Popular Herbal Supplements Research Articles

Short-Term Panax Ginseng Extract Supplementation Reduces Fasting Blood Triacylglycerides and Oxygen Consumption during Sub-Maximal Aerobic Exercise in Male Recreational Athletes.

Ginseng, a popular herbal supplement among athletes, is believed to enhance exercise capacity and performance. This study investigated the short-term effects of Panax ginseng extract (PG) on aerobic capacity, lipid profile, and cytokines. In a 14-day randomized, double-blind trial, male participants took 500 mg of PG daily. Two experiments were conducted: one in 10 km races (n = 31) and another in a laboratory-controlled aerobic capacity test (n = 20). Blood lipid and cytokine profile, ventilation, oxygen consumption, hemodynamic and fatigue parameters, and race time were evaluated. PG supplementation led to reduced total blood lipid levels, particularly in triacylglycerides (10 km races -7.5 mg/dL (95% CI -42 to 28); sub-maximal aerobic test -14.2 mg/dL (95% CI -52 to 23)), while post-exercise blood IL-10 levels were increased (10 km 34.0 pg/mL (95% CI -2.1 to 70.1); sub-maximal aerobic test 4.1 pg/mL (95% CI -2.8 to 11.0)), and oxygen consumption decreased during the sub-maximal aerobic test (VO2: -1.4 mL/min/kg (95% CI -5.8 to -0.6)). No significant differences were noted in race time, hemodynamic, or fatigue parameters. Overall, PG supplementation for 2 weeks showed benefits in blood lipid profile and energy consumption during exercise among recreational athletes. This suggests a potential role for PG in enhancing exercise performance and metabolic health in this population.

Polyphenolic Characterization and Anti-Inflammatory Effect of In Vitro Digested Extracts of Echinacea purpurea L. Plant Parts in an Inflammatory Model of Human Colon Cells.

Echinacea purpurea L. (EP) preparations are globally popular herbal supplements known for their medicinal benefits, including anti-inflammatory activities, partly related to their phenolic composition. However, regarding their use for the management of inflammation-related intestinal diseases, the knowledge about the fate of orally ingested constituents throughout the human gastrointestinal tract and the exposition of in vitro digested extracts in relevant inflammatory models are unknown. This study investigated for the first time the impact of in vitro gastrointestinal digestion (INFOGEST) on the phenolic composition and anti-inflammatory properties of EP extracts from flowers (EF), leaves (EL), and roots (ER) on IL-1β-treated human colon-derived CCD-18Co cells. Among the seven hydroxycinnamic acids identified using HPLC-UV-MS/MS, chicoric and caftaric acids showed the highest concentrations in EL, followed by EF and ER, and all extracts exerted significant reductions in IL-6, IL-8, and PGE2 levels. After digestion, despite reducing the bioaccessibility of their phenolics, the anti-inflammatory effects were preserved for digested EL and, to a lesser extent, for EF, but not for digested ER. The lower phenolic content in digested EF and ER could explain these findings. Overall, this study emphasizes the potential of EP in alleviating intestinal inflammatory conditions and related disorders.

Effect of Ginseng Intake on Muscle Damage Induced by Exercise in Healthy Adults.

One of the most popular herbal supplements in the world is ginseng. Several studies have evaluated the capacity of ginseng as a protective element in the physiological response to exercise. The result produced by the exercise causes an increase in cellular biomarkers of damage in the skeletal muscle, mainly in the pro-inflammatory types. The different types of ginseng are composed of ginsenosides, which are active ingredients that act on the central nervous system and have antioxidant and anti-inflammatory properties, as well as effects on cortisol modulation. The use of ginseng as a nutritional supplement can help muscle regeneration and renewal. The objective of this review is to enrich the knowledge regarding the consumption of ginseng for a specific situation, such as exercise, which would cause an improvement in the tolerance to chronic load stimuli in sport, thus helping the subjects to recover between training sessions. Due to these benefits, it could also be an ideal food supplement for regenerative processes in muscle injuries in which inflammatory markers increase significantly. This review aims to summarise that biological factors can be attenuated after exercise due to the consumption of ginseng in healthy subjects, accelerating and improving muscle regeneration and, therefore, improving the ability to adapt to the stimuli generated by said exercise.

