In Vitro Study on Spermicidal Action of Hydro-methanol Extract of Tinospora cordifolia (Willd.) Stem in Rat and Human Sperm: a Comparative Analysis.

Human fertility regulation is a major way to control overpopulation. In this perspective, this study emphasized the in vitro effect of hydro-methanol extract of Tinospora cordifolia (TCHME) stem for spermicidal and reproductive hypo-functions using human and rat samples. Control, 0.5-, 1-, and 2-mg TCHME-charged groups were considered to assess the relevant parameters. Levels of spermiological parameters like sperm motility, viability, the integrity of plasma and acrosomal membrane, and nuclear chromatin decondensation were significantly reduced (p < 0.05) in the dose- and duration-dependent TCHME-charged groups compared to the control. The inhibitory concentration 50 (IC50) of TCHME on motile human and rat sperms were 0.8 and 0.4 mg/ml, respectively. Testicular androgenic key enzymes and antioxidant enzymes (human sperm pellet, testes, and epididymis of rat)' activities were significantly diminished (p < 0.05), while antioxidant enzymes' activities were significantly elevated (p < 0.05) in renal and insignificantly (p > 0.05) elevated in hepatic tissues of rat in TCHME-charged groups compared to the control. Significant elevation (p < 0.05) of thiobarbituric acid reactive substances (TBARS)' level in human sperm pellet, testes, and epididymis of rats and significant diminution (p < 0.05) in TBARS levels of liver and kidney were observed in TCHME-charged groups. It focused that TCHME is more potent for stress imposition on reproductive tissues and sperm compared to the other tested tissues. Non-significant alterations (p > 0.05) in glutamic oxaloacetic transaminase (GOT) and glutamic pyruvic transaminase (GPT) activities in the said organs of rat indicated its non-toxic effect. It highlighted that TCHME possesses spermicidal and reproductive tissue-specific effects which strengthen the possibilities of male contraceptive development from it.

Antiapoptotic and antioxidative efficacy of rhizomes of Curcuma amada on the management of diabetes-induced male infertility in albino rat: An effective fraction selection study.

Men with diabetes have negative effects on reproduction that causes sexual dysfunction. Medicinal plants are non-toxic and much safer than synthetic drugs because regular use of synthetic drugs shows long-term side effects. Curcuma amada (Roxb) is a medicinal plant used in Ayurveda and Unani medicinal systems in India. The goal of this study is to rummage the potential efficiency of the most potent solvent fraction of effective extract of hydro-methanol 60:40 of C. amada rhizome on male gonadal hypofunction in streptozotocin-induced diabetic rat. Diabetes-induced testicular hypofunction was evaluated by glycemic, spermiological, biochemical, genomic, flow cytometric, and histology of testicular tissue. The n-hexane, chloroform, ethyl-acetate, and n-butanol solvent fractions of the said extract were administrated for 4 weeks at 10 mg dose/100 g body weight/day. Among all the used fractions, the ethyl-acetate solvent fraction-treated group showed maximum recovery in serum insulin (177.42%), sperm count (92.84%), sperm motility (97.15%), and serum testosterone (164.33%). The diabetic rats treated with ethyl-acetate solvent fraction also exhibited the maximum resettlement in flow cytometric analysis of sperm viability (55.84%) and sperm mitochondrial integrity (149.79%), gene expression patterns of key markers for androgenesis (Δ5, 3ß-HSD 87.50%, and 17ß-HSD 74.66%) and apoptosis (Bax 44.63%, Bcl-2 54.03%, and Caspase-3 35.77%) along with testicular histology. The ethyl-acetate fraction contains alkaloids, flavonoids, and polyphenols where all of these components are not present in other fractions, may be the most effective cause for the recovery of diabetes-linked oxidative stress-mediated testicular hypofunctions. PRACTICAL APPLICATIONS: Nowadays worldwide, the use of synthetic drugs are reduced due to their toxic effect. At present, synthetic drugs are replaced by several herbal drugs, the natural source of medicine which has many therapeutic values. C. amada has strong antioxidant activity due to the presence of bio-active compound(s) that can able to manage streptozotocin-induced diabetes linked to oxidative damage of male gonadal organs. Therefore, these bio-active compound(s)-containing said medicinal plant may use as a good source of antioxidative food in the food industry as nutraceuticals and in pharmaceutical industries for the development of the herbal drug to manage diabetes-linked male gonadal hypofunctions. At present, WHO also gives emphasis for developing one drug-multi-disease therapy. From such a viewpoint, this active fraction-containing phytomolecules may have corrective efficacy against diabetes as well as oxidative stress-linked testicular complications.

Effective Inhibition of SARS-CoV-2 Entry by Heparin and Enoxaparin Derivatives.

