucose levels from 359 ± 7 mg/dL in diabetic non-treated mice to 164 ± 2 mg/dL and 174 ± 3 mg/dL in water- and methanol-based-extract-treated mice, respectively. The efficacy of O. stamineus extracts in augmenting glucose transporter-4 (GLUT4) translocation to the plasma membrane (PM) was tested in a rat muscle cell line stably expressing myc-tagged GLUT4 (L6-GLUT4myc) using enzyme-linked immunosorbent assay. The methanol extract was more efficient in enhancing GLUT4 translocation to the PM. It increased GLUT4 translocation at 250 µg/mL to 279 ± 15% and 351 ± 20% in the absence and presence of insulin, respectively. The same concentration of water extract enhanced GLUT4 translocation to 142 ± 2.5% and 165 ± 5% in the absence and presence of insulin, respectively. The methanol and water extracts were safe up to 250 µg/mL as measured with a Methylthiazol Tetrazolium (MTT) cytotoxic assay. The extracts exhibited antioxidant activity as measured by 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. O. stamineus methanol extract reached the maximal inhibition of 77 ± 10% at 500 µg/mL, and O. stamineus water extract led to 59 ± 3% inhibition at the same concentration. These findings indicate that O. stamineus possesses antidiabetic activity in part by scavenging the oxidants and enhancing GLUT4 translocation to the PM in skeletal muscle. Full article

Rosmarinic acid (RA) is present in a broad variety of plants, including those in the Lamiaceae family, and has a wide range of pharmacological effects, particularly antioxidant activity. To extract RA from Orthosiphon stamineus (OS) leaves, a Lamiaceae plant, a suitable extraction process is necessary. The present study used a green extraction method of supercritical carbon dioxide (SCCO₂) extraction with the addition of ethanol as a modifier to objectively measure and correlate the solubility of RA from OS leaves. The solubility of RA in SCCO₂ was determined using a dynamic extraction approach, and the solubility data were correlated using three density-based semi-empirical models developed by Chrastil, del Valle-Aguilera, and Gonzalez. Temperatures of 40, 60, and 80 °C and pressures of 10, 20, and 30 MPa were used in the experiments. The maximum RA solubility was found at 80 °C and 10 MPa with 2.004 mg of rosmarinic acid/L solvent. The RA solubility data correlated strongly with the three semi-empirical models with less than 10% AARD. Furthermore, the fastest RA extraction rate of 0.0061 mg/g min⁻¹ was recorded at 80 °C and 10 MPa, and the correlation using the Patricelli model was in strong agreement with experimental results with less than 15% AARD. Full article

Orthosiphon stamineus is a well-known medicinal herb that has long been used as a traditional treatment for a variety of ailments and disorders. In this study, in vitro grown O. stamineus plantlets were subjected to various stress factors to elucidate the effects of these stresses on the occurrence of somaclonal variation in this species. Murashige and Skoog (MS) media supplemented with 2.0 mg/L kinetin plus 0.5 mg/L IAA was identified as the optimum in vitro regeneration media (OM). The data analysis confirmed the clonal nature of the resulting plantlets. The plantlets were also exposed to various stress factors such as high salinity, abscisic acid (ABA), and high cytokinin concentrations, by subculturing the plantlets on OM added with various concentrations of NaCl, ABA, and high kinetin levels. Exposure to the various stress factors was observed to result in the occurrence of somaclonal variation in O. stamineus, where the incidence of hyperhydricity was found to be the most prominent. An ISSR analysis revealed 70.12% polymorphism among the variants. The results showed that the chlorophyll content and photosynthetic ability of plantlets were reduced when the abiotic stress levels increased. Full article

(1) Background: Orthosiphon stamineus Benth. is a traditional medicine used in the treatment of diabetes and chronic renal failure in southern China, Malaysia, and Thailand. Diabetes is a chronic metabolic disease and the number of diabetic patients in the world is increasing. This review aimed to systematically review the effects of O. stamineus in the treatment of diabetes and its complications and the pharmacodynamic material basis. (2) Methods: This systematic review was conducted following Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA), using the databases ScienceDirect, PubMed, and Web of Science. (3) Results: Thirty-one articles related to O. stamineus and diabetes were included. The mechanisms of O. stamineus in the treatment of diabetes and its complications mainly included inhibiting α-amylase and α-glucosidase activities, antioxidant and anti-inflammatory activities, regulating lipid metabolism, promoting insulin secretion, ameliorating insulin resistance, increasing glucose uptake, promoting glycolysis, inhibiting gluconeogenesis, promoting glucagon-likepeptide-1 (GLP-1) secretion and antiglycation activity. Phenolic acids, flavonoids and triterpenoids might be the main components for hypoglycemia effects in O. stamineus. (4) Conclusion: O. stamineus could be an antidiabetic agent to treat diabetes and its complications. However, it needs further study on a pharmacodynamic substance basis and the mechanisms of effective constituents. Full article