A Comparative Study on Analysis of Ginsenosides in American Ginseng Root Residue by HPLC-DAD-ESI-MS and UPLC-HRMS-MS/MS.

Ginseng (Panax quinquefolius), a popular herbal and nutritional supplement consumed worldwide, has been demonstrated to possess vital biological activities, which can be attributed to the presence of ginsenosides. However, the presence of ginsenosides in ginseng root residue, a by-product obtained during processing of ginseng beverage, remains unexplored. The objectives of this study were to develop a high-performance liquid chromatography-photodiode array detection-mass spectrometry (HPLC-DAD-ESI-MS) and an ultra-high-performance-liquid-chromatography-tandem mass spectrometry (UPLC-HRMS-MS/MS) method for the comparison of ginsenoside analysis in ginseng root residue. Results showed that by employing a Supelco Ascentis Express C18 column (150 × 4.6 mm ID, particle size 2.7 μm) and a gradient mobile phase of deionized water and acetonitrile with a flow rate at 1 mL/min and detection at 205 nm, a total of 10 ginsenosides, including internal standard saikosaponin A, were separated within 18 min and detected by HPLC-DAD-ESI-MS. Whereas with UPLC-HRMS-MS/MS, all the 10 ginsenosides were separated within six minutes by using an Acquity UPLC BEH C18 column (50 × 2.1 mm ID, particle size 1.7 μm, 130 Å) and a gradient mobile phase of ammonium acetate and acetonitrile with column temperature at 50 °C, flow rate at 0.4 mL/min and detection by selected reaction monitoring (SRM) mode. High accuracy and precision was shown, with limit of quantitation (LOQ) ranging from 0.2–1.9 μg/g for HPLC-DAD-ESI-MS and 0.269–6.640 ng/g for UPLC-HRMS-MS/MS. The contents of nine ginsenosides in the ginseng root residue ranged from <LOQ-26.39 mg/g by HPLC-DAD-ESI-MS and <LOQ-21.25 mg/g by UPLC-HRMS-MS/MS, with a total amount of 38.37 and 34.71 mg/g, respectively.

Safety concerns of dietary and herbal supplements for typical patients

The global dietary cum herbal supplements market crossed 140 billion U.S. dollars in 2020 already. Hence, it is evident that the supplements market is growing very fast globally, including India, one of the best potential markets. Market and marketing are always good for a country’s better economy, but safety management is more critical, while health is a concern. This study aims to assess and understand the various safety concerns of dietary cum herbal supplements available globally, where India has focussed more. Some countries believe in the natural products often consumed as supplements without knowing their indications, contraindications, and drug interactions. Hence, this article was written to understand consumers’ and typical patients’ supplements consumption behaviors irrespective of authors’ perception. Easy keywords and phrases such as ‘common dietary supplements,’ ‘popular herbal supplements,’ ‘indications and contraindication of supplements’ were used for the online searches. Many physicians, dietitians, and medical scientists have already shown the adverse effects of some supplements in pregnancy, lactation, and other critical conditions. Still, on the other hand, there are some positive effects in the chronic health issues, including skin and hair health issues, poor immunity, gastric problems, undernutrition. Selective supplements can also help post-operative recovery, muscle, bone, cognitive development, vitamin deficiency, endocrine disorders, and many more. The study has emphasized the government policies and regulations as applicable irrespective of the country. India is the 2 population-based country globally; hence more vigilance is needed at every level of supplement business for public health safety. Moreover, all authors have put their valuable summary that more awareness is required about indications and contraindications of various types of supplements, particularly for typical patients. It’s not only doctors’ or dietitians’ job but everyone’s concern.

Target profiling of flavonol glycosides in the extract of Ginkgo biloba leaf and their pharmacokinetics in rat plasma by ultra‐high‐performance liquid chromatography with tandem mass spectrometry

