A polyphenol fraction from Rosa multiflora var. platyphylala reduces body fat in overweight humans through appetite suppression - a randomized, double-blind, placebo-controlled trial.

BACKGROUND: Rosa species are rich sources of polyphenols with physiological functions. In this study a polyphenol-rich Rosa multiflora (var. platyphylala) petal extract (RoseFit™) was investigated for weight loss in humans. METHODS: In a randomized, placebo-controlled, parallel-group, double-blind clinical trial seventy overweight male and female subjects (20-50 years) with body mass index (BMI) 25-30 kg/m2 were randomly allocated to the active treatment group (RoseFit) and placebo group in a 1:1 ratio. The subjects received 300 mg capsules twice daily for 12 weeks. The primary efficacy outcome measures included body weight, BMI, and body composition, as determined using Dual-energy X-ray absorptiometry (DEXA). Secondary measures consisted of serum lipid profile and appetite marker (leptin and ghrelin) analyses. Safety analyses included biochemical and hematological assessments. RESULTS: At the end of the study, a marked reduction in body weight (-1.20 ± 2.62 kg, p < 0.05) and BMI from baseline was observed in the RoseFit group. In addition, the body fat % (RoseFit = -1.69 ± 2.59%, placebo = 0.96 ± 3.21%; p < 0.001) and fat mass (RoseFit = -1.75 ± 1.80 kg, placebo = 1.61 ± 3.82 kg; p < 0.001) were significantly abated in RoseFit group. Importantly, the lean mass was maintained during the intervention. RoseFit ingestion significantly increased the serum leptin levels compared to the placebo (4.85%; p < 0.05). Further, RoseFit group showed reduction in the hunger hormone ghrelin level (2.27%; p < 0.001) from baseline to the end of study, compared to the placebo. The subjective evaluation of appetite using visual analog scale (VAS) questionnaires further confirmed the appetite-suppression effects of RoseFit. The lipid profile significantly improved in RoseFit-treated subjects. No serious adverse events were observed during the study, indicating the tolerability of RoseFit. CONCLUSIONS: Supplementation with RoseFit significantly impacts body weight management and can thus be a potential nutraceutical ingredient for sustainable weight loss. TRIAL REGISTRATION: CTRI/2019/10/021584 dated 09/10/2019.

Oral and Topical Administration of a Standardized Saw Palmetto Oil Reduces Hair Fall and Improves the Hair Growth in Androgenetic Alopecia Subjects - A 16-Week Randomized, Placebo-Controlled Study.

Purpose: Androgenetic alopecia (AGA) is the most common type of hair loss in humans, affecting self-esteem and emotional well-being. This study aimed to assess the safety and efficacy of VISPOTM, a standardized saw palmetto oil (2-3% ß-sitosterol), in subjects with mild-to-moderate AGA. Methods: In a double-blind, placebo-controlled, four-arm clinical study, 80 healthy male and female subjects aged 18-50 years were randomly allocated (1:1:1:1) to receive either 400 mg capsules of VISPO or 5 mL of a topical formulation containing 20% VISPO or the respective placebo once daily for 16 weeks. The primary endpoints included hair count (hair comb and hair pull tests) and the self-assessment of perceived efficacy. Objective evaluation was performed using the global photographic assessment score. Hair density, thickness, and anagen/telogen ratio were evaluated using phototrichogram analysis. Results: At the end of the study, oral and topical formulations of VISPO reduced hair fall by up to 29% (p<0.001) and 22.19% (p<0.01) from the baseline, respectively. Hair density increased by 5.17% and 7.61% in the oral and topical VISPO groups, respectively (p<0.001). In addition, oral ingestion of VISPO resulted in a marked reduction in serum dihydrotestosterone (DHT) levels in the subjects compared to placebo (p<0.001). However, the effect of the VISPO formulations on the anagen/telogen ratio was insignificant. No serious adverse effects were observed during the study. Conclusion: VISPO formulations reduced hair fall and promoted hair regrowth and scalp appearance in AGA patients.

