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Coffee is commonly consumed beverage in the world and it has been suggested to have beneficial effect. Chlorogenic acids (CGAs) are main ingredient of coffee beans which has been extensively used in nutraceuticals and medicine. Recently, various therapeutic effects of chlorogenic acids have been investigated. However, there are limited studies to investigate its anticancer properties. In the present study, we have used chlorogenic acid complex (CGA7) a decaffeinated water soluble green coffee bean extract to evaluate its cytotoxic effect on human and mouse cancer cell lines by using different approaches. From our results we found CGA7 treatment induces cell death in a dose and time dependent manner in different cancer cell lines. Further, CGA7 induced apoptosis was characterized by DNA fragmentation, PARP-1 cleavage, caspase-9 activation, and down regulation of Bcl-2, an anti-apoptotic protein and up regulation of pro-apoptotic protein BAX. Overall findings indicated that CGA7 complex a potent anticancer molecule found in green coffee beans could be a safe bioactive ingredient for prevention of cancer.

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 + (IC 50 = 19.88 µg/mL) and nitric oxide (IC 50 = 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-1β) 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.

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 VISPO TM , a standardized saw palmetto oil (2-3% β-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., Competing Interests: The investigational product VISPOTM is a proprietary extract manufactured by Vidya Herbs Pvt., Ltd. Heggar Venkataramana Sudeep, Richards Aleksander, Kuluvar Gouthamchandra, and Kodimule Shyamprasad are employed by Vidya Herbs Pvt. Ltd., and Sriram Rashmi s employed by the BGS Global Institute of Medical Sciences, Bangalore, India. Thomas V. Jestin s employed by Leads Clinical Research and Bio Services Private Ltd. (Bangalore, India). The authors declare no conflicts of interest., (© 2023 Sudeep et al.)

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% β-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., Competing Interests: All the authors are employed by Vidya Herbs Pvt Ltd., and hence declare potential conflicts of interest. The authors report no other potential conflicts of interest for this work., (© 2022 Venkatakrishna et al.)

β-caryophyllene (BCP), a natural sesquiterpene present in plants, is a selective agonist of cannabinoid receptor type-2 (CB2) of the endocannabinoid system. In this study, we have prepared an extract from Piper nigrum (black pepper) seeds using supercritical fluid extraction, standardized to contain 30% BCP (Viphyllin TM ). The beneficial effects of prophylactic treatment with Viphyllin on cognitive functions were demonstrated in Scopolamine-induced dementia model mice. Male Swiss albino mice (25-30 g) were administered with Viphyllin (50 mg and 100 mg/kg body weight p.o.) or donepezil (1.60 mg/kg) for 14 days. Subsequently, cognitive deficits were induced by treating the animals intraperitoneally with Scopolamine (0.75 mg/kg). The cognitive behavior of mice was evaluated using a novel object recognition test (NORT) and Morris water maze (MWM) test. The brain homogenates were studied for biochemical parameters including cholinesterase activities and antioxidant status. Western blot analysis was performed to investigate the mechanism of action. Viphyllin dose dependently improved the recognition and spatial memory and cholinergic functions in Scop-treated mice. The extract was found protective against Scop-induced oxidative damage and histopathologic changes in the brain. At 100 mg/kg Viphyllin markedly reduced the proBDNF/mBDNF ratio (p < .05) and augmented the TrkB expression (p < .01). Viphyllin (100 mg/kg) was found to be neuroprotective by reducing the Scop-induced upregulation of p-JNK and p-p38 MAPK proteins, Bax/Bcl-2 ratio, and caspase activation in the brain. Viphyllin also exerted anti-inflammatory effects by downregulating Cox-2, TNF-α, and NOS-2 in Scop-induced mice (p < .05). To summarize, our data encourage Viphyllin as a functional ingredient/dietary supplement for brain health and cognition. PRACTICAL APPLICATIONS: Black pepper is a culinary spice having several medicinal attributes. Essential oils in the seeds of the plant give aroma and flavor to it. Here we have prepared an extract from the seeds of black pepper using supercritical fluid extraction, characterized for the presence of β-caryophyllene (not <30%). This research work further validates the neuroprotective mechanism of the extract in Scopolamine-induced cognitive impairment model mice. The findings from this study strongly suggest the beneficial neuroactive properties of black pepper seed extract having the presence of BCP, a CB2 receptor agonist. It can thus be used potentially as a functional food ingredient for cognition and brain function., (© 2021 Wiley Periodicals LLC.)

