Pharmacological Research - Natural Products最新文献

Background

Despite several initiatives, research, and advancement, the prevalence of essential hypertension keeps on increasing globally and its adverse impacts remain a public health concern.

Aim

To assess the efficacy and safety of a Unani polyherbal formulation in patients of Stage-2 hypertension.

Methods

An open-label, randomized, standard controlled clinical study was conducted in the Department of Moalejat, Ayurvedic and Unani Tibbia College Hospital, Karol Bagh, New Delhi, during 2021–2022.

Both male and female patients, aged 18–65 years with systolic blood pressure ≥140 mmHg and ≤180 mmHg or diastolic blood pressure ≥ 90 mmHg and ≤120 mmHg, were enrolled in the study. Test group patients were treated with Unani Polyherbal formulation (1100 mg daily in two divided doses in a capsule form) while control group patients were given Tablet Telmisartan (40 mg) once daily for 3 weeks.

Results

A total of 60 patients of Stage-2 hypertension (30 in test group and 30 in control group) completed the study, out of them 24 patients in the test group and 25 patients in the control group achieved the target Blood Pressure of 120/80 (±10) mmHg. The mean Blood Pressure of test and control group patients at the end of the study was calculated as 132.86/90.06 mmHg and 131.09/91.92 respectively.

Conclusion

The test drug (Unani polyherbal formulation) was well tolerated and found as safe and efficacious as the control drug (Telmisartan).

Marasmius tax sp, belonging to the Marasmiaceae family, is a mushroom species that demands extensive study of its medicinal values with scientific evidence. Mycochemical profiling of methanolic extract of Marasmius sp was performed with Gas Chromatogram-Mass Spectroscopy (GC-MS) and presence of eighteen organic compounds were confirmed. The extract demonstrated promising results in terms of its ability to inhibit α-amylase and scavenge DPPH free radicals, indicating its potential as an antidiabetic and antioxidant. The anti-diabetic property of the mycochemicals was further explored by employing inverse molecular docking analysis for the identified mycochemicals against 18-diabetes associate targets. The inverse docking analysis showed four mycosterol compounds with a strong binding affinity against all the targets, while all 18 compounds displayed considerable binding scores (-6.0 to −10.0 kcal/mol) against three crucial targets responsible for the mode of antidiabetic effect, suggesting the extract to have a multi-target, multi-drug effect in treating diabetes. All the identified mycochemicals were evaluated for their drug-likeness, pharmacokinetics, adverse side effects, and bioactivity. Out of the 18 molecules, 17 were found to be bioactive, with 5 of them showing no predicted adverse effects. Further, the structure-property relationship of the mycosterols have been explored using Density Functional Theory (DFT) based calculations. Frontier molecular orbitals, electrostatic potential surfaces and global descriptor analysis were carried out to understand the stability and chemical reactivity of the selective mycochemcials.

Introduction

Clerodendrum colebrookianum Walp., also known as East-India glory bower is indigenous to North-eastern region, West Bengal and Sikkim of India. The plant is used in folk medicine for treating different diseases- hypertension, diabetes, dysentery, diarrhoea, gastric and bowel disorders. In North Eastern part of India, the plant finds a unique place amongst the commonly consumed vegetables with potent health benefits. The present study aims at deciphering the traditional, pharmacological potential of the plant with a view on future line of research. The review article also discusses the probable mechanism of action for the plant’s significance as potent antihypertensive, hypolipidemic, antioxidant, anti-inflammatory, anti-obesity, anthelmintic, antimicrobial, antistress, antipyretic and hepatoprotective activity.

Method

Primary data collected from village head, traditional healers, local vendors of different tribes. Scientific literature from year 1979 was reviewed, using electronic databases, like- Pub-Med, Pub-Chem, Sci-hub, NCBI and NIST chemistry web book.

Results

Five novel steroid derivatives (colebrin A-E) were identified for the first time in C. colebrookianum leaf extract, besides clerosterol3β-O- [β-D-glucoside], glyceryl- 1-docosoicate, acteoside, martinoside, osmanthuside B₆, oleanolic acid, maslinic acid, 2-O-methylalluloside, 3β-acetoxyurs-11-cn-28 and bis (2-ethylhexyl) phthalate. Pharmacological application includes hypolipidemic, antihypertensive, antioxidant, anti-inflammatory and analgesic, hepatoprotective, antiobesity, anthelmintic, CNS depressant, antimicrobial, antistress and antipyrectic activity; metabolic syndrome lowering and inducing longer sleep time ability.