The extract of Ginkgo biloba leaf is a popular herbal product or dietary supplement in the world to treat various diseases, and flavonol glycosides are considered as the main bioactive constituents. In this study, 37 flavonol glycosides were rapidly screened out by precursor ion scanning in positive ion mode with production ions at m/z 287.05, 303.05, and 317.06. Subsequently, a reliable and sensitive ultra-high-performance liquid chromatography coupled with triple quadrupole-linear ion trap mass spectrometry approach was established and validated to quantify the 20 prototype flavonol glycosides in rat plasma. Calibration curves showed good linearity (R2 ≥ 0.9894) over the corresponding concentration range. The precision, accuracy, extraction recovery, matrix effect, and stability were also satisfactory. The validated method was successfully applied to a pharmacokinetic study of prototype flavonol glycosides in rat after oral administration of the extract of G. biloba leaf. As a result, the Tmax of flavonol glycosides was short at 0.11-0.60 h. Quercetin-3-O-(2",6″-di-O-rhamnosyl)-glucoside, kaempferol-3-O-(2'',6''-di-O-rhamnosyl)-glucoside, quercetin-3-O-rutinoside, quercetin- 3-O-glucosyl-(1-2)-O-rhamnoside, and kaempferol-3-O-glucoside presented relatively high systemic exposure levels with AUC0-∞ >500 μg h/L and Cmax >100 μg/L. This study would provide the valuable information for further scientific research and clinical application of the extract of G. biloba leaf.

Authentication of garlic (Allium sativum L.) supplements using a trnLUAA mini-barcode.

Garlic (Allium sativum), a widely distributed plant with great cultural and medicinal significance, is one of the most popular herbal dietary supplements in Europe and North America. Garlic supplements are consumed for a variety of reasons, including for their purported antihypertensive, antibacterial, and anticarcinogenic effects. The steady increase in the global herbal dietary supplement market paired with a global patchwork of regulatory frameworks makes the development of assays for authentication of these products increasingly important. A DNA mini-barcode assay was developed using the P6 loop of the plastid trnLUAA intron to positively identify A. sativum products. Analysis of 43 commercially available garlic herbal dietary supplements produced mini-barcode sequences for 33 supplements, all of which contained detectable amounts of A. sativum. The trnLUAA P6 mini-barcode can be highly useful for specimen identification, particularly for samples that may contain degraded DNA.

Attenuation of doxorubicin-induced oxidative damage in rat brain by regulating amino acid homeostasis with Astragali Radix.

The nervous system disorders caused by doxorubicin (DOX) are among the severe adverse effects that dramatically reduce the quality of life of cancer survivors. Astragali Radix (AR), a popular herbal drug and dietary supplement, is believed to help treat brain diseases by reducing oxidative stress and maintaining metabolic homeostasis. Here we show the protective effects of AR against DOX-induced oxidative damage in rat brain via regulating amino acid homeostasis. By constructing a clinically relevant low-dose DOX-induced toxicity rat model, we first performed an untargeted metabolomics analysis to discover specific metabolic features in the brain after DOX treatment and AR co-treatment. It was found that the amino acid (AA) metabolism pathways altered most significantly. To accurately characterize the brain AA profile, we established a sensitive, fast, and reproducible hydrophilic interaction chromatography-tandem mass spectrometry method for the simultaneous quantification of 22 AAs. The targeted analysis further confirmed the changes of AAs between different groups of rat brain. Specifically, the levels of six AAs, including glutamate, glycine, serine, alanine, citrulline, and ornithine, correlated (Pearson |r| > 0.47, p < 0.05) with the brain oxidative damage that was caused by DOX and rescued by AR. These findings present that AAs are among the regulatory targets of DOX-induced brain toxicity, and AR is a promising therapeutic agent for it.

Molecular Docking Evaluation of Some Indonesian’s Popular Herbals for a Possible COVID-19 Treatment

Indonesia’s rich tropical biodiversity offers many possible options for fighting the unprecedented outbreak of coronavirus disease 2019 (COVID-19). In this paper, we evaluate the in silico (molecular docking) performance of some popular herbal supplements and natural remedies, which are usually consumed by Indonesian people and compare them to the docking performance of the control ligand (N3 inhibitor) and some protease-inhibitor drugs. The tested active compounds were grouped based on their popularity in the market, i.e., honey, black seed (Nigella sativa), Javanese turmeric (Curcuma xanthorriza roxb), and mangosteen, which usually served in the form of encapsulated oil or powder. The results show that most of the tested active compounds perform better than N3 inhibitor and protease inhibitor drugs (lopinavir and darunavir) in inhibiting the main protease of SARS-CoV-2 virus of COVID-19 (C19MP). Based on the combined scores of binding affinity, the similarity of active sites (SAS), and the drug-likeness properties of the ligand, gamma mangostin turns out to be the best possible C19MP inhibitor as compared to other ligands. The active site analysis also reveals that His41, Met49, Leu141, and Asn142 are among the most important amino acids that play a significant role in the protein-ligand binding due to their frequent occurrence in the docking simulation.