The neuroprotective potential of Orthosiphon stamineus leaf proteins (OSLPs) has never been evaluated in SH-SY5Y cells challenged by hydrogen peroxide (H₂O₂). This work thus aims to elucidate OSLP neuroprotective potential in alleviating H₂O₂ stress. OSLPs at varying concentrations were evaluated for cytotoxicity (24 and 48 h) and neuroprotective potential in H₂O₂-induced SH-SY5Y cells (24 h). The protective mechanism of H₂O₂-induced SH-SY5Y cells was also explored via mass-spectrometry-based label-free quantitative proteomics (LFQ) and bioinformatics. OSLPs (25, 50, 125, 250, 500, and 1000 µg/mL; 24 and 48 h) were found to be safe. Pre-treatments with OSLP doses (250, 500, and 1000 µg/mL, 24 h) significantly increased the survival of SH-SY5Y cells in a concentration-dependent manner and improved cell architecture—pyramidal-shaped cells, reduced clumping and shrinkage, with apparent neurite formations. OSLP pre-treatment (1000 µg/mL, 24 h) lowered the expressions of two major heat shock proteins, HSPA8 (heat shock protein family A (Hsp70) member 8) and HSP90AA1 (heat shock protein 90), which promote cellular stress signaling under stress conditions. OSLP is, therefore, suggested to be anti-inflammatory by modulating the “signaling of interleukin-4 and interleukin-13” pathway as the predominant mechanism in addition to regulating the “attenuation phase” and “HSP90 chaperone cycle for steroid hormone receptors” pathways to counteract heat shock protein (HSP)-induced damage under stress conditions. Full article

The main challenge facing greenhouse designers is to achieve environment-appropriate greenhouses, especially in tropical regions. The excess radiant energy transmitted into the greenhouse predisposes plants to photo-inhibition and consequently reduces crop production. Lately, photovoltaic (PV) modules are equipped as a greenhouse rooftop to minimize the level of irradiation and air temperature in the greenhouse, simultaneously improving its energy consumption. Nevertheless, due to the low level of irradiation, denser conventional PV internal shading would influence the cultivated crops’ growth. Thus, Dye Sensitized Solar Cell (DSSC) possesses several attractive features such as transparent, sensitive to low light levels, and various color options that render DSSC a perfect choice able to serve substantially in energy buildings. This study assessed the microclimate conditions inside the greenhouse with semi-transparent DSSC mounted on top of it, describing the Photosynthetic Photon Flux Density (PPFD) (µmol m⁻² s⁻¹), Vapor Pressure Deficit VPD (kPa), relative humidity (%), and also temperature (°C). The Overall Thermal Transfer Value (OTTV), which indicates the average thermal energy transmission rate across the external layer of a structure envelope, is also presented. The effects of colored DSSC in altering the spectral of sunlight in reference to the Orthosiphon stamineus growth responses were determined. The information of the condition of DSSC greenhouse microclimate helps to identify the information for designing PV greenhouses and to produce income from both electric power and agronomic activity. Full article

This paper presents the field measured data of the ambient temperature profile and the heat stress occurrences directly underneath ground-mounted solar photovoltaic (PV) arrays (monocrystalline-based), focusing on different temperature levels. A previous study has shown that a 1 °C increase in PV cell temperature results in a reduction of 0.5% in energy conversion efficiency; thus, the temperature factor is critical, especially to solar farm operators. The transpiration process also plays an important role in the cooling of green plants where, on average, it could dissipate a significant amount of the total solar energy absorbed by the leaves, making it a good natural cooling mechanism. It was found from this work that the PV system’s bottom surface temperature was the main source of dissipated heat, as shown in the thermal images recorded at 5-min intervals at three sampling times. A statistical analysis further showed that the thermal correlation for the transpiration process and heat stress occurrences between the PV system’s bottom surface and plant height will be an important factor for large scale plant cultivation in agrivoltaic farms. Full article