A standardized extract of Echinacea purpurea containing higher chicoric acid content enhances immune function in murine macrophages and cyclophosphamide-induced immunosuppression mice.

CONTEXT: Preparations of Echinacea have been used by herbalists to boost the immune system. OBJECTIVE: In this study, Echinacea purpurea (L.) Moench (Asteraceae) extract with enriched chicoric acid content was investigated for immunomodulation. MATERIALS AND METHODS: The standardized hydroalcoholic extract (4% chicoric acid) was prepared from the aerial parts of E. purpurea (SEP). The extract was screened for in vitro antioxidant activities, and immunomodulation in RAW 264.7 cells, at 200 and 400 µg/mL. Further, the male BALB/c mice (20-25 g) were divided into 4 groups (n = 6 per group). All the groups except control, were intraperitoneally injected with 70 mg/kg/day of cyclophosphamide (CTX) for 4 consecutive days. The treatment groups received SEP extract (100 and 200 mg/kg body weight) p.o. from day 5 to 14. RESULTS: The SEP extract inhibited DPPH (IC50 = 106.7 µg/mL), ABTS+ (IC50 = 19.88 µg/mL) and nitric oxide (IC50 = 120.1 µg/mL). The SEP extract's ORAC (oxygen radical absorbance capacity) value was 1931.63 µM TE/g. In RAW 264.7 cells, SEP extract increased the nitric oxide production by 30.76- and 39.07-fold at 200 and 400 µg/mL, respectively, compared to the untreated cells. SEP extract significantly increased phagocytosis and cytokine release (TNF-α, IL-6, and IL-1ß) in the cells. Further, the extract improved immune organ indices, lymphocyte proliferation and serum cytokine levels in CTX-induced mice. The extract at 200 mg/kg significantly increased the natural killer cell activity (24.6%) and phagocytic index (28.03%) of CTX mice. CONCLUSION: Our results strongly support SEP extract with 4% chicoric acid as a functional ingredient for immunomodulation.

Aframomum melegueta Seed Extract with Standardized Content of 6-Paradol Reduces Visceral Fat and Enhances Energy Expenditure in Overweight Adults - A Randomized Double-Blind, Placebo-Controlled Clinical Study.

Purpose: Aframomum melegueta (grains of paradise) seeds have been demonstrated to possess thermogenic potential. However, it is necessary to validate the functional attributes of A. melegueta seed extract in human subjects. Methods: In a double-blind, placebo-controlled clinical trial design, we have examined the thermogenic effects of a standardized A. melegueta seed extract (AfperFit). A total of 70 overweight male and female subjects (BMI ≥25.0 to ≤30.0 kg/m2) aged 20-50 years were enrolled and administered with either 250 mg of AfperFit or placebo in capsule form twice daily for 12 weeks. The primary efficacy endpoints included energy expenditure (indirect calorimetry), body composition (dual-energy X-ray absorptiometry (DEXA)) and fat distribution (computed tomography (CT scan)), analyzed at baseline and after 12 weeks of treatment. The effect of intervention on the quality of life was examined using SF-12 questionnaire. Results: Consumption of AfperFit significantly increased the energy expenditure (p<0.01), visceral fat area (p<0.001) and visceral to subcutaneous fat ratio (p<0.01) compared to placebo group. Consequently, there was significant body weight loss and reduction in BMI of subjects in AfperFit group compared to placebo (p<0.01). The safety evaluation showed that biochemical and hematological parameters were in the normal range. Supplementation of AfperFit was well tolerated during the study and no adverse effects were observed. Conclusion: Overall, this study validates the health benefits of A. melegueta seed extract as fat burner and recommends its use as a functional ingredient to improve the quality of life and general health.

ViphyllinTM, a Standardized Black Pepper Extract Exerts Antihyperglycemic Effect and Improves Sciatic Nerve Conduction in High Fat Diet/Streptozotocin-Induced Diabetic Model Rats.