Application of Cryopreserved Human Intestinal Mucosa and Cryopreserved Human Enterocytes in the Evaluation of Herb-Drug Interactions: Evaluation of CYP3A Inhibitory Potential of Grapefruit Juice and Commercial Formulations of Twenty-Nine Herbal Supplements.

Commercial formulations of 29 commonly used herbal supplements (HSs) and grapefruit juice were evaluated for drug interaction potential via quantification of their CYP3A inhibitory potential in two in vitro experimental models of human small intestine, cryopreserved human intestinal mucosa (CHIM), and cryopreserved human enterocytes (CHEs). Two CYP3A substrates were used-in the studies with CHIM, CYP3A activity was quantified via liquid chromatography tandem mass spectrometry quantification of midazolam 1'-hydroxylation, whereas in CHE, luciferin-IPA metabolism to luciferin was quantified by luminescence. Upon treatment of CHIM with the estimated lumen concentration of the HS upon each oral administration (manufacturers' recommended dosage dissolved in 200 ml of culture medium), >80% CYP3A inhibition was observed for green tea extract, St. John's wort, valerian root, horehound, and grapefruit juice. Less than 50% inhibition was observed for fenugreek, aloe vera, guarana, soy isoflavone, maca, echinacea, spirulina, evening primrose, milk thistle, cranberry, red yeast rice, rhodiola, ginkgo biloba, turmeric, curcumin, white kidney bean, garlic, cinnamon, saw palmetto berries, panax ginseng, black elderberry, wheat grass juice, flaxseed oil, black cohosh, and ginger root. The results were confirmed in a a dose-response study with HSs obtained from three suppliers for the four inhibitory HSs (green tea extract, horehound, St. John's wort, valerian root) and three representative noninhibitory HSs (black cohosh, black elderberry, echinacea). Similar results were obtained with the inhibitory HSs in CHE. The results illustrate that CHIM and CHE represent physiologically relevant in vitro experimental models for the evaluation of drug interaction potential of herbal supplements. Based on the results, green tea extract, horehound, St. John's wort, and valerian root may cause drug interactions with orally administered drugs that are CYP3A substrates, as was observed for grapefruit juice. SIGNIFICANCE STATEMENT: In vitro evaluation of 29 popular herbal supplements in cryopreserved human intestinal mucosa identified green tea extract, horehound, St. John's wort, and valerian root to have CYP3A inhibitory potential similar to that for grapefruit juice, suggesting their potential to have clinically significant pharmacokinetic interaction with orally administered drugs that are CYP3A substrates. The results suggest that cryopreserved human intestinal mucosa can be used for in vitro evaluation of drug interactions involving enteric drug metabolism.

Dietary Interventions to Prevent or Delay Alzheimer's Disease: What the Evidence Shows.

A variety of potentially modifiable risk factors have been investigated in an attempt to delay/prevent Alzheimer's disease (AD). Among these, dietary regimens and nutritional supplements have been most extensively studied. The purpose of this article is to critically review recent evidence for the Mediterranean/MIND diets along with the use of various vitamins and popular herbal supplements, including curcumin, Ginkgo biloba, and fish oil, among others. The Mediterranean and MIND diets are supported by observational studies performed in community settings, especially in the group with high adherence to the Mediterranean diet and with moderate-high adherence to the MIND diet. Randomized controlled trials of various vitamins and supplements have, in general, not shown statistically significant results, although there has been some promising evidence for vitamin D supplementation and curcumin use. There is sufficient data to recommend the Mediterranean and MIND diets to delay the onset of AD. It is judicious to supplement vitamin D, especially in deficient patients, and to consider the use of curcumin to improve cognitive performance. Future research should focus on larger, controlled trials in diverse populations.