Silver nanoparticles (AgNPs) are an interesting metal nanoparticle that can be incorporated into pharmaceutical products, including for diabetic foot ulcers as an antimicrobial agent. Green synthesis of AgNPs using plant extracts has been drawing much attention as it is simple, eco-friendly, stable, and cost-effective. This present study was performed to evaluate the potential of three Indonesian medicinal plant extracts, namely Phyllanthus niruri (PN), Orthosiphon stamineus (OS), and Curcuma longa (CL), as reducing and capping agents in the green synthesis of AgNPs, and to optimize their concentrations. Based on the yields and characteristics of the formed nanoparticles, which were analyzed using a UV-Vis spectrophotometer, particle size analyzer, scanning electron microscope, and X-ray diffractometer, Phyllanthus niruri extract at a concentration of 0.5% was concluded as the best extract in the green synthesis of AgNPs. It is thereby a prospective reducing and capping agent for further scale-up studies. Full article

The anticonvulsive potential of proteins extracted from Orthosiphon stamineus leaves (OSLP) has never been elucidated in zebrafish (Danio rerio). This study thus aims to elucidate the anticonvulsive potential of OSLP in pentylenetetrazol (PTZ)-induced seizure model. Physical changes (seizure score and seizure onset time, behavior, locomotor) and neurotransmitter analysis were elucidated to assess the pharmacological activity. The protective mechanism of OSLP on brain was also studied using mass spectrometry-based label-free proteomic quantification (LFQ) and bioinformatics. OSLP was found to be safe up to 800 µg/kg and pre-treatment with OSLP (800 µg/kg, i.p., 30 min) decreased the frequency of convulsive activities (lower seizure score and prolonged seizure onset time), improved locomotor behaviors (reduced erratic swimming movements and bottom-dwelling habit), and lowered the excitatory neurotransmitter (glutamate). Pre-treatment with OSLP increased protein Complexin 2 (Cplx 2) expression in the zebrafish brain. Cplx2 is an important regulator in the trans-SNARE complex which is required during the vesicle priming phase in the calcium-dependent synaptic vesicle exocytosis. Findings in this study collectively suggests that OSLP could be regulating the release of neurotransmitters via calcium-dependent synaptic vesicle exocytosis mediated by the “Synaptic Vesicle Cycle” pathway. OSLP’s anticonvulsive actions could be acting differently from diazepam (DZP) and with that, it might not produce the similar cognitive insults such as DZP. Full article

Alzheimer’s disease (AD) is a chronic neurodegenerative brain disease that is characterized by impairment in cognitive functioning as well as the presence of intraneuronal neurofibrillary tangles (NFTs) and extracellular senile plaques. There is a growing interest in the potential of phytochemicals to improve memory, learning, and general cognitive abilities. The Malaysian herb Orthosiphon stamineus is a traditional remedy that possesses anti-inflammatory, anti-oxidant, and free-radical scavenging abilities, all of which are known to protect against AD. Previous studies have reported that intracerebroventricular (ICV) administration of streptozotocin (STZ) mimics a condition similar to that observed in AD. This experiment thus aimed to explore if an ethanolic leaf extract of O. stamineus has the potential to be a novel treatment for AD in a rat model and can reverse the STZ- induced learning and memory dysfunction. The results of this study indicate that O. stamineus has the potential to be potentially effective against AD-like condition, as both behavioral models employed in this study was observed to be able to reverse memory impairment. Treatment with the extract was able to decrease the up-regulated expression levels of amyloid precursor protein (APP), microtubule associated protein tau (MAPT), Nuclear factor kappa-light-chain-enhancer of activated B cells (NFᴋB), glycogen synthase kinase 3 alpha (GSK3α), and glycogen synthase kinase 3 beta (GSK3β) genes indicating the extract’s neuroprotective ability. These research findings suggest that the O. stamineus ethanolic extract demonstrated an improved effect on memory, and hence, could serve as a potential therapeutic target for the treatment of neurodegenerative diseases such as AD. Full article