Conclusion

Clinical investigations supported the conventional wisdom that the leaf extract can treat hypertension and this approach should be used to assess the qualities of other diseases as well. Further, in-depth research is also required to fully understand the mechanism underlying the potential for anti-diabetic effects.

Introduction

Rhynchostylis retusa (L.) Blume lies in the heart of majestic Himalayan mountains and is well-documented in Traditional System of Medicine. R. retusa roots are used to treat rheumatic disease, asthma, tuberculosis, epilepsy, kidney, and menstrual disorders. Besides earlier reports, current study was focused to investigate locational variations of polyphenols, antioxidant, antimicrobial and cytotoxicity activities of R. retusa roots.

Method

R. retusa roots of four locations of Himachal Pradesh, India were used in the current study. The targeted polyphenols were determined using UPLC-PDA while total phenolic and total flavonoid contents were by spectroscopic method. The antioxidant activity was assessed by DPPH ֹ and ABTS ֗⁺ assays. Antimicrobial activity was performed against gram-positive (Bacillus subtilis and Staphylococcus aureus) and gram-negative bacteria (Salmonella typhimurium and Escherichia coli) while cytotoxicity activity was against HT29 cancer cell line.

Result

In present study, 50 % ethanol revealed higher yield in Kangra region (1375 m; 32.1109° N, 76.5363° E) sample followed by water and ethanol. Among all extracts, gallic acid and protocatechuic acid were most abundant phenolic acids. The highest TPC and TFC were found in the ethanol extract of Bilaspur (680 m; 31.33°N 76.75°E) sample (155.58±6.92 mg GAE/g and 262.25±8.32 mg RE/g) and Kangra (135.64±4.36 mg GAE/g and 281.75±4.38 mg RE/g) regions, respectively. The ethanol extract from Hamirpur (790 m 31.6862° N, 76.5213° E), exhibited highest antioxidant activity (IC₅₀ 33.31±0.72 µg/mL and 12.45±0.68 µg/mL), in DPPH ֹ and ABTS ֗⁺ assays, respectively. The ethanol extract from Bilaspur (5 mm and 3 mm ZOI for B. subtilis and S. aureus), Kangra (4 mm and 2.5 mm for B. subtilis and S. aureus), and Hamirpur showed most potent antimicrobial activity. Whereas, Mandi (760 m; 31.7087° N, 76.9320° E) samples showed least potential as compared to other targeted locations. Further, ethanol extracts of all locations were found most effective in terms of their cytotoxic activity against HT29 cancer cell lines.

Conclusion

Current investigations illuminate ethanol's pivotal role in extracting polyphenols and unleashing the pharmacological potential of R. retusa root extract. Thus, ethanol may be considered as a suitable solvent to extract, fractionate and isolate the bioactive compounds for health perspectives. Findings also suggested that Kangra region (1375 m; 32.1109° N, 76.5363° E) sample has highest potential and can be focused for further study.

Background

Cryptolepis buchanani Roem. & Schutt. (Asclepiadaceae) used in traditional medicines to cure various illnesses such as rickets in children, bone fractures, paralysis, muscle tension, and arthritis.

Objective

The current review aims to assemble the maximum information possible regarding ethnobotanical usage, phytochemical constituents, and pharmacological activities of this important plant species.

Methodology

The information related to this review was retrieved from various online databases including SCOPUS, Web of Science/Knowledge, PubMed, Elsevier Science Direct, and Mendeley. The taxonomic data was validated through “The World Flora Online” (http://www.worldfloraonline.org/) and “Medicinal Plant Names Services” (http://mpns.kew.org/).

Results

This review revealed that overall, a total number of 48 compounds have been isolated from C.buchanani Roem. & Schutt. belonging to different chemical groups such as alkaloids, flavonoids, fatty acids, phenolics, terpenoids, lignans, tannins, and many others. Although compounds are reported from different parts such as leaf, stem, root, and latex, but highest compounds were from the leaf extract. Moreover, both crude extracts and purified compounds of C.buchanani Roem. & Schutt. are reported to possess a wide range of biological activities such as antioxidant, anticancer, anti-inflammatory, antimicrobial, hepatoprotective, anti-rheumatic, anti-osteoporosis, and insecticidal activities.

Conclusion

This collective data on the pharmaceutical potentiality of the plant may facilitate future research in drug discovery.