Purpose: Research on plant-based formulations has drawn considerable attention in the management of diabetic neuropathy (DN) for having lesser side effects than the synthetic counterparts. Here, we have investigated for the first time the therapeutic effects of a standardized Piper nigrum L., (black pepper) seed extract, ViphyllinTM in mitigating hyperglycemia and neuropathic pain of type 2 diabetes model rats. Methods: Type 2 diabetes was induced in male Wistar rats using high fat diet and a single dose of streptozotocin (60 mg/kg i.p.). The diabetic rats were orally administered with Viphyllin containing not less than 30% ß-caryophyllene (BCP), at 25 mg, 50 mg and 100 mg/kg/day doses for 6 weeks. Changes in body weight, fasting blood glucose (FBG), glucose tolerance, and blood biochemical parameters were measured. The nociceptive response to thermal stimulus (tail flick test) and sciatic nerve conduction velocity (NCV) were recorded at the end of study. Results: Viphyllin treatment markedly improved the body weight and glucose tolerance in diabetic rats. Also, the extract could significantly reduce the diabetes-induced elevation in FBG, liver and kidney indices. Further, Viphyllin dose-dependently increased the nociception latency in tail flick test compared to untreated diabetic rats (p<0.05). Viphyllin at 100 mg/kg significantly increased the NCV (44.12±1.91*** m/s vs diabetic control 25.80±1.88 m/s). The antioxidant enzyme activities in sciatic nerve tissue were considerably increased in Viphyllin-treated groups compared to diabetic control. A 6-week treatment with Viphyllin markedly reversed the pathological manifestations of diabetes in vital organs such as liver, kidney and pancreas. Conclusion: The study concludes that Viphyllin exerts antidiabetic effects and improves nerve conduction to mitigate neuropathic pain.

Viphyllin™, a standardized extract from black pepper seeds, mitigates intestinal inflammation, oxidative stress, and anxiety-like behavior in DSS-induced colitis mice.

Inflammatory bowel diseases (IBD) are the common health concern in populations across the world. Clinical evidence suggests that IBD, characterized by intestinal inflammation, is associated with neuronal manifestations to a greater extent. In this study, we have investigated the protective effects of Viphyllin™, a standardized black pepper (Piper nigrum) seed extract containing 30% ß-caryophyllene against dextran sodium sulfate (DSS)-induced colitis in mice. Oral pretreatment of Viphyllin at the 50 mg and 100 mg/kg doses significantly reversed the clinical symptoms of colitis in mice. Viphyllin markedly inhibited NLRP3 inflammasome activation and improved barrier function in colon tissue. Viphyllin further mitigated the DSS-induced anxiety-like behavior in mice. Interestingly, Viphyllin improved brain antioxidant status and promoted neuronal cell survival in colitis model mice. In conclusion, our findings strongly support the health claims of Viphyllin as a functional ingredient to deal with IBD and related neuronal symptoms. PRACTICAL APPLICATIONS: Prevalence of inflammatory bowel diseases is not uncommon in the modern lifestyle. Gut health is associated with neurological disorders that contribute substantially to the deterioration of quality of life and socioeconomic development. In this research work, the protective action of a black pepper seed extract standardized to 30% ß-caryophyllene (Viphyllin) is evaluated against Dextran sodium sulfate-induced experimental colitis model. Here we have demonstrated the beneficial role of Viphyllin in mitigating intestinal inflammation as a function of NLRP3 inflammasome inhibition. Further, the extract improves intestinal barrier function. In an important aspect of the study, we have provided the data on the effect of Viphyllin on neurological symptoms and brain health in colitis model mice.

ViphyllinTM, a Standardized Black Pepper Seed Extract Exerts Antinociceptive Effects in Murine Pain Models via Activation of Cannabinoid Receptor CB2, Peroxisome Proliferator-Activated Receptor-Alpha and TRPV1 Ion Channels.