Seven pimarane diterpenes (1–7) were isolated from Orthosiphon stamineus Benth. by assay-guided isolation. All of the isolates possessed a 2-deoxy-2-((7-nitro-2,1,3-benzoxadiazol-4-yl)amino)-d-glucose uptake effect in 3T3-L1 adipocytes at concentrations of 5 and 10 μM. Most of them showed potent inhibition against protein tyrosine phosphatase 1B with IC₅₀ values ranging from 0.33 to 9.84 μM. In the kinetic study, all inhibition types were exposed for the examined potencies, including mixed-competitive (1), non-competitives (3 and 5), competitive (6), and uncompetitive (7). The results suggested that O. stamineus and its pimarane diterpenes might exert the hypoglycemic effect via the insulin signaling pathway targeting inhibition of protein tyrosine phosphatase 1B (PTP1B) activity. Full article

Orthosiphon stamineus has been widely used as traditional remedy for various illnesses and diseases, such as cardiovascular diseases and epileptic seizures. In this study, direct regeneration through nodal segment of this species was attempted using Kinetin (6-Furfurylaminopurine) and IAA (indole-3-acetic acid). Optimum regeneration media was identified as MS media supplemented with 2.0 mg L⁻¹ Kin plus 0.5 mg L⁻¹ IAA. This yielded the highest number of shoots (5.57 ± 0.42) and leaves (20.53 ± 1.91) per explant. Acclimatization of the resulting in vitro regenerants was successful in all potting mixtures tested. However, potting mixture PF (1:1:1 ratio of black soil/red soil/compost) was identified as the best medium for acclimatization of this species, as it yielded 100% survival percentage after 90 days of acclimatization. Ten in vitro regenerants of O. stamineus were randomly collected after the third subculture and subjected to genetic variation analysis using inter-simple sequence repeat (ISSR) markers. Out of 20 ISSR markers tested, 10 working primers were observed to produce satisfactory amplification of bands, with an average of 7.11 bands per primer. A total of 610 bands were produced by the 10 primers. The percentage of polymorphism was observed to be very low, yielding only 7.32% polymorphism among all samples. Jaccard dissimilarity analysis was also conducted and very low genetic distance (about 0.1) was found among the in vitro regenerants and between the regenerants with the mother plant, thus ascertaining the clonal nature of the plantlets produced in this study. Full article

Primarily, optimization of ultrasonic-assisted extraction (UAE) conditions of Orthospihon stamineus was evaluated and verified using a central composite design (CCD) based on three factors including extraction time (minutes), ultrasound amplitude (A), and solvent concentration (%). The response surface methodology (RSM) was performed to develop an extraction method with maximum yield and high rosmarinic acid content. The optimal UAE conditions were as follows: extraction time 21 min, ultrasound amplitudes 62 A, and solvent composition 70% ethanol in water. The crude extract was further fractionated using solid-phase extraction (SPE), where six sequential fractions that varied in polarity (0–100% Acetonitrile in water) were obtained. Next, the six fractions were evaluated for their antioxidant and anti-cancer properties. This study found that Fraction 2 (F2) contained the highest rosmarinic acid content and showed the strongest antioxidant activity. Additionally, F2 showed an anti-proliferative effect against prostate cancer (DU145) with no harmful effect on normal cells. Full article

Orthosiphon stamineus Benth. (OS) is a traditional folk medicine for the treatment of kidney stones and other urinary tract diseases. In this study, a rapid and sensitive Ultra high-performance liquid chromatography (UHPLC)-MS/MS approach was established and validated for the simultaneous quantification of nine bioactive components in rat plasma. The nine components from OS extract detected in rat plasma were danshensu, protocatechuic acid, caffeic acid, rosmarinic acid, salvianolic acid A, salvianolic acid B, cichoric acid, sinensetin and eupatorin. After liquid-liquid extraction with ethyl acetate, the plasma samples were subjected to a triple quadrupole mass spectrometer employing electrospray ionization (ESI) technique and operating in multiple reaction monitoring (MRM) with both positive and negative ion modes. The standard curves showed good linear regression (r > 0.9915) over the concentration range for the nine analytes. The inter-day and intra-day precision and accuracy were found to be within 15% of the nominal concentration. The recovery and stability of nine compounds were all demonstrated to be within acceptable limits. The approach was successfully applied to investigate the pharmacokinetic analysis of the nine bioactive components after oral administration of OS extract in rats. Full article