Severe acute respiratory syndrome-related coronavirus 2 (SARS-CoV-2) has caused a pandemic of historic proportions and continues to spread globally, with enormous consequences to human health. Currently there is no vaccine, effective therapeutic, or prophylactic. As with other betacoronaviruses, attachment and entry of SARS-CoV-2 are mediated by the spike glycoprotein (SGP). In addition to its well-documented interaction with its receptor, human angiotensin-converting enzyme 2 (hACE2), SGP has been found to bind to glycosaminoglycans like heparan sulfate, which is found on the surface of virtually all mammalian cells. Here, we pseudotyped SARS-CoV-2 SGP on a third-generation lentiviral (pLV) vector and tested the impact of various sulfated polysaccharides on transduction efficiency in mammalian cells. The pLV vector pseudotyped SGP efficiently and produced high titers on HEK293T cells. Various sulfated polysaccharides potently neutralized pLV-S pseudotyped virus with clear structure-based differences in antiviral activity and affinity to SGP. Concentration-response curves showed that pLV-S particles were efficiently neutralized by a range of concentrations of unfractionated heparin (UFH), enoxaparin, 6-O-desulfated UFH, and 6-O-desulfated enoxaparin with 50% inhibitory concentrations (IC50s) of 5.99 µg/liter, 1.08 mg/liter, 1.77 µg/liter, and 5.86 mg/liter, respectively. In summary, several sulfated polysaccharides show potent anti-SARS-CoV-2 activity and can be developed for prophylactic as well as therapeutic purposes.IMPORTANCE The emergence of severe acute respiratory syndrome coronavirus (SARS-CoV-2) in Wuhan, China, in late 2019 and its subsequent spread to the rest of the world has created a pandemic situation unprecedented in modern history. While ACE2 has been identified as the viral receptor, cellular polysaccharides have also been implicated in virus entry. The SARS-CoV-2 spike glycoprotein (SGP) binds to glycosaminoglycans like heparan sulfate, which is found on the surface of virtually all mammalian cells. Here, we report structure-based differences in antiviral activity and affinity to SGP for several sulfated polysaccharides, including both well-characterized FDA-approved drugs and novel marine sulfated polysaccharides, which can be developed for prophylactic as well as therapeutic purposes.

Antidiabetic and antioxidative efficacy of the constituents present in the fraction solvents of Curcuma amada rhizomes: An experimental study on the diabetic rat model.

All over the world, the prevalence of diabetes mellitus is increasing. The main goal of this experiment was to identify the most effective fraction of aqueous-methanol extract of Curcuma amada rhizome for its antidiabetic and antioxidative properties. The fractions (n-hexane or chloroform or ethyl-acetate or n-butanol) of aqueous-methanol extract were administered to the streptozotocin-induced diabetic groups at a dose of 10 mg/100 g body weight/day for 4 weeks. The antidiabetic and antioxidative efficacies of the fractions on glycemic, enzymatic, genomic, and histological sensors and pancreatic ß-cells population and general toxicity were assessed. After the fraction treatment, out of the fraction used, the significant recovery in most sensors was noted at the ethyl-acetate fraction in glycemic, enzymatic, genomic, ß cells population, diameter of the pancreatic islet and toxicity level. In conclusion, it may be stated that the ethyl-acetate fraction of C. amada was the most effective solvent in this study. PRACTICAL APPLICATIONS: The ethyl-acetate fraction of aqueous-methanol extract of Curcuma amada has antidiabetic property, it gives a clue to the herbal medicine manufacturing company to produce phytotherapeutic drugs to cure the complication related to diabetes.

Antidiabetic and antioxidative properties of the hydro-methanolic extract (60:40) of rhizomes of Curcuma amada roxb. (Zingiberaceae) in streptozotocin-induced diabetic male albino rat: a dose-dependent study through biochemical and genomic approaches.

Background Curcuma amada is the most popular traditional medicine in India for the treatment of diabetes. The present study aimed to focus the antidiabetic and antioxidative activity of C. amada through the analysis of biochemical and genomic levels in a dose-dependent manner in streptozotocin-induced male adult rat. Method Streptozotocin-induced diabetic rats were administered orally with hydro-methanolic extract of C. amada at the dose of 10, 20, 40 and 80 mg/100 g body weight of rats for 28 days. The antidiabetic and antioxidative efficacy of the extract on glycemic, enzymatic, genomic and histological sensors along with toxicity study was investigated. Results The result showed a significant antidiabetic and antioxidative effect of the extract at dose-dependent manner. The significant recovery of fasting blood glucose level, serum insulin, activity of carbohydrate metabolic enzymes and antioxidative enzymes in extract-treated diabetic group as compared to untreated diabetic group were noted. After the extract treatment, the size of pancreatic islet and cell population densities were significantly increased. Activities of glutamate oxaloacetate transaminase and glutamate pyruvate transaminase in liver were significantly recovered along with the correction of Bax and Bcl-2 gene expression in hepatic tissue after the extract treatment in diabetic rats in respect to untreated diabetic group. Out of all the doses, the significant effects were noted at the dose of 20 mg/100 g body weight which has been considered as threshold dose in the concern. Conclusion It may be concluded that the significant and corrective effect in most of the sensors was noted at the minimum dose of 20 mg/100 g body weight of hydro-methanolic extract of C. amada without producing any toxicity.