Toxicity of Panax genseng - An herbal medicine and dietary supplement

Ginseng is one of the most popular herbal dietary supplements in the U.S. market, with five to six million persons using it even before the recent boom in the herbal supplement industry. Ginsana (G115 ginseng), a standardized extract of Panax ginseng (Asian ginseng, also called Chinese or Korean ginseng) controls half of this market. Numerous reports of adverse effects from products containing ginseng have been filed with the U.S. Food and Drug Administration (FDA). The literature also documents "ginseng abuse syndrome" among regular users. The chronic effects of ginseng are not well characterized. Because of its significant human exposure and little information on toxicity is available, Panax ginseng has been nominated by the U.S. National Institutes of Health (NTH) to the U.S. National Toxicology Program (NTP) for assessing its carcinogenic potential. In this review, we discuss the environmental occurrence, purported therapeutic effects, biological effects, and toxicity of ginseng, with focus on Panax ginseng. To demonstrate how NTP chronic tumorigenicity bioassays are conducted, the turnorigenicity bioassay of Panax ginseng is detailed described.

Govanoside B, a new steroidal saponin from rhizomes of Trillium govanianum

Trillium govanianum, commonly known as Nag Chhatri and Teen Patra, is a popular herbal supplement traditionally used for curing different inflammatory and sexual disorders, infection and wound healing. Steroidal saponins are considered as active components of this species. The present study demonstrated the isolation of nine steroidal saponins, including one new compound named as govanoside B (9) and eight known, pregna-chacotrioside (1), pennogenin-triglycoside (2), borassoside E (3), pennogenin-tetraglycoside (4), protodioscin (5), clintonioside B (6), pennogenin-diglycoside (7) and borassoside D (8). This is the first report on the isolation of 1, 2, 4, 5, 6, 7 and 8 from rhizomes of T. govanianum. The extract, fractions and isolated compounds were further evaluated for their DPPH and ABTS radical scavenging activity.

Effects of Gut Microbiota on the Bioavailability of Bioactive Compounds from Ginkgo Leaf Extracts.

Ginkgo leaf extract (GLE) is a popular herbal medicine and dietary supplement for the treatment of various diseases, including cardiovascular disease. GLE contains a variety of secondary plant metabolites, such as flavonoids and terpenoids, as active components. Some of these phytochemicals have been known to be metabolized by gut microbial enzymes. The aim of this study was to investigate the effects of the gut microbiota on the pharmacokinetics of the main constituents of GLE using antibacterial-treated mice. The bilobalide, ginkgolide A, ginkgolide B, ginkgolide C, isorhamnetin, kaempferol, and quercetin pharmacokinetic profiles of orally administered GLE (600 mg/kg), with or without ciprofloxacin pretreatment (150 mg/kg/day for 3 days), were determined. In the antibacterial-treated mice, the maximum plasma concentration (Cmax) and area under the curve (AUC) of isorhamnetin were significantly (p < 0.05) increased when compared with the control group. The Cmax and AUC of kaempferol and quercetin (other flavonol glycosides) were slightly higher than those of the control group, but the difference was not statistically significant, while both parameters for terpenoids of GLE showed no significant difference between the antibacterial-treated and control groups. These results showed that antibacterial consumption may increase the bioavailability of isorhamnetin by suppressing gut microbial metabolic activities.

The Secrets in the Leaves: Memory Retention in C. elegans

A mutant strain of Caenorhabditis elegans overexpresses a protein, amyloid precursor‐like protein (APL‐1), that is similar to the human amyloid precursor protein (APP) linked to early‐onset Alzheimer's disease (AD). AD is characterized by amyloid plaques which accumulate and contribute to the progressive neurodegeneration. The mutant strain of C. elegans (ynIs‐79) overexpresses APL‐1 specifically in neurons. Overexpression in C. elegans causes molting issues, motor dysfunction, and disrupts morphogenesis in the nematode. Ginkgo biloba (GB) extract is a popular herbal supplement which may delay or improve the memory problems associated with AD. We hypothesize that individual flavonoids, like quercetin, are likely to be the positive contributing factors because of known protective roles in preventing oxidative stress. After purifying an extract from GB leaves, we determined the concentration of quercetin using HPLC analysis and then using a standard analytical grade solution of quercetin we applied a similar concentration to both the mutant and wild type C. elegans strains. Anterior and posterior tap habituation was used to determine the ability of each stain to recognize a nonthreatening stimulus. We expected that exposing the mutant nematodes to quercetin would decrease the number of taps needed for habituation, and our results show a significant decrease, suggesting increased memory retention and rescue of neurodegenerative dysfunction for the ynIs‐79 strain.Support or Funding InformationGail Dillard Faculty Development FundThis abstract is from the Experimental Biology 2019 Meeting. There is no full text article associated with this abstract published in The FASEB Journal.