Many studies have revealed that sea fish is a rich source of nutrients, especially protein and there peptide. In this study, antidiabetic activity of the fish masses of three sea-fishes ‘volavetki’ (Panna microdon, Bleeker 1849), ‘ruli’ (Coilia dussumieri, Valenciennes 1848), ‘tapra’ (Opisthopterus tardoore, Cuvier 1829) and one fresh-water fish ‘murola’ (Amblypharyngodon mola, Hamilton 1822),evaluated high lipid diet (HLD) and STZ induced Type 2 Diabetic Mellitus (T2DM) rats. Supplementation of sea-fish masses and antidiabetic effect was monitored by fasting plasma blood glucose and HbA1c. Also, insulin, c-peptide, glucagon-like peptide-1, dipeptidyl peptidase-IV, glucokinase, glucose-6 phosphatase, superoxide dismutase, glutathione peroxidase, catalase, plasma total cholesterol, low density lipoprotein, triglycerides, high density lipoprotein and histopathology of free radical activity of pancreatic tissues were evaluated. Out of four fish masses, volavetki sea fish masses oral supplementation resulted in significant reduction of plasma blood glucose, HbA1c of T2DM rat. All other parameters in T2DM rats were returned to near normal by treatment of volavetki sea fish mass. Our findings strongly indicated that volavetki sea fish highly showed antidiabetic activity.

Silkworm pupae oils have emerged as a great source of functional fatty acids in recent days. However, certain wild races of silkworm pupae are yet to be explored to know their potentiality in human health. Therefore, the current study aims to validate their efficacy towards therapeutic values through a comparative analysis between two races of silkworm pupae oil, namely, oak tasar pupae oil (OTPO) and mulberry silkworm pupae oil (MSPO). The pupae oils were extracted using the Soxhlet method followed by the fatty acids profile and functional group analysis using Gas Chromatography Mass Spectrometry (GC-MS) and Fourier Transform Infrared (FTIR) respectively. The radical scavenging activities of both oils were determined by 2,2-azino-bis-3-ethylbenzothiazoline-6-sulphonic acid (ABTS) and 1,1-diphenyl-2-picryl-hydrazyl (DPPH). Further, both the oils were tested for their antibacterial activity using the agar well diffusion method. The oil yield was recorded as 24.62 ± 0.341 % and 24.16 ± 0.764 % for OTPO and MSPO respectively. GC-MS analysis revealed the presence of conjugated linoleic acid (ω-6 fatty acids) as a prominent component in both OTPO (23.49 %) and MSPO (37.99 %), followed by other bioactive constituents in minor amounts. The FTIR analysis and chemical properties correlated to the peaks of common edible oils. Meanwhile, MSPO (150.50±0.45 μg/mL) had a higher TPC when compared to OTPO (44.599±0.514 μg/mL). Moreover, OTPO showed better radical scavenging properties than MSPO. Further, OTPO exhibited antibacterial activity against E. coli, E. cloacae, and S. typhi at different dilutions. However, MSPO was found to be ineffective against the tested bacterial strains. In conclusion, the present study indicates that both oils could be used as an alternative edible oil source as well as a therapeutic agent in the near future.

Essential oil nanoemulsions (EONs) of two wild cinnamons, Cinnamomum heyneanum (CH) and Cinnamomum Palghatensis (CP), were formulated, characterized and investigated for their antidiabetic activity. Leaf essential oils (EOs) were extracted and characterized by GC-MS and GC-FID. Two sets of EONs were formulated and characterized by zeta analyzer, viscometer and TEM. Antioxidant activity was studied using DPPH, ABTS, superoxide, hydroxyl and hydrogen peroxide assays. Antidiabetic activity was evaluated by α-amylase inhibition, α-glucosidase inhibition, glucose uptake and glucose-stimulated insulin secretion assays. In silico studies were performed to support the efficacy. Methyl eugenol (60.3 %), safrole (27.8 %) in CH EO and bicyclogermacrene (19.5 %), (E)-caryophyllene (14 %) in CP EO were major components. Of two sets of EONs, 1:2 ratio showed better hydrodynamic average diameter [CH 42.9±0.78 nm & CP 27.9±1.70 nm] and better zeta potential [CH −38.4±0.85 mV & CP −38.4±0.45 mV (1st day)]. TEM observation showed that 1:2 ratio EONs were spherical with an average diameter of 85 nm (CH) and 8.98 nm (CP). Both CH and CP showed remarkable antioxidant activity. CP showed better α-glucosidase inhibition (IC50 0.599±0.008 mg/mL), enhanced glucose uptake (0.53±0.08 fold vs. control) and insulin secretion (1.40±0.06 fold vs. control). In silico analysis reveals that all major components of CH and CP interact with key residues of the protein targets associated with diabetes, α-amylase, α-glucosidase, insulin receptor, Glugagon like peptide1 Receptor and Glut 4. In vitro and in silico studies revealed that EON of CH and CP have pharmacological properties due to the presence of various compounds against diabetes mellitus.