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., Competing Interests: The authors are all employees of Vidya Herbs Pvt Ltd. The authors declare that they have no other potential conflicts of interest for this work., (© 2021 Gouthamchandra et al.)

Background: Withania somnifera is an Indian medicinal herb known for the multipotential ability to cure various therapeutic ailments as described in the ayurvedic system of medicine., Objective: In the present study, we have evaluated the antiproliferative activity of a standardized W. somnifera root extract (Viwithan) against different human and murine cancer cell lines., Materials and Methods: The cytotoxicity of Viwithan was determined using thiazolyl blue tetrazolium blue assay and crystal violet staining. The apoptotic changes in B16F1 cells following treatment with Viwithan were observed by acridine orange/ethidium bromide (AO/EB) staining and DNA fragmentation assay. The binding affinity of withanolides in Viwithan with antiapoptotic proteins B-cell lymphoma 2, B-cell lymphoma-extra large, and myeloid cell leukemia 1 (MCL-1) were studied using in silico approach., Results: The half maximal inhibitory concentration (IC50) values of Viwithan against liver hepatocellular carcinoma, Henrietta Lacks cervical carcinoma cells, human colorectal carcinoma cell line, and Ehrlich ascites carcinoma cells were 1830, 968, 2715, and 633 μg/ml, respectively. Interestingly, Viwithan was highly effective against B16F1 cells with an IC50 value of 220 μg/ml after 24 h treatment. The morphological alterations of apoptotic cell death were clearly observed in the AO/EB-stained cells after treatment with Viwithan. Viwithan induced late apoptotic changes in treated B16F1 cells as evident by the ladder formation of fragmented DNA in a time-dependent manner. The findings of molecular docking showed that withanolides present in Viwithan have a more binding affinity with the antiapoptotic proteins, particularly MCL-1., Conclusion: We have reported for the first time that Viwithan with 5% withanolides has a potent cytotoxic effect, particularly against B16F1 murine melanoma cells among the different cancer cell lines tested., Summary: The present study reports for the first time that Viwithan, a standardized 5% Withania somnifera root extract, has potent cytotoxicity against B16F1 murine melanoma cellsWe have investigated the in vitro cytotoxicity of Viwithan in different human and murine cancer cells. Interestingly, we found that Viwithan was particularly very effective against B16F1 melanoma cells with a half maximal inhibitory concentration value of 220 μg/mlThe microscopic observations following acridine orange/ethidium bromide staining and DNA fragmentation assays clearly indicated that Viwithan might initiate late apoptosis in B16F1 cellsThe binding affinity of withanolides in Viwithan with antiapoptotic proteins of B-cell lymphoma 2 family was predicted using AutoDock tool. The results from in silico studies indicated a plausible synergistic effect of withanolides attributing to the Viwithan-induced apoptosis through suppression of intrinsic pathway for carcinogenesis. Abbreviations used: MTT: Thiazolyl blue tetrazolium blue; DMSO: Dimethyl sulfoxide; BSA: Bovine serum albumin; DMEM: Dulbecco's minimum essential medium; NCCS: National Centre for Cell Science; PBS: Phosphate-Buffered Saline; HepG2: Liver hepatocellular carcinoma; HeLa: Henrietta Lacks cervical carcinoma cells; HCT-116: Human colorectal carcinoma cell line; EAC: Ehrlich ascites carcinoma cells; IC50: Half maximal inhibitory concentration; AO/EB: Acridine orange/Ethidium bromide; BCL-2: B-cell lymphoma 2; BCL-XL: B-cell lymphoma-extra large; MCL-1: Myeloid cell leukemia 1; PDB: Protein Data Bank; ANOVA: Analysis of variance., Competing Interests: There are no conflicts of interest.