Quantification of natural products in herbal supplements: A combined NMR approach applied on goldenseal

Authentication of natural products is of major relevance in the context of manufactured drugs or herbal supplements since such active products generate a lucrative market. The analytical method to identify and quantify valuable natural products is critical for quality control and product assignment of herbal supplements. In this framework, we propose to apply a recently developed quantitative 2D NMR approach called Q QUIPU (Quick QUantItative Perfected and pUre shifted) in combination with 1D 1H NMR capable to access the concentration of three major alkaloids, berberine, β-hydrastine and canadine, in the root extract of goldenseal (Hydrastis canadensis), one of the 20 most popular herbal supplements used worldwide. We highlight the complementarity of 1D and 2D quantitative NMR to accurately assess the amount of alkaloids with different range of concentrations and stability within extracts. In particular, unstable natural products having non-overlapped signals like berberine could only be quantified by sensitive and fast 1D 1H, while overlapped signals of β-hydrastine and low intense ones of canadine could only be quantified with the recent 2D Q QUIPU HSQC.Results obtained from this combined approach have led to a good accuracy (<10%) as compared with coupled UHPLC-MS/UV techniques. This quantitative NMR approach paves the way to numerous applications where the accurate quantification of targeted compounds in complex mixtures is required, for instance in agricultural, food and pharmaceuticals products.

Oral curcumin in elective abdominal aortic aneurysm repair: a multicentre randomized controlled trial.

Curcumin, a popular herbal supplement from the plant turmeric, has prevented ischemic reperfusion and toxin-induced injury in many animal studies and a single-centre randomized human trial. We sought to test whether perioperative oral curcumin (compared with placebo) affects the inflammatory response and risk of postrepair complications after elective abdominal aortic aneurysm repair in humans. We conducted a parallel-group, randomized, placebo-controlled trial of patients from 10 hospitals in Canada who were scheduled to undergo elective repair of an unruptured abdominal aortic aneurysm (November 2011 to November 2014). Patients in the treatment group received perioperative oral curcumin (2000-mg doses 8 times over 4 d). Patients, health care providers and local research staff were unaware of the treatment assignment. The primary outcomes were median concentrations of 4 bio markers indicating injury and inflammation (postoperative urine interleukin-18 and perioperative rise in serum creatinine, plasma N-terminal pro-B-type natriuretic peptide and plasma high-sensitivity C-reactive protein). Baseline characteristics were similar in the 2 groups (606 patients overall; median age 76 yr). More than 85% of patients in each group took more than 80% of their scheduled capsules. Neither curcumin nor placebo significantly affected any of the 4 biomarkers (p > 0.05 for all comparisons). Regarding the secondary outcomes, there was a higher risk of acute kidney injury with curcumin than with placebo (17% v. 10%, p = 0.01), but no between-group difference in the median length of hospital stay (5 v. 5 days, p > 0.9) or the risk of clinical events (9% v. 9%, p = 0.9). Curcumin had no beneficial effects when used in elective abdominal aortic aneurysm repair. These findings emphasize the importance of testing turmeric and curcumin before espousing their health benefits, as is currently done in the popular media. ClinicalTrials.gov, no. NCT01225094.

Orthosiphon stamineus (Misai Kucing) ameliorated postmenopausal osteoporosis in rat model.