As of 2021, an estimated 537 million people had diabetes worldwide, accounting for 10.5 % of the adult population, with type 2 making up about 90 % of all cases. The common antidiabetic drugs have several problems like hypoglycemia, skin rash and itching, weight gain, kidney complications, etc. So, there is a need to explore safer alternative medications from natural sources. This study examines the antidiabetic potential and metabolomic profiling of Conium maculatum, a homeopathic medicine prescribed for diabetic patients. Potent DPPH scavenging of the sample was observed with an IC₅₀ value of 75.05 ± 6.33 μg/mL. α-Amylase and α-glucosidase enzyme inhibition by the mother tincture of Conium maculatum was evaluated through in-vitro studies, highlighting effective antidiabetic activity with IC₅₀ values of 86.53±1.76 μg/mL and 124±7.903 μg/mL, respectively. Metabolomic profiling of the mother tincture of Conium maculatum was done by LC-MS/MS to identify a total of 47 phyto-compounds that were subjected to ADMET profiling, followed by in-silico docking and MDS with target receptors associated with diabetes. Six compounds were short-listed for in-silico docking studies with five target proteins, α-amylase, α-glucosidase, GLUT-4, GLP-1, and IRS1. Three compounds, Schidigeragenin B, 10-oxo-11-octadecen-13-olide, and Distichonic acid A, showed strong binding affinities to these protein receptors, crucial for diabetes remediation. Among these compounds, Schidigeragenin B, a novel triterpenoid shows the strongest binding affinities towards these receptors, and the ADMET properties highlighted its drug likeness. Conclusively, the present study identified Schidigeragenin B, resourced from the mother tincture of Conium maculatum, as the potent bioactive antidiabetic molecule for combating diabetes.

Introduction

Ayurveda, a traditional Indian medicinal system, possesses extensive knowledge regarding the therapeutic attributes of herbs and their synergistic interactions with various substances. Within Ayurveda literature, numerous formulations incorporate herbs into dairy products such as medicated ghee (Ghrita), curd (Dadhi), buttermilk (Takra), etc. This review delves into the pharmacological properties of over 65 medicinal herbs, their natural habitats in India, and their integration into contemporary milk products and the dairy industry, emphasizing the potential synergistic advantages they offer.

Aim of the review

To provide insights into the utilization of herbs in dairy products, bridging ancient Ayurveda knowledge with contemporary scientific understanding. The review targets researchers, industry stakeholders, and healthcare professionals interested in harnessing the health benefits of herb-infused dairy products.

Materials and methods

A systematic literature search across databases and official dairy industry websites identified relevant studies on Ayurveda herbs in dairy. Keywords like 'Ayurveda,' ‘herbs', ‘pharmacology’ and 'dairy,' guided the search, excluding Ayurveda medicated ghee products to streamline focus.

Results

The review reveals the immunomodulatory, antioxidant, antimicrobial, and anti-inflammatory properties of herbs like turmeric, holy basil, Ashwagandha, ginger, and others when integrated into dairy. These herbs enhance dairy product quality, overall nutritional value, and shelf life. Incorporating more than 65 Ayurveda herbs into dairy products offers a promising avenue for augmenting their therapeutic potential and enhancing consumer health. The synergistic effects of herbs with dairy constituents contribute to the development of innovative products with enhanced functionality and nutritional value.

Conclusion

While previous research has explored the application of herbs in dairy products, further investigation is warranted to optimize their effects and promote consumer well-being. Continued research endeavours are imperative to unlock the full potential of herbs in the dairy industry and leverage their benefits on a global scale. Furthermore, individuals are encouraged to incorporate dairy products infused with Ayurveda herbs to enhance immunity and maintain overall health and fitness, aligning with the fundamental principle of Ayurveda literature that, "Prevention is always better than cure."