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1.
Clin Cosmet Investig Dermatol ; 16: 3251-3266, 2023.
Article in English | MEDLINE | ID: mdl-38021422

ABSTRACT

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.

2.
Pharm Biol ; 61(1): 1211-1221, 2023 Dec.
Article in English | MEDLINE | ID: mdl-37585723

ABSTRACT

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.


Subject(s)
Echinacea , Mice , Male , Animals , Echinacea/chemistry , Nitric Oxide , Cytokines , Plant Extracts/pharmacology , Plant Extracts/chemistry , Macrophages , Immunosuppression Therapy , Immunity
3.
J Pain Res ; 15: 355-366, 2022.
Article in English | MEDLINE | ID: mdl-35153513

ABSTRACT

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.

4.
J Inflamm Res ; 14: 859-868, 2021.
Article in English | MEDLINE | ID: mdl-33737826

ABSTRACT

OBJECTIVE: It is well known that regular turmeric extract with 95% curcuminoid is comprised of curcumin (70.07%), desmethoxycurcumin (20.28%), and bisdemethoxycurcumin (BDMC) (3.63%). In the current study for the first time, we have enriched about 3% of bisdemethoxycurcumin (BDMC) to 70% as well as named it as REVERC3 and compared anti-inflammatory activity with regular turmeric extract using in vitro and in vivo models of inflammation. METHODS: To reveal the potential anti-inflammatory mechanism of action, we investigated nitric oxide (NO) scavenging, xanthine oxidase, and lipoxygenase inhibitory activity, further determined the level of pro-inflammatory cytokines, such as interleukin 6 (IL-6), tumor necrosis factor (TNF-α) and major inflammatory mediators like cyclooxygenase (COX-2) and inducible nitric oxide synthase (iNOS), inhibition in lipopolysaccharide (LPS) induced inflammation in RAW macrophage cells. In the other hand, a carrageenan-stimulated inflammatory rat model was carried out. RESULTS: Our study findings exhibited a significant anti-inflammatory activity of REVERC3 together with nitric oxide (NO), xanthine oxidase, and lipoxygenase inhibition. Further, we attenuated the levels of cyclooxygenase (COX-2), inducible nitric oxide synthase (iNOS), interleukin (IL-6) and tumor necrosis factor (TNF-α) expressions in the LPS-elicited RAW macrophage cells. REVERC3 showed a potential anti-inflammatory activity by inhibiting carrageenan induced paw edema after 4 hr at the dose of 100mg/kg body weight. CONCLUSION: Thus, our findings collectively indicated that the REVERC3 could efficiently inhibit inflammation compared to regular turmeric extract. Since bisdemethoxycurcumin is a stable molecule it could be effectively used in the applications of health care and the nutraceutical industry, indeed which deserves further investigations.

5.
Eur J Med Chem ; 55: 467-74, 2012 Sep.
Article in English | MEDLINE | ID: mdl-22877623

ABSTRACT

A series of 5-bromo-2-(3,5-diaryl-4,5-dihydro-1H-pyrazol-1-yl)pyrimidine were prepared under conventional heating as well as microwave reaction condition. The newly synthesized compounds were characterized on the basis of elemental, spectral and single crystal X-ray studies. These new compounds were screened for their antioxidant, anti-inflammatory and analgesic activities. Some of these compounds exhibited potent biological activities compared to the standard drug.


Subject(s)
Pyrazoles/chemical synthesis , Pyrazoles/pharmacology , Pyrimidines/chemistry , Analgesics/chemical synthesis , Analgesics/chemistry , Analgesics/pharmacology , Animals , Anti-Inflammatory Agents/chemical synthesis , Anti-Inflammatory Agents/chemistry , Anti-Inflammatory Agents/pharmacology , Chemistry Techniques, Synthetic , Free Radical Scavengers/chemical synthesis , Free Radical Scavengers/chemistry , Free Radical Scavengers/pharmacology , Free Radicals/chemistry , Mice , Models, Molecular , Molecular Conformation , Pyrazoles/chemistry
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