Orthosiphon stamineus (OS) or Misai Kucing (Java tea) is a popular herbal supplement from Southeast Asia for various metabolic, age-related diseases. This study investigated the potential use of OS leaf extracts to ameliorate osteoporosis in ovariectomized rats. Fifty-six female Sprague-Dawley rats were randomly allocated into eight groups (n = 7): SHAM (healthy sham control); OVX (ovarietomized) nontreated rats (negative control); OVX + Remifemin (100 mg/kg body weight), and 2% green tea extract (positive controls); OVX + OS 50% ethanolic and aqueous extracts, both at either 150 or 300 mg/kg. After 16 weeks, the rats' bones and blood were evaluated for osteoporosis indicators (protein and mRNA expressions), micro-computed tomography for bone histomorphometry, and three-point bending test for tibia mechanical strength. The extracts dose-dependently and significantly (P < 0.05) improved bone strength and flexibility, bone mineral density, bone formation protein markers (P1NP), and bone histomorphometry. All extracts reduced the inflammation biomarker (interleukin-6). The extracts up-regulated osteoblastogenesis (bone morphogenetic protein-2) and collagen-1 synthesis (collagen type 1 alpha-1) mRNA expressions, and down-regulated bone resorption (TNFSF11 and nuclear factor-kappa B) mRNA expressions. Both the water and 50% ethanolic extract were effective. The effective dose is equivalent to 25 to 50 mg/kg extract for humans. The extract showed bone-protective and antiosteoporotic effects (improving bone strength, flexibility, bone density, and bone morphometry) by reducing inflammation and the bone resorption biomarkers, while enhancing bone formation biomarkers and collagen synthesis.

Authentication of Eleutherococcus and Rhodiola herbal supplement products in the United Kingdom

Siberian ginseng (Eleutherococcus senticosus, Araliaceae) and roseroot (Rhodiola rosea, Rosaceae) are popular herbal supplements which have been shown to improve resilience to conditions such as stress and exhaustion. Using DNA barcoding methods we tested 25 Siberian ginseng and 14 roseroot products which are widely available to UK customers to test whether the herbal ingredient stated on the label is also in the product. All Siberian ginseng supplements contained E. senticosus, however, 36% also contained an Eleutherococcus species other than E. senticosus. In three out of the 13 roseroot products which produced amplifiable DNA, we could only retrieve sequences matching alfalfa (declared on the product label) and fenugreek (not declared). In the other 10 supplements Rhodiola was detected but only five matched the target species R. rosea. As DNA can get severely degraded during the manufacturing process we did not take the absence of Rhodiola DNA as proof for a compromised product. Contamination could explain the presence of non-target species such as fenugreek but is unlikely to be account for the detection of congeneric Rhodiola species in roseroot preparations. Our results therefore suggest that the substitution or mixing of the target medicinal ingredient in these two popular supplements with other species is common.

Stauntonia hexaphylla (Lardizabalaceae) leaf methanol extract inhibits osteoclastogenesis and bone resorption activity via proteasome-mediated degradation of c-Fos protein and suppression of NFATc1 expression.

BackgroundNatural plants, including common vegetables and fruits, have been recognized as essential sources for drug discovery and the development of new, safe, and economical medicaments. Stauntonia hexaphylla (Lardizabalaceae) is widely distributed in Korea, Japan, and China, and is a popular herbal supplement in Korean and Chinese folk medicine owing to its analgesic, sedative, and diuretic properties. However, the exact pharmacological effects of S. hexaphylla extract, particularly its effect on osteoclastogenesis, are not known.MethodsOsteoclast differentiation and function were identified with tartrate-resistant acid phosphatase (TRAP) staining and bone resorption assay, and the underling mechanisms were determined by real-time RT-PCR and western blot analysis.ResultsS. hexaphylla was found to inhibit early-stage receptor activator of nuclear factor-κB (NF-κB) ligand (RANKL)-mediated osteoclast differentiation in bone marrow macrophages (BMMs) without cytotoxicity and bone-resorbing activity in mature osteoclasts in a dose-dependent manner. This S. hexaphylla-mediated blockade of osteoclastogenesis involved abrogation of the NF-κB, ERK, and c-Src-Btk-PLCγ2 calcium signal pathways. Interestingly, we found that S. hexaphylla down-regulated RANKL-associated c-Fos protein induction by suppressing its translation. Furthermore, ectopic overexpression of c-Fos and NFATc1 rescued the inhibition of osteoclast differentiation by S. hexaphylla. Furthermore, S. hexaphylla inhibited the c-Fos- and NFATc1-regulated expression of genes required for osteoclastogenesis, such as TRAP, OSCAR, β3-integrin, ATP6v0d2, and CtsK.ConclusionsThese findings suggest that S. hexaphylla might be useful for the development of new anti-osteoporosis agents.