Hepatitis C virus (HCV) is a leading cause of chronic viral hepatitis, but an effective vaccine is still not available to prevent infection. Use of neutralizing antibodies could be a potential therapeutic option. In this study, the presence of anti-HCV antibodies in HCV-infected patients was assessed from 50 patients and the presence of neutralizing antibodies was examined using 'hepatitis C virus-like particles'. Antibodies from two samples exhibited significant inhibitory activity, suggesting that these may neutralize viral infection. Antigenic determinants generating the neutralizing antibodies from these two samples were delineated by epitope mapping using the core, E1 and E2 regions and a stretch of 45 amino acid peptide (E2C45) derived from the C-terminal region of HCV-E2 protein (aa 634-679) was designed. Results suggest that this hitherto uncharacterized region has the potential to generate neutralizing antibodies against HCV and thus be effective in preventing virus entry into liver cells. Computational analysis of the structure of the modelled peptide (E2C45) suggested high conformational entropy for this region. Furthermore, E2C45 peptide-generated antibodies could block virus entry and monoclonal antibodies generated against this peptide could also significantly reduce virus replication in a cell culture system. It is possible that the inhibition could be partly due to a conformational alteration of the CD81-binding region, preventing virus attachment to liver cells. In conclusion, this work focused on the discovery of a novel epitope at the C terminus of E2 that induces potent neutralizing antibodies in HCV-infected patients.

Persistent infection of hepatitis C virus (HCV) can lead to liver cirrhosis and hepatocellular carcinoma, which are currently diagnosed by invasive liver biopsy. Approximately 15-20 % of cases of chronic liver diseases in India are caused by HCV infection. In North India, genotype 3 is predominant, whereas genotype 1 is predominant in southern parts of India. The aim of this study was to identify differentially regulated serum proteins in HCV-infected Indian patients (genotypes 1 and 3) using a two-dimensional electrophoresis approach. We identified eight differentially expressed proteins by MS. Expression levels of one of the highly upregulated proteins, retinol-binding protein 4 (RBP4), was validated by ELISA and Western blotting in two independent cohorts. We also confirmed our observation in the JFH1 infectious cell culture system. Interestingly, the HCV core protein enhanced RBP4 levels and partial knockdown of RBP4 had a positive impact on HCV replication, suggesting a possible role for this cellular protein in regulating HCV infection. Analysis of RBP4-interacting partners using a bioinformatic approach revealed novel insights into the possible involvement of RBP4 in HCV-induced pathogenesis. Taken together, this study provided information on the proteome profile of the HCV-infected Indian population, and revealed a link between HCV infection, RBP4 and insulin resistance., (© 2014 The Authors.)

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., (Copyright © 2012 Elsevier Masson SAS. All rights reserved.)

Three successive extracts of Clerodendrum infortunatum L. leaves have been studied for their potential as antioxidants in 1,1-diphenyl-2-picrylhydrazyl (DPPH) model. The scavenging activity of ethanol extract was found to be high when compared to petroleum ether and chloroform extracts. Hence, it was selected to evaluate the beneficial properties using in vitro and in vivo models. The antioxidant and its protective effects against CCl(4) induced oxidative stress in rats were significantly high. Further, to validate the traditional therapeutic claim, wound healing activity of the plant extracts was also carried out. Among the three extracts tested the petroleum ether and ethanol extracts exhibited a significant response. The presence of high antioxidant and pharmacological properties correlates to the total phenolic contents in the plant Clerodendrum infortunatum L., (Copyright © 2010 Elsevier B.V. All rights reserved.)

We have characterized a new class of 2-mercapto/2-selenobenzo[h]quinoline-3-carbaldehyde (3/4). Antibacterial potential of these compounds against a wide range of gram-positive and gram-negative bacteria was studied. The selenium containing compound 4 showed significant inhibition zone on Staphylococcus aureus (22.76+/-0.14), Bacillus subtilis (20.63+/-0.24), and Streptococcus pyogenes (19.54+/-0.20) over sulfur containing compound 3. To validate the ethnotherapeutic claims of the synthetic compounds in skin diseases, wound healing activity was studied, besides antioxidant activity to understand the mechanism of wound healing. The interaction behavior of these compounds with DNA was investigated by absorption spectra (obtained K(b) constant for 3 is 2.7x10(5) and for 4 is 3.8x10(6)), viscosity, and thermal denaturation studies. Finally, the results show that the DNA intercalated 3/4 compounds are strong antioxidants; they show significant wound healing activity and protect oxidative DNA damage from harmful free radical reactions.