PURPOSE: Plant-based natural products as anti-nociceptors have enormous potential as safer alternatives to conventional opiates and NSAIDS. Piper nigrum (black pepper) is one of the major culinary spices with medicinal attributes. METHODS: In the present study, the antinociceptive activity of a standardized black pepper seed extract (Viphyllin) containing not less than 30% ß-caryophyllene (BCP) was evaluated using pain models in mice, namely acetic acid-induced writhing test, formalin-induced paw licking test, hot plate test and tail flick test. Further, the antagonists SR141716A (0.1 mg/kg i.p.), AM630 (5 mg/kg i.p.), capsazepine (0.1 mg/kg body weight i.p.), and GW6471 (1 mg/kg i.p.) were used to evaluate the involvement of cannabinoid receptors CB1 and CB2, TRPV1 ion channel and PPARα receptor, respectively. Molecular docking (AutoDock 4.2) was used to study the interaction of BCP with the agonist-binding sites of the selected pain receptors. RESULTS: Viphyllin at 10 mg, 25 mg and 50 mg/kg (i.p.) significantly inhibited the writhings in mice as compared to untreated control group (p < 0.001). Further, Viphyllin at 50 mg/kg showed strong antinociceptive effect in formalin-induced paw licking test (p < 0.05). Pretreatment of mice with AM630 significantly reversed the antinociceptive activity of Viphyllin in both early and late phases of formalin test (p < 0.05). Administration of Viphyllin markedly increased the latency time of mice in hot plate test (p < 0.001). Further, Viphyllin markedly increased the latency time of tail flick compared to control group from 30 min to 90 min after treatment. AM630, Capsazepine, and GW6471 abolished the analgesic effect of Viphyllin. These findings clearly suggest the involvement of CB2 receptor, TRPV1 ion channel and PPARα receptor activation in Viphyllin-mediated antinociceptive activity. Docking score predictions further supported the possible involvement of BCP in the antinociceptive mechanism of Viphyllin. CONCLUSION: In conclusion, Viphyllin could be a natural pain-relieving agent involving safer pain signaling mechanisms, unlike conventional opiates and NSAIDs.

A phytosterol-enriched saw palmetto supercritical CO2 extract ameliorates testosterone-induced benign prostatic hyperplasia by regulating the inflammatory and apoptotic proteins in a rat model.

BACKGROUND: Benign prostatic hyperplasia (BPH) is a pathological condition affecting older men. BPH complications often lead to deterioration in the quality of life. Serenoa repens (Saw Palmetto) is used for treating lower urinary tract infections in traditional medicine. METHODS: This study was performed to compare the efficacy of ß-sitosterol enriched saw palmetto oil (VISPO) and conventional saw palmetto oil (SPO) extracted using supercritical fluid extraction, in alleviating the BPH complications using testosterone-induced BPH model rats. The animals received testosterone (5 mg/kg s.c.) with or without SPO and VISPO (200 and 400 mg/kg b.w.) or Finasteride (1 mg/kg b.w.) p.o. for 28 days. At the end of the experiment, overnight fasted animals were euthanized, blood samples collected for serum analysis of testosterone. Prostate tissue histomorphology was examined by hematoxylin and eosin (H&E) staining. Western blot analysis was performed using prostate tissue homogenates. RESULTS: VISPO exhibited superior efficacy compared to SPO as evident from the significant decrease in prostate weight to body weight ratio, serum testosterone level and increase in growth inhibition of prostate tissue compared to BPH group (p < 0.001). Histological examination of prostate tissue samples showed that VISPO treatment was comparatively better than SPO in improving the hyperplastic patterns. Further, VISPO significantly regulated the expression of inflammatory and apoptotic marker proteins in BPH rats. CONCLUSION: Our data provide experimental evidence that ß-sitosterol enriched saw palmetto oil could be higher efficacious in treating the BPH complications compared to the conventional saw palmetto oil preparations.